Page last updated: 2024-12-06

6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID40634
CHEMBL ID153
CHEBI ID82625
SCHEMBL ID3226
MeSH IDM0056270

Synonyms (82)

Synonym
OPREA1_727377
smr001233218
MLS002153860
BRD-A17846016-001-03-0
einecs 258-422-8
trolox c
6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid
3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2h-1-benzopyran-2-carboxylic acid
2h-1-benzopyran-2-carboxylic acid, 3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-, (+-)-
brn 5052542
PRESTWICK_855
NCGC00179534-01
PRESTWICK2_000530
PRESTWICK3_000530
BSPBIO_000519
2h-1-benzopyran-2-carboxylic acid, 3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-
53188-07-1
trolox ,
6-hydroxy-2,5,7,8-tetramethyl-chromane-2-carboxylic acid
(+/-)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, 97%
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
PRESTWICK1_000530
PRESTWICK0_000530
SPBIO_002440
BPBIO1_000571
3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2h-1-benzopyran-2- carboxylic acid
56305-04-5
(r,s)-6-hydroxy-2,5,7,8-tetramethyl-2-chromanecarboxylic acid
6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2h-chromene-2-carboxylic acid
chebi:82625 ,
CHEMBL153
6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydrochromene-2-carboxylic acid
H0726
HMS1569J21
HMS2096J21
HMS2230A15
S3665
s18ul9710x ,
unii-s18ul9710x
bdbm50359629
FT-0621156
AKOS015856256
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid, (+/-)-
(+/-)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
(+/-)-trolox
trolox [inci]
trolox [mi]
2h-1-benzopyran-2-carboxylic acid, 3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-, (+/-)-
HMS3369E20
CCG-207912
SCHEMBL3226
6-hydroxy-3,4-dihydro-2,5,7,8-tetramethyl-2h-1-benzopyran-2-carboxylic acid
6-hydroxy-2,5,7,8-tetramethyl-chroman-2-carboxylic acid
(6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)carboxylic acid
6-hydroxy-2,5,7,8-tetramethychroman-2-carboxylic acid
(+/-)- 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
6-hydroxy-2,5,7,8-tetramethyl-2-chromanecarboxylic acid #
HY-101445
CS-8035
GEO-03688
(+/-)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid
mfcd00006846
6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2h-1-benzopyran-2-carboxylic acid
SR-01000841227-2
sr-01000841227
trolox(tm)
6-hydroxy-2,5,7,8-tetramethyl-2-chromancarboxylic acid
HMS3713J21
BBL103047
STL556856
FT-0770514
BCP16474
DTXSID60866306
3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2h-1-benzopyran-2-carboxylic acid;
(s)-(-)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylicacid
Q245489
AS-30121
BRD-A17846016-001-07-1
HMS3885K19
trolox is also know as 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid.
EN300-370592
Z3013814504

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In isolated perfused livers from fasted rats, sodium orthovanadate (2 mmol/l) led to toxic responses including reduction of oxygen consumption, release of cytosolic (glutamate-pyruvate-transaminase (GPT) and lactate dehydrogenase (LDH)) and mitochondrial (glutamate-dehydrogenase (GLDH)) enzymes, intracellular accumulation of calcium, a marked depletion of glutathione (GSH) and an enhanced formation and release of thiobarbituric acid- (TBA) reactive material."( Effect of antioxidants on vanadate-induced toxicity towards isolated perfused rat livers.
Kayser, E; Strubelt, O; Younes, M, 1991
)
0.28
" In contrast to arachidonic acid, oleic acid was not toxic to the Hep G2-MV2E1-9 cells."( Cytotoxicity and apoptosis produced by arachidonic acid in Hep G2 cells overexpressing human cytochrome P4502E1.
Cederbaum, AI; Chen, Q; Galleano, M, 1997
)
0.3
"Ethanol and polyunsaturated fatty acids such as arachidonic acid were shown to be toxic and cause apoptosis in HepG2 cells which express CYP2E1 but not in control HepG2 cell lines."( Ethanol and arachidonic acid produce toxicity in hepatocytes from pyrazole-treated rats with high levels of CYP2E1.
Cederbaum, AI; Wu, D, 2000
)
0.31
" It is primarily considered as a neurotoxin but its other toxic manifestations are also well documented."( Pharmacological interventions of cyanide-induced cytotoxicity and DNA damage in isolated rat thymocytes and their protective efficacy in vivo.
Bhattacharya, R; Lakshmana Rao, PV, 2001
)
0.31
" The specific metal responsible for the toxicity was not determined; the metals common to each of the toxic archwires were nickel, iron, and chromium."( In vitro cytotoxicity of orthodontic archwires in cortical cell cultures.
David, A; Lobner, D, 2004
)
0.32
" Tat is neurotoxic and a constantly growing body of evidence suggests that the toxic effects of Tat are oxidative stress-dependent."( Cocaine-mediated enhancement of Tat toxicity in rat hippocampal cell cultures: the role of oxidative stress and D1 dopamine receptor.
Aksenov, MY; Aksenova, MV; Booze, RM; Mactutus, CF; Nath, A; Ray, PD, 2006
)
0.33
"The ability of the water-soluble Vitamin E analog, Trolox, to prevent the toxic effects of copper exposure on the behavior and neuronal physiology of the freshwater oligochaete Lumbriculus variegatus was examined."( The Vitamin E analog Trolox reduces copper toxicity in the annelid Lumbriculus variegatus but is also toxic on its own.
Hoyt, EM; Leigh-Logan, T; Murray, PM; O'Gara, BA; Smeaton, MB, 2006
)
0.33
" In addition, a short-term toxicity assessment in rats was also conducted for the identification of certain toxic effects of AG after heat processing."( Increase in the free radical scavenging activities of American ginseng by heat processing and its safety evaluation.
Kang, KS; Kim, HY; Okamoto, T; Sei, Y; Yamabe, N; Yokozawa, T, 2007
)
0.34
"Amiodarone (AM), a drug used in the treatment of cardiac dysrrhythmias, can produce severe pulmonary adverse effects, including fibrosis."( Direct mitochondrial dysfunction precedes reactive oxygen species production in amiodarone-induced toxicity in human peripheral lung epithelial HPL1A cells.
Brien, JF; Comeau, JL; Hill, BC; Ji, Y; Massey, TE; Nicolescu, AC; Racz, WJ; Takahashi, T, 2008
)
0.35
" The aim of this study was to address the toxic effects of MnCl2 and MnSO4 on the immortalized rat brain microvessel endothelial cell line (RBE4) and to characterize toxic mechanism associated with exposure to Mn."( Antioxidants prevent the cytotoxicity of manganese in RBE4 cells.
Aschner, M; Au, C; Batoréu, MC; Marreilha dos Santos, AP; Milatovic, D; Santos, D, 2008
)
0.35
" possible adverse neurological damage caused by MeHg."( The in vitro effects of Trolox on methylmercury-induced neurotoxicity.
Aschner, M; Evje, L; Kaur, P; Syversen, T, 2010
)
0.36
" While these results make it unlikely that hemin toxicity is due to interactions with endogenous H(2)O(2), hemin toxicity was increased in the presence of supraphysiological levels of H(2)O(2) and this increase was ameliorated by PHEN, indicating that the iron released from hemin can be toxic under some pathological conditions."( The metabolism and toxicity of hemin in astrocytes.
Bishop, GM; Dang, TN; Dringen, R; Robinson, SR, 2011
)
0.37
" In this study we compared the effects of CB1 and CB2 receptor-selective ligands, the endocannabinoid anandamide and the phytocannabinoid cannabidiol, against oxidative stress and the toxic hallmark Alzheimer's protein, β-amyloid (Aβ) in neuronal cell lines."( Contrasting protective effects of cannabinoids against oxidative stress and amyloid-β evoked neurotoxicity in vitro.
Harvey, BS; Mååg, JL; Musgrave, IF; Ohlsson, KS; Smid, SD, 2012
)
0.38
" In conclusion, the nanoparticles containing antioxidant actives were safe for topical use and presented anti-aging activity in vivo and are suitable to be used as cosmetic ingredient."( Safety and efficacy of antioxidants-loaded nanoparticles for an anti-aging application.
Bruschi, M; Carvalho, AR; Felippi, CC; Oliveira, D; Raffin, RP; Ströher, A; Van Etten, EA, 2012
)
0.38
"01-1000μM) did not show neurotoxicity, 2'-OH- and 4'-OH-deltamethrin (10-1000μM) were more toxic than deltamethrin (10-1000μM)."( Cytotoxicity induced by deltamethrin and its metabolites in SH-SY5Y cells can be differentially prevented by selected antioxidants.
Anadón, A; Ares, I; Castellano, V; Martínez, M; Martínez, MA; Martínez-Larrañaga, MR; Ramos, E; Romero, A, 2012
)
0.38
" In this study, we investigated the toxic effect of ketamine on neurons differentiated from hESCs."( Ketamine induces toxicity in human neurons differentiated from embryonic stem cells via mitochondrial apoptosis pathway.
Bai, X; Bosnjak, ZJ; Canfield, S; Corbett, JA; Kikuchi, C; Muravyeva, MY; Wells, CW; Yan, Y, 2012
)
0.38
" We previously identified the toxic conformer of Aβ42 with a turn at positions 22 and 23 ("toxic turn") by solid-state NMR and demonstrated that a monoclonal antibody (11A1) against the toxic turn in Aβ42 mainly detected the oligomer in the brains of AD patients."( Toxicity in rat primary neurons through the cellular oxidative stress induced by the turn formation at positions 22 and 23 of Aβ42.
Akaike, A; Irie, K; Izumi, Y; Izuo, N; Kume, T; Murakami, K; Sato, M, 2012
)
0.38
" Our evidence suggests that specific organic ligands available in the receiving waters can differentially surface modify AgNPs and alter their environmental persistence (changing dissolution dynamics) and subsequently the toxicity; hence, we caveat to generalize that surface modified nanoparticles upon environmental release may not be toxic to receptor organisms."( Impacts of select organic ligands on the colloidal stability, dissolution dynamics, and toxicity of silver nanoparticles.
Dubey, B; Pokhrel, LR; Scheuerman, PR, 2013
)
0.39
"T-2 toxin is a highly toxic mycotoxin produced by various Fusarium species, mainly, Fusarium sporotrichoides, and has been reported to have toxic effects on reproductive system of adult male animals."( T-2 toxin-induced cytotoxicity and damage on TM3 Leydig cells.
Matias, FB; Wu, J; Yi, JE; Yuan, Z,
)
0.13
" No serious treatment-emergent adverse events were reported."( The KHENERGY Study: Safety and Efficacy of KH176 in Mitochondrial m.3243A>G Spectrum Disorders.
Beukema, R; Beyrath, J; de Laat, P; Groothuis, J; Hemelaar, P; Janssen, MCH; Koene, S; Pickkers, P; Smeitink, J; Spaans, E; Verhaak, C, 2019
)
0.51
" To address this issue, the adverse effects of Au@PEG on human neuroblastoma SHSY5Y cells were first investigated."( Surface Functionalization of Pegylated Gold Nanoparticles with Antioxidants Suppresses Nanoparticle-Induced Oxidative Stress and Neurotoxicity.
Du, L; Guan, L; Guo, W; Guo, X; Kang, X; Wu, H; Yang, H; Zhang, X, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
" Reduced NO bioavailability causes the so-called "endothelial dysfunction," which seems to be the common molecular disorder comprising stable atherosclerotic narrowing lesions or acute plaque rupture causing unstable angina or myocardial infarction."( Endothelial dysfunction in acute and chronic coronary syndromes: evidence for a pathogenetic role of oxidative stress.
Cicchitelli, G; Ferrari, R; Macrì, G; Malagutti, P; Merli, E; Soukhomovskaia, O; Valgimigli, M, 2003
)
0.32
" However, flavonoids are poorly absorbed by humans, and the increase in plasma antioxidant capacity observed after consumption of flavonoid-rich foods often greatly exceeds the increase in plasma flavonoids."( The increase in human plasma antioxidant capacity after apple consumption is due to the metabolic effect of fructose on urate, not apple-derived antioxidant flavonoids.
Frei, B; Lotito, SB, 2004
)
0.32
" The findings demonstrated herein therefore strongly suggest that the amphiphilic character enhances the bioavailability of the antioxidants and allows for a selective targeting of mitochondria."( Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
Böker, J; Durand, G; Hardeland, R; Ortial, S; Pappolla, MA; Poeggeler, B; Polidori, A; Pucci, B, 2006
)
0.33
" N-(1-adamantyl)-2-oxo-chromene-3-carboxamide (8), N-adamantan-1-yl-5-dimethyl-amino-1-naphthalenesulfonic acid (11) and N-(1-cyano-2H-isoindol-2-yl) adamantan-1-amine (12) were found to possess a high degree of multifunctionality with favourable physical-chemical properties for bioavailability and blood-brain barrier permeability."( Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
Green, IR; Joubert, J; Malan, SF; van Dyk, S, 2011
)
0.37
" Owing to aldose reductase pharmacophore requirements for an acidic proton, most aldose reductase inhibitors contain an acetic acid moiety, ionized at physiological pH, resulting in poor bioavailability of the drugs."( (2-Benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl)-acetic acid: an aldose reductase inhibitor and antioxidant of zwitterionic nature.
Juskova, M; Milackova, I; Snirc, V; Stefek, M; Triantos, N; Tsantili-Kakoulidou, A, 2011
)
0.37
" Although oral bioavailability of cyclosporine A (CsA) was decreased by increased first-pass metabolism through CYP3A and P-glycoprotein (P-gp) specifically in the upper small intestine after liver I/R, the mechanism responsible for them remained to be clarified."( An antioxidant Trolox restores decreased oral absorption of cyclosporine A after liver ischemia-reperfusion through distinct mechanisms between CYP3A and P-glycoprotein in the small intestine.
Ikemura, K; Inoue, K; Iwamoto, T; Mizutani, H; Oka, H; Okuda, M, 2012
)
0.38
" To assess the bioavailability of EM, we examined the in vitro uptake using the Caco-2 human colonic cell line."( Extraction of antioxidant components from Bidens pilosa flowers and their uptake by human intestinal Caco-2 cells.
Chang, CH; Chyau, CC; Huang, SH; Lee, WC; Peng, CC, 2013
)
0.39
" Here, a new series of orally bioavailable multifunctional antioxidants (MFAO-2s) possessing a 2-diacetylamino-5-hydroxypyrimidine moiety is described."( Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
Kador, PF; Kawada, H, 2015
)
0.42
" Compound 13d, having good in vitro ADME profile and moderate oral bioavailability in mice, showed potent anti-inflammatory activity against hapten-induced contact hypersensitivity reaction in mice following topical and oral administration."( Synthesis and biological evaluation of novel orally available 1-phenyl-6-aminouracils containing dimethyldihydrobenzofuranol structure for the treatment of allergic skin diseases.
Fujiwara, N; Hasegawa, F; Inoue, Y; Isobe, M; Isobe, Y; Tobe, M; Tsuboi, K, 2016
)
0.43
" However, it has major drawbacks of very poor bioavailability and solubility."( An appraisal on recent medicinal perspective of curcumin degradant: Dehydrozingerone (DZG).
Hampannavar, GA; Karpoormath, R; Palkar, MB; Shaikh, MS, 2016
)
0.43
" These activities, associated to a good predictive bioavailability and a lack of cytotoxicity, design it as a promising hit for further in vivo investigation."( Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer's disease treatment.
Corvaisier, S; Cresteil, T; Dallemagne, P; El Kihel, L; Jourdan, JP; Lecoutey, C; Legay, R; Malzert-Fréon, A; Rochais, C; Since, M; Sopkova-de Oliveira Santos, J, 2016
)
0.43
" In that respect, augmenting the water solubility by structural modification of the curcumin scaffold may result in improved bioavailability and pharmacokinetics."( Synthesis and biological assessment of novel N-(hydroxy/methoxy)alkyl β-enaminone curcuminoids.
D'hooghe, M; De Vreese, R; Grootaert, C; Theppawong, A; Van Camp, J; Vannecke, L, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" Hydroxybutyl methylcellulose improved the linearity of the dose-response curve in a peroxidase-based antioxidant assay and stabilized light emission post-consumption of the antioxidant (Trolox)."( Effect of polymers on enhanced chemiluminescent assays for peroxidase and peroxidase labels.
Ji, X; Kricka, LJ,
)
0.13
" Dose-response curves were made for each of the additives (n> or =4 for each dose)."( Improving the preservation of isolated rat skeletal muscles stored for 16 hours at 4 degrees C.
Bär, DP; de Smet, M; de With, MC; Kon, M; Kroese, AB; van der Heijden, EP; Werker, PM, 2000
)
0.31
" The antioxidant capacity of Gala apples and seven phenolic standards, determined by both ABTS(*)(-) and DPPH(*) scavenging assays, showed a dose-response of the first-order."( Vitamin C equivalent antioxidant capacity (VCEAC) of phenolic phytochemicals.
Kim, DO; Lee, CY; Lee, HJ; Lee, KW, 2002
)
0.31
" This dose-response curve had nadirs at 300 and 800 microM."( A scavenger of peroxynitrite prevents long-term memory formation using a single trial passive avoidance task for the day-old chick.
Edwards, TM; Rickard, NS, 2005
)
0.33
" The pro-oxidant or antioxidant effect for these antioxidants at different concentration, may provide useful information about the selection of the suitable antioxidant and dosage in experimental and clinical application."( Peroxynitrite and heme protein--mediated nitrative/oxidative modification of human plasma protein: the role of free radical scavenging vs. complex forming.
Gao, Z; Lu, N; Pei, D; Yi, L; Zhou, G, 2009
)
0.35
" All of the compounds showed a significant and dose-response efficacy although weaker than that exercised by the standard Trolox®."( abeo-abietanes from Teucrium polium roots as protective factors against oxidative stress.
D'Abrosca, B; D'Angelo, G; Fiorentino, A; Monaco, P; Pacifico, S; Scognamiglio, M, 2010
)
0.36
" There were few differences between treatments after thawing, with Trolox reducing MDA production in a dose-response manner."( Reduced glutathione and Trolox (vitamin E) as extender supplements in cryopreservation of red deer epididymal spermatozoa.
Alvarez, M; Alvarez-Rodríguez, M; Anel, L; Anel-López, L; de Paz, P; García-Álvarez, O; Garde, JJ; Maroto-Morales, A; Martínez-Pastor, F, 2012
)
0.38
" Injection of the same dosage of the ligand 3,5-diisopropyl salicylate has no effect on streptozotocin-induced hyperglycemia."( The antioxidant activity of copper(II) (3,5-diisopropyl salicylate)4 and its protective effect against streptozotocin-induced diabetes mellitus in rats.
Abdul-Ghani, AS; Abdul-Ghani, R; Abu-Hijleh, AL; Husein, R; Metani, M; Qazzaz, M, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
radical scavengerA role played by a substance that can react readily with, and thereby eliminate, radicals.
Wnt signalling inhibitorA substance that inhibits any of the Wnt signalling pathway, a group of signal transduction pathways made of proteins that pass signals from outside of a cell through cell surface receptors to the inside of the cell.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
ferroptosis inhibitorAny substance that inhibits the process of ferroptosis (a type of programmed cell death dependent on iron and characterized by the accumulation of lipid peroxides) in organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
chromanolAny member of the class of chromanes that is chromane substituted by one or more hydroxy groups.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
monocarboxylic acidAn oxoacid containing a single carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency7.94330.044717.8581100.0000AID485294
GLS proteinHomo sapiens (human)Potency7.94330.35487.935539.8107AID624170
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency14.12540.035520.977089.1251AID504332
gemininHomo sapiens (human)Potency1.81170.004611.374133.4983AID624296; AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyphenol oxidase 2Agaricus bisporusIC50 (µMol)200.00000.03403.987110.0000AID635123
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)2,090.70000.00000.933210.0000AID1256880; AID1802996
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.13000.00021.557410.0000AID295042
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.00070.97749.7000AID295044
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)6.62500.00010.995010.0000AID240679; AID295043
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC50 (µMol)1,000.00000.00132.81389.8200AID295041
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (107)

Processvia Protein(s)Taxonomy
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
allantoin metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of protein phosphorylationXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell proliferationXanthine dehydrogenase/oxidaseHomo sapiens (human)
guanine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
inosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyinosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
adenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyadenosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
deoxyguanosine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
AMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
IMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
lactationXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of gene expressionXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron-sulfur cluster assemblyXanthine dehydrogenase/oxidaseHomo sapiens (human)
amide catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of endothelial cell differentiationXanthine dehydrogenase/oxidaseHomo sapiens (human)
GMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dGMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
dAMP catabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of p38MAPK cascadeXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vascular endothelial growth factor signaling pathwayXanthine dehydrogenase/oxidaseHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processXanthine dehydrogenase/oxidaseHomo sapiens (human)
negative regulation of vasculogenesisXanthine dehydrogenase/oxidaseHomo sapiens (human)
androgen metabolic processDehydrogenase/reductase SDR family member 9Homo sapiens (human)
epithelial cell differentiationDehydrogenase/reductase SDR family member 9Homo sapiens (human)
progesterone metabolic processDehydrogenase/reductase SDR family member 9Homo sapiens (human)
retinol metabolic processDehydrogenase/reductase SDR family member 9Homo sapiens (human)
9-cis-retinoic acid biosynthetic processDehydrogenase/reductase SDR family member 9Homo sapiens (human)
steroid metabolic processDehydrogenase/reductase SDR family member 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Processvia Protein(s)Taxonomy
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
xanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
xanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
iron ion bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
protein homodimerization activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
molybdopterin cofactor bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine dehydrogenase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
hypoxanthine oxidase activityXanthine dehydrogenase/oxidaseHomo sapiens (human)
FAD bindingXanthine dehydrogenase/oxidaseHomo sapiens (human)
alcohol dehydrogenase (NAD+) activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
all-trans-retinol dehydrogenase (NAD+) activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
racemase and epimerase activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
androsterone dehydrogenase activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityDehydrogenase/reductase SDR family member 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo sapiens (human)
peroxisomeXanthine dehydrogenase/oxidaseHomo sapiens (human)
cytosolXanthine dehydrogenase/oxidaseHomo sapiens (human)
sarcoplasmic reticulumXanthine dehydrogenase/oxidaseHomo sapiens (human)
extracellular spaceXanthine dehydrogenase/oxidaseHomo sapiens (human)
endoplasmic reticulum membraneDehydrogenase/reductase SDR family member 9Homo sapiens (human)
intracellular membrane-bounded organelleDehydrogenase/reductase SDR family member 9Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (838)

Assay IDTitleYearJournalArticle
AID1381601Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 30 mins dark incubation2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
AID551406Antioxidant activity of the compound assessed as DPPH radical scavenging activity at 0.5 mM after 2 hrs2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Synthesis, structure, theoretical and experimental in vitro antioxidant/pharmacological properties of α-aryl, N-alkyl nitrones, as potential agents for the treatment of cerebral ischemia.
AID19477Partition coefficient (logD) (octanol/phosphate buffer)1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
A cardioselective, hydrophilic N,N,N-trimethylethanaminium alpha-tocopherol analogue that reduces myocardial infarct size.
AID1152637Antioxidant activity assessed as hydroxyl radical scavenging activity at 5 uM after 1 hr by 2-Deoxy-D-ribose degradation assay in presence of FeCl32014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Synthesis and radical scavenging activity of phenol-imidazole conjugates.
AID469415Neuroprotective activity against human SH-SY5Y cells assessed as cytoprotection at 1 uM coincubated with rotenone/oligomycin A measured after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1581656Antioxidant activity assessed as ABTS radical scavenging activity at 30 uM measured after 60 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID195554The IC50 value was measured for inhibition of lipid autoxidation in rat brain homogenate.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Cardioselective ammonium, phosphonium, and sulfonium analogues of alpha-tocopherol and ascorbic acid that inhibit in vitro and ex vivo lipid peroxidation and scavenge superoxide radicals.
AID257313DPPH radical scavenging activity of Cudriana tricuspidata extracts2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Antioxidant and cytotoxic activities of xanthones from Cudrania tricuspidata.
AID504307Antioxidant activity assessed as superoxide radical scavenging activity by chemiluminescence analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Antioxidant and anti-inflammatory phenylpropanoid derivatives from Calamus quiquesetinervius.
AID269151Antioxidant activity assessed as ability to scavenge hydroxyl radicals by ABTS competition assay2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Solid-phase synthesis of quinol fatty alcohols, design of N/O-substituted quinol fatty alcohols and comparative activities on axonal growth.
AID444235Cytoprotection in human SRA1 cells assessed as protection against H2O2-induced cell death after 2 hrs by MTS assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Multifunctional antioxidants for the treatment of age-related diseases.
AID257903Antioxidant potency assessed chemically2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Chroman/catechol hybrids: synthesis and evaluation of their activity against oxidative stress induced cellular damage.
AID1493970Antiproliferative activity against human T47D cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID103204Compound was tested for antiproliferative activity against human breast cancer cell line MCF-7 in MTT assay1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of analogs of vitamin E: antiproliferative activity against human breast adenocarcinoma cells.
AID203485Glycation-induced fluorescence changes of bovine serum albumin when exposed to fructose (1 mM); p<0.0012003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID1493968Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID736487Antioxidant activity assessed as inhibition of DPPH radical formation measured every min for 45 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Exploring nature profits: development of novel and potent lipophilic antioxidants based on galloyl-cinnamic hybrids.
AID541259Inhibition of AAPH-induced linoleic acid lipid peroxidation2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
1,5-Benzoxazepines vs 1,5-benzodiazepines. one-pot microwave-assisted synthesis and evaluation for antioxidant activity and lipid peroxidation inhibition.
AID444242Antioxidant activity in human HAh cells assessed as inhibition of Fenton's reagent-induced reduction of cellular glutathione level after 2 hrs by DTNB method2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Multifunctional antioxidants for the treatment of age-related diseases.
AID536049Antioxidant activity assessed as protection against 340 Gy gamma-radiation-induced thymidine degradation in 12.5 mM phosphate buffer at 50 uM by competitive immuno-enzymatic assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Synthesis and antioxidant properties of pulvinic acids analogues.
AID218991Oxidation was assessed indirectly by measuring bovine serum albumin (BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 10 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID1713228Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 12.5 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID459654Cytotoxicity against human MRC5 cells assessed as plasma membrane damage at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1179730Cytoprotection in mouse CRL2181 cells assessed as reduction in UV-oxidized LDL-induced cytotoxicity by measuring cell viability at 10 uM after 24 hrs by MTT assay relative to untreated control2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID1357814Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as cell viability at 25 uM pre-incubated for 1 hr followed by H2O2 addition and measured after 4 hrs by MTT assay relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID1564979Antioxidant activity assessed as DPPH radical scavenging activity measured after 120 mins2019European journal of medicinal chemistry, Nov-15, Volume: 182Novel multi target-directed ligands targeting 5-HT
AID1651391Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as cell viability at 25 uM preincubated for 1 hr followed by H2O2 addition and measured after 4 hrs by CCK8 assay (Rvb = 61.14 +/- 1.05%)2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Isolation of triterpenoid saponins from Medicago sativa L. with neuroprotective activities.
AID445117Prooxidant effect on Cu2+-induced pBR322 DNA damage at 0.35 to 45 uM after 1 hr2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antioxidant properties of dendritic polyphenols.
AID459650Cytotoxicity against human Caco-2 cells assessed as cell death at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1335587Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 1 x 10'-4 M by UV-absorbance method relative to control2016European journal of medicinal chemistry, Nov-29, Volume: 124Novel urea and bis-urea primaquine derivatives with hydroxyphenyl or halogenphenyl substituents: Synthesis and biological evaluation.
AID264479Lipophilicity, log k'w of the compound2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID639373Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 0.3 uM treated 24 hrs before rotenone/oligomycin A challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID490944Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 60 mins2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID639458Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 0.3 uM after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1325285Antioxidant activity assessed as ABTS radical scavenging activity after 30 mins2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID1424234Antioxidant activity assessed as singlet oxygen scavenging activity by measuring rate constant using VIS irradiation by ESR spin trapping method2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID196393Compound was evaluated for its inhibitory concentration against hydrogen peroxide- induced oxidative neuronal damage in primary cultured rat cortical cells2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Synthesis and evaluation of 4-hydroxyphenylacetic acid amides and 4-hydroxycinnamamides as antioxidants.
AID1892624Antioxidant activity in rat brain homogenate assessed as inhibition of lipid peroxidation by measuring MDA concentration at 10 uM relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID604215Antioxidant activity assessed as inhibition of ABTS free radicals at 1 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID708013Inhibition of AAPH-induced oxidative stress in human U373MG cells assessed as peroxy radical scavenging activity at 8 uM by ORAC assay2012Journal of natural products, Oct-26, Volume: 75, Issue:10
Diterpenoids isolated from Sideritis species protect astrocytes against oxidative stress via Nrf2.
AID1326574Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID490420Cytoprotective activity against cell-mediated LDL oxidation in HMEC1 cells at 10 uM after 6 hrs by MTT assay2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antioxidant activity evaluation of a syringic hydrazones family.
AID1298953Antioxidant activity assessed as DPPH free radical scavenging activity at 100 uM after 40 mins by UV-Vis spectrophotometry2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of benzothiadiazine derivatives exhibiting dual activity as aldose reductase inhibitors and antioxidant agents.
AID1325287Antioxidant activity assessed as ferric ion reducing activity by measuring Fe2+ levels using fe3+-TPTZ at 750 ug/ml after 30 mins by FRAP assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID1465117Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalents at 20 uM after 1 hr by UV/Vis spectrophotometric method-based ABTS radical cation decolorization assay2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.
AID1198127Antioxidant activity assessed as DPPH scavenging activity after 30 mins by spectrophotometry2015European journal of medicinal chemistry, Mar-26, Volume: 93Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
AID634729Antioxidant activity assessed as inhibition of DPPH free radical scavenging activity2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Bis-chalcone analogues as potent NO production inhibitors and as cytotoxic agents.
AID431301Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 0.1 mM2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Urea and carbamate derivatives of primaquine: synthesis, cytostatic and antioxidant activities.
AID1678099Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM relative to control2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID1402942Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced ROS production measured after 4 hrs by H2DCFDA-AM probe based fluorescence assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Synthesis and biological evaluation of diarylheptanoids as potential antioxidant and anti-inflammatory agents.
AID1610480Inhibition of porcine liver carboxylesterase at 20 uM using 4-NPA as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis relative to control2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.
AID604211Antioxidant activity assessed as inhibition of DPPH free radicals at 0.1 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID619941Antioxidant activity assessed as ferric to ferrous reduction at 20 ug/ml by FRAP assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1465118Antioxidant activity assessed as ABTS radical cation scavenging activity after 1 hr by UV/Vis spectrophotometric method-based ABTS radical cation decolorization assay2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.
AID1474959Antioxidant activity assessed as ABTS radical scavenging activity at 3 mg/ml incubated for 2 hrs in dark by spectrophotometric analysis (Rvb = 1 to 9%)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID625355Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 100 uM2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of (2,5-dihydro-1H-pyrrol-1-yl)-2H-chromen-2-ones as free radical scavengers.
AID1143754Inhibition of calcium channel in human SH-SY5Y cells assessed as blockade of K+-evoked cytosolic calcium increase at 3 uM after 15 mins using Fluo-4/AM by fluorescence microplate reader analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID1179762Ratio of compound IC50 to trolox IC50 for ABTS radical scavenging activity after 12 hrs by spectrophotometry2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Phenylpropanoid acid esters from Korean propolis and their antioxidant activities.
AID1581654Antioxidant activity assessed as ABTS radical scavenging activity at 75 uM measured after 30 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1326580Cytotoxicity against human CEM13 cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1242923Antioxidant activity in rat brain assessed as inhibition of MDA production at 100 uM by TBARS assay relative to control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.
AID381849DPPH radical scavenging activity2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
AID1264041Neuroprotective activity against Fenton reagent-induced hydroxy radical-stimulated cytotoxicity in human SH-SY5Y cells assessed as cell survival at 1 to 1000 uM preincubated for 1 hr followed by Fenton reagent challenge for 2 hrs by fluorescence-based LIV2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1143747Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 0.3 uM preincubated for 24 hrs before rotenone-oligomycin addition measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID228133Reaction rate constant of the compound2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Imidazolopyrazinones as potential antioxidants.
AID196902Effect of compound on in vitro accumulation of MDA content in heart at concentration of 5 uM2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Novel potent inhibitors of lipid peroxidation with protective effects against reperfusion arrhythmias.
AID1179729Antioxidant activity assessed as reduction in mouse CRL2181 cells-mediated human LDL oxidation by measuring TBARS level at 1 uM after 18 hrs2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID619934Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 24 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID81332Compound was evaluated for in vitro inhibition of proliferation measured by inhibition of [3H]thymidine incorporation by HMVEC-L cells1999Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
Novel esters and amides of nonsteroidal antiinflammatory carboxylic acids as antioxidants and antiproliferative agents.
AID247976Inhibition concentration against DPPH radical scavenging activity in rat was determined2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and evaluation of 6-hydroxy-7-methoxy-4-chromanone- and chroman-2-carboxamides as antioxidants.
AID1256875Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by microplate reader analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1456006Antioxidant activity assessed as DPPH radical scavenging activity measured after 30 mins2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease.
AID567051Antioxidant activity assessed as inhibition of linoleic acid peroxidation at 0.1 mM by AAPH assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.
AID1581659Antioxidant activity assessed as increase in total ferric ion reducing activity at 30 uM using FeCl3.H2O and TPTZ incubated for 5 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1083341Antiviral activity against Sindbis virus infected Hela cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1179732Antioxidant activity assessed as superoxide anion radical scavenging activity at 10 uM by PMS-NADH-NBT system based spectrophotometry2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID1485933Neuroprotective activity against H2O2-induced cell death in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by H2O2 induction after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID451365Antioxidant activity assessed as inhibition of Fe3+ ion-induced 2-deoxyribose oxidation after 24 hrs by TBA method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Antioxidant efficacy of iridoid and phenylethanoid glycosides from the medicinal plant Teucrium chamaedris in cell-free systems.
AID1333939Oxidation potential of compound against Ag/Agcl reference electrode at 1 mM by cyclic voltametry2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Synthesis, antioxidant and antichagasic properties of a selected series of hydroxy-3-arylcoumarins.
AID1372025Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced hydroxyl radical scavenging activity by measuring Kaox/Kst ratio using DMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID469404Neuroprotective activity against human SH-SY5Y cells assessed as protection reduction in H2O2-induced LDH release at 1 uM after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1083350Antioxidant activity assessed as DPPH radical scavenging activity at 1 X 10'-4 M after 60 min2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID548349Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 60 uM after 24 hrs by UV-vis spectroscopy2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1428457Inhibition of Acyrthosiphon pisum phenoloxidase using L-DOPA as substrate preincubated for 5 mins followed by substrate addition measured after 120 to 240 mins by spectrophotometric method2016Journal of natural products, Dec-23, Volume: 79, Issue:12
Antioxidant Flavonols and Phenolic Compounds from Atraphaxis frutescens and Their Inhibitory Activities against Insect Phenoloxidase and Mushroom Tyrosinase.
AID1256118Antioxidant activity in rat PC12 cells assessed as inhibition of Fe2+-induced reactive oxygen species formation after 1 hr by DCFH-DA dye-based fluorometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
AID195539Compound was tested for 50% Inhibition of lipid peroxidation in rat brain homogenate2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID745285Antioxidant activity assessed as Fe3+/ascorbic acid-induced hydroxyl radical scavenging activity at 100 uM after 30 mins2013European journal of medicinal chemistry, May, Volume: 63Analysis of the antioxidant properties of differently substituted 2- and 3-indolyl carbohydrazides and related derivatives.
AID1174517Antioxidant activity assessed as radical scavenging activity after 1 hr by ABTS competition assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Neuroprotective effects of a brain permeant 6-aminoquinoxaline derivative in cell culture conditions that model the loss of dopaminergic neurons in Parkinson disease.
AID604216Antioxidant activity assessed as inhibition of DPPH free radicals after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID736291Antioxidant activity assessed as ABTS free radical scavenging activity measured up to 6 mins by spectrophotometric analysis2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Antioxidant and anti-inflammatory meroterpenoids from the brown alga Cystoseira usneoides.
AID459652Cytotoxicity against HEK293 cells assessed as plasma membrane damage at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1486134Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalent antioxidant capacity after 1 hr by UV/Vis spectrophotometric analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, molecular docking, and biological activity of polyfluoroalkyl dihydroazolo[5,1-c][1,2,4]triazines as selective carboxylesterase inhibitors.
AID1603221Antioxidant activity in rat brain homogenate assessed as inhibition of FeCl2/ascorbic acid-induced lipid peroxidation by measuring reduction in TBARS level at 100 uM measured after 30 mins by spectrophotometric method relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID392746Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 100 uM2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
Synthesis of hydroxycoumarins and hydroxybenzo[f]- or [h]coumarins as lipid peroxidation inhibitors.
AID1306592Antioxidant activity in HMEC1 assessed as inhibition of cell induced LDL oxidation by measuring TBARS level at 1 uM relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1311886Antioxidant activity in human SH-SY5Y cells assessed as inhibition of H2O2-induced ROS production preincubated for 1 day prior H2O2 treatment at 25 uM by DCFH-DA-based fluorescence analysis2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, and evaluation of Trolox-conjugated amyloid-β C-terminal peptides for therapeutic intervention in an in vitro model of Alzheimer's disease.
AID736009Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by microplate reader2013Journal of natural products, Feb-22, Volume: 76, Issue:2
Flavone tetraglycosides and benzyl alcohol glycosides from the Mongolian medicinal plant Dracocephalum ruyschiana.
AID1365821Antioxidant activity in rat hepatic microsomes assessed as inhibition of FeSO4-induced lipid peroxidation measured after 45 mins by spectrophotometry2017Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
Dual antioxidant structures with potent anti-inflammatory, hypolipidemic and cytoprotective properties.
AID619938Antioxidant activity assessed as residual ABTS+ radical scavenging activity after 30 mins by spectrophotometric analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1083351Antioxidant activity assessed as DPPH radical scavenging activity at 1 X 10'-4 M after 20 min2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID463458Antioxidant activity against peroxynitrite-induced tyrosine nitration after 15 mins by HPLC2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
New pyrazoles incorporating pyrazolylpyrazole moiety: synthesis, anti-HCV and antitumor activity.
AID264673Hydroxyl radical scavenging activity by ABTS assay2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Quinol fatty alcohols as promoters of axonal growth.
AID381850Antioxidant activity assessed as inhibition of DOPC liposomes2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
AID363319Antioxidant activity assessed as inhibition of peroxynitrite-induced evans blue bleaching at 50 uM2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
AID774817Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antioxidant activity of novel Mannich base of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan.
AID1083337Antiviral activity against Vesicular stomatitis virus infected HEL cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1238055Antioxidant activity assessed as nitric oxide radical scavenging activity at 500 uM incubated for 60 mins with light exposure at room temperature by Griess assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Nitric oxide inhibitory activity and antioxidant evaluations of 2-benzoyl-6-benzylidenecyclohexanone analogs, a novel series of curcuminoid and diarylpentanoid derivatives.
AID1755236Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM incubated for 24 hrs by Thioflavin T based fluorometric assay relative to control
AID1424232Antioxidant activity assessed as superoxide anion free radical scavenging activity by measuring rate constant using UV irradiation by ESR spin trapping method2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID1075913Antioxidant activity assessed as ROS scavenging activity at 1 to 10 uM by DCFDA assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
MHY884, a newly synthesized tyrosinase inhibitor, suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress.
AID1713223Permeability of the compound at pH 7.4 by PAMPA-BBB assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1306590Antioxidant activity assessed as inhibition of DPPH free radical scavenging activity after 60 mins by UV-Visible spectrophotometry2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID75288In vitro glutathione peroxidase activity at 2*10e-7M using tert-butyl hydroperoxide, activity given in percentage of ebselen''s activity1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity.
AID497113Antioxidant activity against DPPH free radical assessed as compound able to consume half the amount of free radical after 1 hr2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
AID1493969Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID639374Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 1 uM treated 24 hrs before rotenone/oligomycin A challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID436260Antioxidant activity assessed as DPPH radical scavenging activity2008Journal of natural products, Nov, Volume: 71, Issue:11
Synthesis and biological activities of thio-avarol derivatives.
AID663247Neuroprotective activity in human SH-SY5Y cells assessed as protection against H2O2-induced oxidative stress at 10 uM incubated for 1 hr prior to H2O2-challenge measured after 12 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases.
AID1392723Cytoprotection against H2O2-induced oxidative stress in rat PC12 cells assessed as increase in cell viability up to 10 uM after 24 hrs by MTT assay
AID23927The compound was evaluated for lipophilicity2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Novel potent inhibitors of lipid peroxidation with protective effects against reperfusion arrhythmias.
AID1348943Antioxidant activity assessed as DPPH radical scavenging activity after 60 mins by spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1256114Antioxidant activity assessed as ABTS radical scavenging activity after 7 mins2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
AID1310992Antioxidant activity assessed as inhibition of allopurinol-xanthine oxidase system-mediated superoxide formation measured over 7 mins by lucigenin-based chemiluminescence analysis2016European journal of medicinal chemistry, Aug-25, Volume: 119On the vasoprotective mechanisms underlying novel β-phosphorylated nitrones: Focus on free radical characterization, scavenging and NO-donation in a biological model of oxidative stress.
AID1141995Antioxidant activity assessed as inhibition of Fe3+/ascorbic acid-induced hydroxyl radical formation by measuring DMSO-induced formaldehyde production at 100 uM after 30 mins relative to control2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes and evaluation of their antioxidant and lipid peroxidation activity.
AID1306599Inhibition of oxidized LDL induced intracellular ROS formation in HMEC1 at 10 uM preincubated for 30 to 40 mins followed by H2DCFDA-AM addition by fluorescence analysis2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1493753Antioxidant activity assessed as ABTS radical scavenging activity measured after 12 to 16 hrs2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID247569In vitro inhibitory concentration against hydroxyl radical (-OH)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Nitrone derivatives of trolox as neuroprotective agents.
AID1581657Antioxidant activity assessed as ABTS radical scavenging activity at 75 uM measured after 60 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1300894Antioxidant activity assessed as ABTS radical scavenging activity after 30 mins under dark conditions2016European journal of medicinal chemistry, Jul-19, Volume: 117Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.
AID16876The reaction rate constant (K) by measuring competition with nitroblue tetrazolium of the superoxide radicals formed by xanthine oxidase/xanthine1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Cardioselective ammonium, phosphonium, and sulfonium analogues of alpha-tocopherol and ascorbic acid that inhibit in vitro and ex vivo lipid peroxidation and scavenge superoxide radicals.
AID1581650Antioxidant activity assessed as ABTS radical scavenging activity at 30 uM measured after 5 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1762401Inhibition of porcine liver carboxylesterase using 4-NPA as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
AID1071846Antioxidant activity assessed as rosebengal-induced singlet oxygen radical scavenging activity by ESR spin trapping method relative to 4-OH-TEMP2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID477898Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2010Journal of natural products, Apr-23, Volume: 73, Issue:4
Sesquiterpenoid aminoquinones from the marine sponge Dysidea sp.
AID1659474Inhibition of AKR1A1 in rat kidney at 10 uM relative to control2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID1320857Antioxidant activity assessed as DPPH free radical scavenging activity after 60 mins2016European journal of medicinal chemistry, Oct-04, Volume: 121Do cinnamylideneacetophenones have antioxidant properties and a protective effect toward the oxidation of phosphatidylcholines?
AID1428456Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins2016Journal of natural products, Dec-23, Volume: 79, Issue:12
Antioxidant Flavonols and Phenolic Compounds from Atraphaxis frutescens and Their Inhibitory Activities against Insect Phenoloxidase and Mushroom Tyrosinase.
AID548347Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 3 uM after 24 hrs by UV-vis spectroscopy2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1647676Neuroprotective activity against glutamate-induced cell damage in mouse HT22 assessed as increase cell viability at 1.3 to 15 uM after 24 hrs by luminescent cell viability assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
Palhinosides A-H: Flavone Glucosidic Truxinate Esters with Neuroprotective Activities from
AID1713222Antioxidant activity assessed as DPPH radical scavenging activity incubated for 60 mins in absence of light2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1252287Inhibition of Fe-dependent reactive oxygen species formation at 10 to 5000 uM after 90 mins by H2DCF-DA-based fluorescence assay2015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
A multifunctional, light-activated prochelator inhibits UVA-induced oxidative stress.
AID1892586Antioxidant activity assessed as DPPH radical scavenging activity at 5 uM incubated for 30 mins by DPPH assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID403309DPPH radical scavenging activity assessed as ratio of IC50 for trolox to IC50 for test compound2004Journal of natural products, Jul, Volume: 67, Issue:7
New lamellarin alkaloids from the Indian ascidian Didemnum obscurum and their antioxidant properties.
AID604212Antioxidant activity assessed as inhibition of DPPH free radicals at 1 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID458692Cytotoxicity against human MG63 cells assessed as cell death at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1424254Antioxidant activity assessed as effect on linolenic acid autooxidation in presence of DLPC liposomes2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID751207Antioxidant activity in rat PC12 cells assessed as inhibition of Fe2+-induced ROS production after 1 hr by DCFH-DA staining-based fluorometric analysis2013Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.
AID218995Oxidation was assessed indirectly by measuring bovine serum albumin(BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 100 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID492253Antioxidant activity assessed as ABTS radical scavenging activity2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Tryptamine-derived alkaloids from Annonaceae exerting neurotrophin-like properties on primary dopaminergic neurons.
AID492248Antioxidant activity in mesecephalic neuron assessed as ROS production at 10 uM by dihydrorhodamine-123 incorporation assay relative to control2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Tryptamine-derived alkaloids from Annonaceae exerting neurotrophin-like properties on primary dopaminergic neurons.
AID281656Hydroxyl radical scavenging activity after 2 hrs by ABTS competition assay2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Effects of indole fatty alcohols on the differentiation of neural stem cell derived neurospheres.
AID195018The concentration of compound required to inhibit generation of superoxide by 50 percent in rat liver1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
AID1436065Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as reduction in LDH release at 100 uM pretreated for 2 hrs followed by H2O2 challenge measured after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID427663Antioxidant activity assessed as potassium ferric cyanide ion reducing power after 10 mins by Oyaizu method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Potential antioxidants and tyrosinase inhibitors from synthetic polyphenolic deoxybenzoins.
AID1892578Antioxidant activity in rat brain homogenate assessed as inhibition of lipid peroxidation by measuring MDA concentration at 1 uM by TBARS assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID1767564Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM incubated for 1 hrs under light restrictive condition by UV-microplate reader assay relative to control2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID459648Cytotoxicity against human SH-SY5Y cells assessed as cell death at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1083352Antioxidant activity assessed as DPPH radical scavenging activity at 5 X 10'-5 M after 60 min2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1592381Cytotoxicity against human SH-SY5Y cells assessed as cell metabolic activity at 50 uM incubated for 24 hrs by MTT assay relative to control
AID181705Compound was evaluated for prevention of spontaneous lipid peroxidation in rat brain homogenate.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
A cardioselective, hydrophilic N,N,N-trimethylethanaminium alpha-tocopherol analogue that reduces myocardial infarct size.
AID1298962Reduction of MDA level in Wistar rat brain at 100 uM after 30 mins in presence of ascorbic acid by UV-vis spectrophotmetry relative to control2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of benzothiadiazine derivatives exhibiting dual activity as aldose reductase inhibitors and antioxidant agents.
AID1729067Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM incubated for 30 mins under dark condition relative to control2021European journal of medicinal chemistry, Mar-05, Volume: 213A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities.
AID462444Antioxidant activity assessed as DPPH radical scavenging activity at 0.2 mM2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
AID1713235Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 25 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1372027Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced alkoxyl scavenging activity by measuring Kaox/Kst ratio using DMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1248048Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 200 ug/ml after 3 hrs by TBA-MDA test2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis, electronic properties, antioxidant and antibacterial activity of some new benzimidazoles.
AID1298960Antioxidant activity assessed as DPPH free radical scavenging activity at 1 uM after 40 mins by UV-Vis spectrophotometry2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of benzothiadiazine derivatives exhibiting dual activity as aldose reductase inhibitors and antioxidant agents.
AID592727Antioxidant activity assessed as inhibition of free radical production at 0.58 mM within 6 mins by ABTS+ decolorization assay2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
In vitro and QSAR studies of cucurbitacins on HepG2 and HSC-T6 liver cell lines.
AID548181Antioxidant activity assessed as DPPH radical scavenging activity2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Benzophenones and biflavonoids from Rheedia edulis.
AID240679Anti-oxidant activity in DPPH radical scavenging assay; n=3-42005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.
AID1743179Antioxidant activity assessed as AAPH scavenging activity by measuring residual fluorescence at 50 uM measured at 1 min interval for 30 mins by ORAC fluorescein assay relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1357811Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation after 24 hrs by thioflavin-T fluorescence assay2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID490943Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 20 mins2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID639369Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as LDH release at 3 uM incubated for 24 hrs before H2O2 challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1892589Antioxidant activity in rat brain homogenate assessed as inhibition of lipid peroxidation by measuring MDA concentration at 100 uM by TBARS assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID1596339Antioxidant activity assessed as DPPH free radical scavenging activity at 10 uM after 30 mins incubation in dark by UV-Visible spectrophotometric analysis relative to control2019European journal of medicinal chemistry, Jul-15, Volume: 174Multi-targeted ChEI-copper chelating molecules as neuroprotective agents.
AID125798Evaluated for the antioxidant property by measuring the inhibition of microsomal lipid peroxidation2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
Synthesis and evaluation of caffeic acid amides as antioxidants.
AID248540Inhibition concentration against lipid peroxidation initiated by [Fe2+] and L-ascorbic acid in rat brain homogenates2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and evaluation of 6-hydroxy-7-methoxy-4-chromanone- and chroman-2-carboxamides as antioxidants.
AID548959Antioxidant activity against AAPH-induced lipid peroxidation assessed as inhibition of conjugated diene hydroperoxide production at 0.1 mM by UV spectrophotometry2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Does conjugation of antioxidants improve their antioxidative/anti-inflammatory potential?
AID683737Antioxidant activity against AAPH-induced lipid peroxidation assessed as induction time of inhibition at 0.1 mM2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Α-aryl-N-alkyl nitrones, as potential agents for stroke treatment: synthesis, theoretical calculations, antioxidant, anti-inflammatory, neuroprotective, and brain-blood barrier permeability properties.
AID1320872Inhibition of human serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method2016European journal of medicinal chemistry, Oct-04, Volume: 121New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
AID550004Antioxidant activity assessed as ABTS radical scavenging activity by decolorization assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Terpenoids from the aerial parts of Parasenecio deltophylla.
AID567041Antioxidant activity assessed as Fe3+/ascorbic acid-induced hydroxyl radical scavenging activity at 0.1 mM2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.
AID442507Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 100 uM2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Syntheses and evaluation of the antioxidant activity of acitretin analogs with amide bond(s) in the polyene spacer.
AID457182Antioxidant activity assessed as hydroxyl radical scavenging activity by chemiluminescence assay2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Quiquelignan A-H, eight new lignoids from the rattan palm Calamus quiquesetinervius and their antiradical, anti-inflammatory and antiplatelet aggregation activities.
AID277123DPPH radical scavenging activity2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent.
AID1318718Antioxidant activity assessed as DPPH free radical scavenging activity at 100 uM after 30 mins by UV-spectrophotometric method relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121A series of pyrido[2,3-b]pyrazin-3(4H)-one derivatives as aldose reductase inhibitors with antioxidant activity.
AID1143751Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 1 uM co-incubated with rotenone-oligomycin measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID1333872Antioxidant activity assessed as reduction in AAPH free radical-induced linoleic acid peroxidation activity measured at 100 ug/ml by UV spectroscopic analysis2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Synthesis of new morpholine-connected pyrazolidine derivatives and their antimicrobial, antioxidant, and cytotoxic activities.
AID406774DPPH radical scavenging activity at 100 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Efficient synthesis and neuroprotective effect of substituted 1,3-diphenyl-2-propen-1-ones.
AID1474956Antioxidant activity assessed as ABTS radical scavenging activity at 1 mg/ml incubated for 2 hrs in dark by spectrophotometric analysis (Rvb = 1 to 9%)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID264485Viability of rotifers against hydrogen peroxide toxicity at 10 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID228717Antioxidant efficiency of compounds was evaluated by the lag phase duration until onset of linoleate peroxidation induced by AAPH2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Protective effect of imidazolopyrazinone antioxidants on ischemia/reperfusion injury.
AID490948Antioxidant activity assessed as inhibition of lipid peroxidation at 10 uM2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID1075988Neuroprotective activity against H2O2-induced oxidative stress in mouse/rat NG108-15 cells assessed as cell viability at 100 uM incubated for 2 hrs prior to H2O2 challenge for 2 hrs by MTT assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1543564Neuroprotective activity against H2O2-induced oxidative damage in human SH-SY5Y cells assessed as cell viability at 10 uM measured after 24 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease.
AID1306595Cytoprotective activity in HMEC1 assessed as inhibition of oxidized LDL induced toxicity measured as residual viability at 1 uM after 24 hrs by MTT assay (Rvb = 20 +/- 5 %)2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID196391Compound was evaluated for its inhibitory concentration against [Fe2+]/AA- induced oxidative neuronal damage in primary cultured rat cortical cells2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Synthesis and evaluation of 4-hydroxyphenylacetic acid amides and 4-hydroxycinnamamides as antioxidants.
AID419627Antioxidant activity in 2',7'-dichlorodihydrofluorescein diacetate-treated human MCF7 cells assessed as reduction of H2O2 production at 100 uM during after 24 hrs by FACS analysis2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Synthesis and antioxidant potential of novel synthetic benzophenone analogues.
AID1071843Antioxidant activity assessed as AAPH-induced alkoxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1083349Inhibition of Glycine max (soybean) lipoxygenase using sodium linoleate as substrate at 1 X 10'-42011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1406257Antioxidant activity assessed as DPPH free radical scavenging activity after 90 mins dark incubation2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID1372032Antioxidant activity assessed as rate constant for photolysis-induced methyl radical scavenging activity using DMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1610481Inhibition of human erythrocyte AChE at 20 uM using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method relative to control2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.
AID1179727Antioxidant activity assessed as DPPH radical scavenging activity by UV-Visible spectrophotometry2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID1228329Antioxidant activity assessed as inhibition of AAPH-induced crocin oxidation in hydrophilic medium at 5 to 500 uM by crocin bleaching assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Interaction of α-Hexylcinnamaldehyde with a Biomembrane Model: A Possible MDR Reversal Mechanism.
AID1603220Antioxidant activity assessed as DPPH radical scavenging activity at 1 uM relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID1624742Antioxidant activity assessed as hydroxyl radical scavenging activity at 0.1 mM measured after 30 mins2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment.
AID639456Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 3 uM treated 24 hrs before rotenone/oligomycin A challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1437794Antioxidant activity of the compound assessed as DPPH radical scavenging activity after 30 mins2017European journal of medicinal chemistry, Feb-15, Volume: 127Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.
AID1713238Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 3.1 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID469935Antioxidant activity assessed as DPPH radical scavenging activity2009Journal of natural products, Aug, Volume: 72, Issue:8
Constituents of the leaves of Magnolia ovata.
AID459651Cytotoxicity against human MG63 cells assessed as plasma membrane damage at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1326568Antioxidant activity in Salmonella typhimurium TA102 harboring hysG428 mutant assessed as inhibition of t-BuO2H-dependant mutant formation at 30 uM preincubated with compound followed by t-BuO2H addition after 48 hrs by Ames test2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID401039Antioxidant activity assessed as DPPH radical scavenging activity1998Journal of natural products, May, Volume: 61, Issue:5
Isolation, identification, and antioxidant activity of three stilbene glucosides newly extracted from vitis vinifera cell cultures
AID1713226Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 50 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1326582Cytotoxicity against mouse LMTK cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1435201Antioxidant activity assessed as DPPH radical scavenging activity incubated for 15 mins under dark condition2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
New insights into highly potent tyrosinase inhibitors based on 3-heteroarylcoumarins: Anti-melanogenesis and antioxidant activities, and computational molecular modeling studies.
AID551409Antioxidant activity assessed as hydroxyl radical scavenging activity at 50 uM after 2 hrs by benzoic acid method2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Synthesis, structure, theoretical and experimental in vitro antioxidant/pharmacological properties of α-aryl, N-alkyl nitrones, as potential agents for the treatment of cerebral ischemia.
AID635123Inhibition of mushroom tyrosinase activity using L-tyrosin as substrate after 20 mins2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Inhibitory activity of novel kojic acid derivative containing trolox moiety on melanogenesis.
AID1581658Antioxidant activity assessed as ABTS radical scavenging activity at 150 uM measured after 60 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID197084Inhibition of in vitro peroxidation (LP) of rat Hepatic microsomal membrane lipid2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Novel potent inhibitors of lipid peroxidation with protective effects against reperfusion arrhythmias.
AID452854Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 10 uM by uV spectrophotometry2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID426426Inhibition of soybean lipoxygenase assessed as conversion of sodium linoleate to 13-hydroperoxylinoleic acid at 0.1 mM2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.
AID1310990Antioxidant activity assessed as DPPH scavenging activity measured after 3 mins by spectrophotometric method2016European journal of medicinal chemistry, Aug-25, Volume: 119On the vasoprotective mechanisms underlying novel β-phosphorylated nitrones: Focus on free radical characterization, scavenging and NO-donation in a biological model of oxidative stress.
AID1381602Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 30 mins dark incubation2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
AID619936Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 36 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1311931Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.
AID1323133Antioxidant activity assessed as DPPH free radical scavenging activity at 5 uM after 15 to 60 mins in presence of CuSO4.5H2O2016Journal of natural products, 07-22, Volume: 79, Issue:7
Effects of Functional Groups and Sugar Composition of Quercetin Derivatives on Their Radical Scavenging Properties.
AID1474958Antioxidant activity assessed as ABTS radical scavenging activity at 2.5 mg/ml incubated for 2 hrs in dark by spectrophotometric analysis (Rvb = 1 to 9%)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID1228617Antioxidant activity assessed as hydroxy radical-scavenging activity2015Journal of natural products, May-22, Volume: 78, Issue:5
Anti-inflammatory Hydrolyzable Tannins from Myricaria bracteata.
AID1264042Neuroprotective activity against Fenton reagent-induced hydroxy radical-stimulated cytotoxicity in human ARPE19 cells assessed as cell survival at 1 to 1000 uM preincubated for 1 hr followed by Fenton reagent challenge for 2 hrs by fluorescence-based LIVE2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID450086Antioxidant activity assessed as ABTS radical scavenging activity2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Antioxidant activity of 5,10-dihydroindeno[1,2-b]indoles containing substituents on dihydroindeno part.
AID1603218Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID548346Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 1 uM after 24 hrs by UV-vis spectroscopy2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1678472Antioxidant activity in pH 4.5 phosphate buffer assessed as PTIO radical scavenging activity after 1 hr by microplate reader based assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-
AID356014Antioxidant activity assessed as inhibition of AAPH-induced hemolysis in rat RBC after 3 hrs2003Journal of natural products, Jun, Volume: 66, Issue:6
Antioxidative glycosides from the leaves of Ligustrum robustum.
AID1264035Cytotoxicity against human ARPE19 cells assessed as reduction in cell viability at 1 mM after 2 hrs by MTS assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1348939Inhibition of xanthine oxidase (unknown origin) using xanthine as substrate preincubated for 5 mins followed by substrate addition measured every min for 10 mins by spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1143752Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 3 uM co-incubated with rotenone-oligomycin measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID1300892Antioxidant activity of the compound after 30 mins by CUPRAC method2016European journal of medicinal chemistry, Jul-19, Volume: 117Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.
AID1892587Antioxidant activity assessed as DPPH radical scavenging activity at 1 uM incubated for 30 mins by DPPH assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID536051Antioxidant activity assessed as protection against Fenton oxidation-induced thymidine degradation in 11.4 mM phosphate buffer at 100 uM by competitive immuno-enzymatic assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Synthesis and antioxidant properties of pulvinic acids analogues.
AID1721452Antioxidant activity assessed as DPPH radical scavenging activity incubated for 1 hr under dark condition2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.
AID34986In vitro inhibitory activity against aldose reductase of rat lens at 10E-5 M concentration2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID549274Antioxidant activity in mouse BNL-CL2 cells assessed as inhibition of H2O2-induced ROS production at 20 ug/ml by DCFHDA assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Inhibition of melanogenesis and oxidation by protocatechuic acid from Origanum vulgare (oregano).
AID1152636Antioxidant activity assessed as hydroxyl radical scavenging activity at 5 uM after 1 hr by 2-Deoxy-D-ribose degradation assay in presence of FeCl3 and EDTA2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Synthesis and radical scavenging activity of phenol-imidazole conjugates.
AID497109Antioxidant activity assessed as DPPH free radical scavenging activity at 100 uM after 1 hr2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
AID619931Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 6 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1610479Inhibition of porcine liver carboxylesterase using 4-NPA as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.
AID286753Antioxidant activity assessed as DPPH reducing activity at 0.1 mM after 20 mins2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.
AID344046Antioxidant activity assessed as superoxide radical anion scavenging activity after 8 mins2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Cyathuscavins A, B, and C, new free radical scavengers with DNA protection activity from the Basidiomycete Cyathus stercoreus.
AID1480871Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 100 uM pretreated for 30 mins followed by glutamate challenge after 10 hrs by DCFH-DA probe based FACS an2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID567040Antioxidant activity assessed as Fe3+/ascorbic acid-induced hydroxyl radical scavenging activity at 0.01 mM2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.
AID1143540Antioxidant activity assessed as DPPH radical scavenging activity by spectrophotometric analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Thiaflavan scavenges radicals and inhibits DNA oxidation: a story from the ferrocene modification.
AID663248Neuroprotective activity in human SH-SY5Y cells assessed as protection against H2O2-induced oxidative stress at 30 uM incubated for 1 hr prior to H2O2-challenge measured after 12 hrs by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases.
AID1126662Antioxidant activity assessed as DPPH radical scavenging activity by spectrophotometry2014European journal of medicinal chemistry, May-06, Volume: 78One-pot synthesis and radical scavenging activity of novel polyhydroxylated 3-arylcoumarins.
AID1256878Selectivity ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1534716Antioxidant activity assessed as ferric ion reduction by measuring trolox equivalents after 3 to 5 mins by FRAP assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID1264038Neuroprotective activity against Fenton reagent-induced ROS generation in human SH-SY5Y cells assessed as increase in GSH level at 1 mM after 2 hrs by DTNB method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1678101Antioxidant activity assessed as DPPH radical scavenging activity at 5 uM relative to control2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID471315Antioxidant activity assessed as ABTS radical scavenging activity2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Captopril and 6-mercaptopurine: whose SH possesses higher antioxidant ability?
AID1326573Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID489923Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 100 uM by UV spectrophotometry2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
A novel synthesis of 3-aryl coumarins and evaluation of their antioxidant and lipoxygenase inhibitory activity.
AID235285Free radical scavenging assessed as DPPH color reduction2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship.
AID1382194Antioxidant activity assessed as ferric ion reduction by measuring FeSO4 equivalents reducing Fe3+-TPTZ to Fe2+-TPTZ measured every 15 secs for 4 mins by FRAP assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Regioselective synthesis of 7-O-esters of the flavonolignan silibinin and SARs lead to compounds with overadditive neuroprotective effects.
AID277126Cytotoxicity against microglial cells at 25 uM2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent.
AID1424236Antioxidant activity assessed as peroxyl radical scavenging activity by measuring rate constants for hydrogen atom transfer from substituted phenols to polystyrene peroxyl radicals2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID427661Antioxidant activity assessed as inhibition of FeCl2-induced lipid peroxidation by thiocyanate method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Potential antioxidants and tyrosinase inhibitors from synthetic polyphenolic deoxybenzoins.
AID759441Antioxidant activity in human SH-SY5Y cells assessed as decrease in t-BuOOH-induced intracellular ROS production at 5 to 20 uM incubated for 24 hrs prior to t-BuOOH challenge measured after 30 mins by DCFHDA-based fluorescence assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Design, synthesis, and evaluation of multitarget-directed resveratrol derivatives for the treatment of Alzheimer's disease.
AID1628628Cytoprotection against AAPH-induced haemolysis in human erythrocytes at 0.01 to 1 mg/l pre-incubated for 20 mins before 60 mM AAPH addition for 4 hrs by spectrophotometric analysis2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Antioxidant properties of thio-caffeine derivatives: Identification of the newly synthesized 8-[(pyrrolidin-1-ylcarbonothioyl)sulfanyl]caffeine as antioxidant and highly potent cytoprotective agent.
AID1083335Antiviral activity against Mammalian orthoreovirus 1 infected VERO cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1399480Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics.
AID344044Antioxidant activity assessed as DPPH radical scavenging activity after 10 mins2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Cyathuscavins A, B, and C, new free radical scavengers with DNA protection activity from the Basidiomycete Cyathus stercoreus.
AID567050Antioxidant activity assessed as reduction of ABTS radical at 0.1 mM2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.
AID594793Antioxidant activity in rat liver homogenates assessed as inhibition of lipid peroxidation by measuring formation of thiobarbituric acid-reactive substance after 30 mins2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors.
AID1713224Antioxidant activity in human SH-SY5Y cells assessed as inhibition of H2O2-induced DCFH oxidation measured after 1 hr by DCFH-DA dye based fluorescence assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID197085The compound was evaluated for the interaction with 0.2 mM of the stable free radical DPPH2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Novel potent inhibitors of lipid peroxidation with protective effects against reperfusion arrhythmias.
AID1330214Aqueous solubility of the compound in sodium phosphate buffer at pH 6.8 after 24 hrs by shake flask method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Synthesis and biological assessment of novel N-(hydroxy/methoxy)alkyl β-enaminone curcuminoids.
AID1194492Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins by UV absorption spectrometry2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities.
AID378808Antioxidant activity assessed as inhibition of total reactive oxygen species generation in Wistar rat kidney by 2',7'-dichlorofluorescein based fluorescence spectroscopy2006Journal of natural products, Oct, Volume: 69, Issue:10
Antioxidative phenolics from the fresh leaves of Ternstroemia japonica.
AID635125Depigmentation activity in mouse Melan-a cells assessed as inhibition of melanin formation after 4 days2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Inhibitory activity of novel kojic acid derivative containing trolox moiety on melanogenesis.
AID774815Antioxidant activity assessed as ferric ion reducing activity using ferric-TPTZ by measuring concentration of compound with antioxidant capacity equivalent to ferrous sulfate at 0.5 mmol/L by FRAP assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antioxidant activity of novel Mannich base of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan.
AID277124Cytotoxicity against microglial cells at 5 uM2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent.
AID537164Antioxidant activity in L-alpha-phosphatidylcholine dioleoyl liposome assessed as inhibition of AAPH-induced lipid peroxidation by LOOH assay2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID604214Antioxidant activity assessed as inhibition of ABTS free radicals at 0.1 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID344830Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
New diterpenoids and the bioactivity of Erythrophleum fordii.
AID1381603Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM after 30 mins dark incubation2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
AID426422Antioxidant activity against hydroxyl radical assessed as inhibition of formaldehyde production at 0.1 mM after 30 mins relative to DMSO2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.
AID1155646Antioxidant activity assessed as reduction of TPTZ-Fe3+ to TPTZ-Fe2+ at 0.15 to 1.5 mM after 5 mins by FRAP assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Lignans from the fruit of Schisandra glaucescens with antioxidant and neuroprotective properties.
AID1402940Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 30 uM after 18 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Synthesis and biological evaluation of diarylheptanoids as potential antioxidant and anti-inflammatory agents.
AID1892581Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 30 mins by DPPH assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID619935Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 30 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1563226Antioxidant activity in pH 7.4 phosphate buffer assessed as DPPH radical scavenging activity after 30 mins by spectrophotometric analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Synthesis and Biological Assessment of Pyrrolobenzoxazine Scaffold as a Potent Antioxidant.
AID683736Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 0.1 mM by UV spectrophotometric analysis2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Α-aryl-N-alkyl nitrones, as potential agents for stroke treatment: synthesis, theoretical calculations, antioxidant, anti-inflammatory, neuroprotective, and brain-blood barrier permeability properties.
AID406773DPPH radical scavenging activity at 50 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Efficient synthesis and neuroprotective effect of substituted 1,3-diphenyl-2-propen-1-ones.
AID731498Antioxidant activity assessed as inhibition of xanthine-xanthine oxidase generated superoxide anion radical production by NBT reduction assay2013Journal of natural products, Jan-25, Volume: 76, Issue:1
Neolignanamides, lignanamides, and other phenolic compounds from the root bark of Lycium chinense.
AID203497Formation of DNPH-reactive carbonyl groups in bovine serum albumin exposed to fructose; p<0.0012003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID203469In vitro ability to inhibit the irreversible modification of the model protein albumin in the presence of fructose as glycating agent (1 mM)2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID1348941Antioxidant activity assessed as DPPH radical scavenging activity at 30 uM after 60 mins by spectrophotometric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1083338Antiviral activity against Vaccinia virus infected human HEL cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1324204Antioxidant activity assessed as ABTS radical scavenging activity after 6 mins by spectrophotometric analysis2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID427664Antioxidant activity assessed as ABTS radical scavenging activity2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Potential antioxidants and tyrosinase inhibitors from synthetic polyphenolic deoxybenzoins.
AID1406253Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 1 min by Ellman's assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID1589464Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM incubated for 30 mins under dark condition by spectrophotometry2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID550003Antioxidant activity assessed as DPPH radical scavenging activity2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Terpenoids from the aerial parts of Parasenecio deltophylla.
AID403308Antioxidant activity assessed as DPPH radical scavenging activity by HPLC2004Journal of natural products, Jul, Volume: 67, Issue:7
New lamellarin alkaloids from the Indian ascidian Didemnum obscurum and their antioxidant properties.
AID1592385Electrochemical behavior of the compound assessed as redox potential corrected toward saturated Ag/AgCl reference electrode by cyclic voltammetry
AID653293Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation by measuring conjugated diene hydroperoxide level2012European journal of medicinal chemistry, May, Volume: 51Novel NSAID 1-acyl-4-cycloalkyl/arylsemicarbazides and 1-acyl-5-benzyloxy/hydroxy carbamoylcarbazides as potential anticancer agents and antioxidants.
AID196215Ability to protect cerebellar granule cells (CGC) from iodoacetate (IAA)-induced toxicity2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID770310Antioxidant activity assessed as AAPH-induced free radical scavenging activity at 25 uM preincubated for 30 mins followed by AAPH induction measured every 5 mins for 9 hrs by ORAC assay relative to vehicle-treated control2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
Discovery of novel (1S)-(-)-verbenone derivatives with anti-oxidant and anti-ischemic effects.
AID604213Antioxidant activity assessed as inhibition of ABTS free radicals at 0.01 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID1762403Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method2021European journal of medicinal chemistry, Jun-05, Volume: 218Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
AID1330213Aqueous solubility of the compound in sodium phosphate buffer at pH 6.8 after 90 mins by shake flask method2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Synthesis and biological assessment of novel N-(hydroxy/methoxy)alkyl β-enaminone curcuminoids.
AID1399484Inhibition of porcine liver carboxylesterase using 4-nitrophenol acetate as substrate incubated for 10 mins followed by substrate addition by spectrophotometric method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics.
AID1755237Antioxidant activity assessed as trolox equivalent antioxidant capacity
AID1326576Cytotoxicity against hamster AG17-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID751209Antioxidant activity assessed as free radical scavenging activity after 7 mins by ABTS radical cation decolorization assay2013Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12
Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.
AID1228618Antioxidant activity assessed as DPPH radical-scavenging activity incubated for 30 mins by spectrophotometry2015Journal of natural products, May-22, Volume: 78, Issue:5
Anti-inflammatory Hydrolyzable Tannins from Myricaria bracteata.
AID1581664Antioxidant activity assessed as increase in total ferric ion reducing activity at 150 uM using FeCl3.H2O and TPTZ incubated for 30 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID548353Neuroprotective activity against rotenone and oligomycin-induced mitochondrial oxidative stress in human SH-SY5Y cells assessed as LDH release at 30 uM after 24 hrs using DCFH-DA fluorescent dye2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID504308Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NO production after 24 hrs2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Antioxidant and anti-inflammatory phenylpropanoid derivatives from Calamus quiquesetinervius.
AID619942Antioxidant activity assessed as ferric to ferrous reduction at 30 ug/ml by FRAP assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1563219Antioxidant activity in pH 7.4 potassium phosphate buffer assessed as CuCl2/ascorbic acid induced hydroxyl radical scavenging activity by measuring deoxyribose degradation product formation after 20 mins by thiobarbituric acid based absorbance analysis2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Synthesis and Biological Assessment of Pyrrolobenzoxazine Scaffold as a Potent Antioxidant.
AID1143750Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 0.3 uM co-incubated with rotenone-oligomycin measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID736835Antioxidant activity assessed as DPPH free radical scavenging activity at 20 uM2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship study of vitamin k derivatives yields highly potent neuroprotective agents.
AID1071844Antioxidant activity assessed as riboflavin/EDTA-induced superoxide anion radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1729071Antioxidant activity assessed as ABTS radical scavenging activity at 10 uM relative to control2021European journal of medicinal chemistry, Mar-05, Volume: 213A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities.
AID1810904Binding affinity to human serum BChE assessed as half life
AID1326572Cytotoxicity against human CEM13 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID490949Antioxidant activity assessed as inhibition of lipid peroxidation at 100 uM2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID247539In vitro inhibitory concentration against NO (nitrous oxide)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Nitrone derivatives of trolox as neuroprotective agents.
AID616482Antioxidant activity assessed as DPPH free radical scavenging activity2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and antioxygenic activities of seabuckthorn flavone-3-ols and analogs.
AID419626Antioxidant activity in 2',7'-dichlorodihydrofluorescein diacetate-treated hTERT-HME1 cells assessed as reduction of H2O2 production at 100 uM during after 24 hrs by FACS analysis2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Synthesis and antioxidant potential of novel synthetic benzophenone analogues.
AID1713240Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 0.8 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1713237Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 6.3 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1480857Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as increase in cell viability at 100 uM pretreated for 30 mins followed by glutamate challenge measured after 24 hrs by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1083339Antiviral activity against Human herpesvirus 2 strain G infected human HEL cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1428458Inhibition of mushroom tyrosinase using L-DOPA as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by spectrophotometric method2016Journal of natural products, Dec-23, Volume: 79, Issue:12
Antioxidant Flavonols and Phenolic Compounds from Atraphaxis frutescens and Their Inhibitory Activities against Insect Phenoloxidase and Mushroom Tyrosinase.
AID1083334Antiviral activity against Human coxsackievirus B4 infected VERO cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID380424Cytotoxicity against human HL60 cells by XTT assay2006Journal of natural products, Mar, Volume: 69, Issue:3
Schisandrene, a dibenzocyclooctadiene lignan from Schisandra chinensis: structure-antioxidant activity relationships of dibenzocyclooctadiene lignans.
AID1083347Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 1 X 10'-4 M2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1071842Antioxidant activity assessed as t-butylhyroperoxide-induced alkylperoxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1659475Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM relative to control2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID469416Neuroprotective activity against human SH-SY5Y cells assessed as cytoprotection at 3 uM coincubated with rotenone/oligomycin A measured after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1379030Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.
AID1603222Antioxidant activity in rat brain homogenate assessed as inhibition of FeCl2/ascorbic acid-induced lipid peroxidation by measuring reduction in TBARS level at 50 uM measured after 30 mins by spectrophotometric method relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID387150Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
ortho-dihydroxyisoflavone derivatives from aged Doenjang (Korean fermented soypaste) and its radical scavenging activity.
AID1143541Antioxidant activity assessed as galvinoxyl radical scavenging activity by spectrophotometric analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Thiaflavan scavenges radicals and inhibits DNA oxidation: a story from the ferrocene modification.
AID1655201Antioxidant activity assessed as ABTS radical scavenging activity incubated for 40 mins2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
AID1238056Antioxidant activity assessed as DPPH radical scavenging activity at 200 uM incubated for 30 mins under dark conditions2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Nitric oxide inhibitory activity and antioxidant evaluations of 2-benzoyl-6-benzylidenecyclohexanone analogs, a novel series of curcuminoid and diarylpentanoid derivatives.
AID1333862Antioxidant activity assessed as ABTS radical scavenging activity at 100 ug/ml after 30 mins2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Synthesis of new morpholine-connected pyrazolidine derivatives and their antimicrobial, antioxidant, and cytotoxic activities.
AID469414Neuroprotective activity against human SH-SY5Y cells assessed as cytoprotection at 0.3 uM coincubated with rotenone/oligomycin A measured after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID497112Antioxidant activity assessed as ABTS free radical scavenging activity after 12 hrs2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
AID1436860Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM after 240 mins by UV spectrophotometer relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis and structure-activity relationship studies of phenolic hydroxyl derivatives based on quinoxalinone as aldose reductase inhibitors with antioxidant activity.
AID1324203Antioxidant activity assessed as hydroxyl radical scavenging activity measured 10 mins after H2O2 addition by pyronin B dye based assay2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID1647679Neuroprotective activity in human SH-SY5Y cells assessed as reduction in H2O2-induced cell death at 1 uM preincubated for 1 hr followed by H2O2 addition and measured after 4 hrs by MTT assay relative to control2020Journal of natural products, 02-28, Volume: 83, Issue:2
Modified Eremophilanes from
AID1755235Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation incubated for 24 hrs by Thioflavin T based fluorometric assay
AID288848Antioxidant activity assessed as ABTS radical scavenging activity after 30 mins2007Journal of natural products, Jun, Volume: 70, Issue:6
Cyathusals A, B, and C, antioxidants from the fermented mushroom Cyathus stercoreus.
AID264484Inhibition of doxorubicin-induced death of mixed cortical cells of E15 Sprague-Dawley rat embryo at 10 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID1493751Antioxidant activity assessed as cupric ion reducing activity after 30 mins by CUPRAC assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID1320870Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method2016European journal of medicinal chemistry, Oct-04, Volume: 121New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
AID1480864Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 50 uM pretreated for 30 mins followed by glutamate challenge measured after 6 hrs by DCFH-DA probe based 2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1624744Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalents at 10 uL after 1 min2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment.
AID1592389Cytotoxicity against human HepG2 cells assessed as cell metabolic activity at 50 uM incubated for 48 hrs by resazurin assay relative to control
AID1306594Cytotoxicity against HMEC1 assessed as cell viability at 1 uM after 24 hrs by MTT assay in absence of oxidized LDL2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1256880Inhibition of human recombinant AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID445120Antioxidant activity assessed as protection against AAPH-induced pBR322 plasmid DNA strand open circular form at 0.35 to 45 uM after 4 hrs by agarose gel electrophoresis2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antioxidant properties of dendritic polyphenols.
AID1141997Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid peroxidation by UV spectrophotometric analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes and evaluation of their antioxidant and lipid peroxidation activity.
AID1306597Antiangiogenic activity in HMEC1 assessed as inhibition of oxidized LDL induced tube formation at 10 uM after 18 hrs by calcein staining based fluorescence microscopy2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID504305Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by ELISA reader2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Antioxidant and anti-inflammatory phenylpropanoid derivatives from Calamus quiquesetinervius.
AID1480859Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as normal neurite appearance at 100 uM pretreated for 30 mins followed by glutamate challenge measured after 18 hrs by phase-contrast microscopic method2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1596340Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins incubation in dark by UV-Visible spectrophotometric analysis2019European journal of medicinal chemistry, Jul-15, Volume: 174Multi-targeted ChEI-copper chelating molecules as neuroprotective agents.
AID1326577Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID490422Antioxidant activity against superoxide radical generation in HMEC1 cells2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antioxidant activity evaluation of a syringic hydrazones family.
AID1729655Neuroprotective activity against H2O2-induced lipid peroxidation in mouse SN-56 cells assessed as increase in MDA level at 100 uM incubated for 24 hrs by lipid peroxidation MDA assay kit method2021European journal of medicinal chemistry, Jan-15, Volume: 210Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity.
AID471313Antioxidant activity assessed as DPPH radical scavenging activity2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Captopril and 6-mercaptopurine: whose SH possesses higher antioxidant ability?
AID1474954Antioxidant activity assessed as ABTS radical scavenging activity incubated for 2 hrs in dark by spectrophotometric analysis2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID440884Antioxidant activity against Fe3+/ascorbic acid system generated hydroxyl radicals assessed as inhibition of formaldehyde production at 0.1 mM2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins.
AID1678471Antioxidant activity in pH 7.4 phosphate buffer assessed as PTIO radical scavenging activity after 1 hr by microplate reader based assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-
AID1859601Antioxidant activity assessed as DPPH radical scavenging activity incubated for 1 hrs under dark condition by DPPH assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1534714Antioxidant activity assessed as inhibition of DPPH free radical after 30 mins by UV-Visible spectrophotometric analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID778759Antioxidant activity assessed as inhibition of H2O2-induced ROS production by DCFH assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Multifunctional cyclic D,L-α-peptide architectures stimulate non-insulin dependent glucose uptake in skeletal muscle cells and protect them against oxidative stress.
AID1651606Cytoprotective activity against LPS-induced NRK-52E cells assessed as reduction in cell death measured every 5 min for 72 hrs by xCELLigence based RTCA analysis2020Journal of natural products, 04-24, Volume: 83, Issue:4
Renoprotective Mono- and Triterpenoids from the Fruit of
AID1264037Neuroprotective activity against Fenton reagent-induced ROS generation-stimulated cytotoxicity in human ARPE19 cells assessed as cell viability at 1 mM after 2 hrs by MTS assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1298959Antioxidant activity assessed as DPPH free radical scavenging activity at 10 uM after 40 mins by UV-Vis spectrophotometry2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of benzothiadiazine derivatives exhibiting dual activity as aldose reductase inhibitors and antioxidant agents.
AID1326571Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1306596Cytoprotective activity in HMEC1 assessed as inhibition of oxidized LDL induced toxicity measured as residual viability at 10 uM after 24 hrs by MTT assay (Rvb = 20 +/- 5 %)2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1326569Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1511011Antioxidant activity assessed as ABTS radical scavenging activity incubated for 40 mins2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID1713236Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 12.5 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID377346Antioxidant activity assessed as ABTS radical scavenging activity2005Journal of natural products, Feb, Volume: 68, Issue:2
Resveratrol derivatives from the roots of Vitis thunbergii.
AID406771DPPH radical scavenging activity at 200 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Efficient synthesis and neuroprotective effect of substituted 1,3-diphenyl-2-propen-1-ones.
AID1720092Antioxidant activity assessed as ABTS radical scavenging activity incubated in dark for 1 min2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Discovery of a new potent inhibitor of mushroom tyrosinase (Agaricus bisporus) containing 4-(4-hydroxyphenyl)piperazin-1-yl moiety.
AID1372026Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced methyl radical scavenging activity by measuring Kaox/Kst ratio using DMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1543559Antioxidant activity assessed as ABTS radical scavenging activity incubated for 6 mins2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease.
AID1083340Antiviral activity against Human simplex virus 1 KOS infected in human HEL cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1892585Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM incubated for 30 mins by DPPH assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID1327542Reactive carbonyl species trapping activity of compound assessed as MGO adduct formation at 10 mM preincubated for 24 hrs with MGO measured after 15 mins by LCMS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease.
AID1405944Antioxidant activity assessed as inhibition of lipid peroxidation relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Current progress on antioxidants incorporating the pyrazole core.
AID427138Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
p-Terphenyls from the fruiting bodies of Paxillus curtisii and their antioxidant properties.
AID635126Cytotoxicity against mouse Melan-a cells by modified crystal voilet assay2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Inhibitory activity of novel kojic acid derivative containing trolox moiety on melanogenesis.
AID380423Antioxidant activity in human HL60 cells assessed as inhibition of TPA-stimulated hydrogen peroxide induced DCFH-DA oxidation by fluorometric microplate assay2006Journal of natural products, Mar, Volume: 69, Issue:3
Schisandrene, a dibenzocyclooctadiene lignan from Schisandra chinensis: structure-antioxidant activity relationships of dibenzocyclooctadiene lignans.
AID1071840Antioxidant activity assessed as rosebengal-induced singlet oxygen radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1713230Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 3.1 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1762408Antioxidant activity assessed as decrease in ABTS radical cation scavenging activity incubated for 24 hrs by UV-Vis spectrophotometric analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
AID598280Antioxidant activity in rat liver homogenates assessed as inhibition of iron-ascorbic acid mix-induced lipid peroxidation after 30 mins by TBARS assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties.
AID537163DPPH radical scavenging activity assessed as initial rate of interaction at 0.2 mM2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID724354Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 100 uM by spectrophotometric analysis2013European journal of medicinal chemistry, Feb, Volume: 60Syntheses and evaluation of the antioxidant activity of novel methoxypsoralen derivatives.
AID1173942Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 100 uM2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
Structural modifications of coumarin derivatives: Determination of antioxidant and lipoxygenase (LOX) inhibitory activity.
AID1810910Inhibition of human AChE using acetylthiocholine iodide as substrate at 10 uM incubated for 20 mins followed by substrate addition by Ellman's method
AID1399482Inhibition of equine serum BChE using butylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics.
AID363318DPPH radical scavenging activity assessed as ratio of drug concentration to DPPH concentration producing 50% decrease in DPPH after 5 mins2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
AID1277568Antioxidant activity assessed as suppression of H2O2/DETAPAC-Fe2+-mediated hydroxyl radical formation by measuring oxidation of dihydrorhodamine after 5 mins by fluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Synthesis and biological evaluation of novel orally available 1-phenyl-6-aminouracils containing dimethyldihydrobenzofuranol structure for the treatment of allergic skin diseases.
AID1257023Anti-inflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip after 3.5 hrs2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Synthesis and biological evaluation of new C-10 substituted dithranol pleiotropic hybrids.
AID1143753Antioxidant activity in human SH-SY5Y cells assessed as rotenone-oligomycin-induced sequestering of mitochondrial free radicals at 0.3 uM after 120 mins using DCFH-DA by fluorescence microplate reader analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID184572Inhibition of spontaneous lipid peroxidation at 10e-5 M in rat brain homogenate1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity.
AID1465114Inhibition of pig liver carboxylesterase using 4-nitrophenol acetate as substrate by spectrophotometric analysis2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.
AID548348Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 30 uM after 24 hrs by UV-vis spectroscopy2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1372028Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced peroxyl scavenging activity by measuring Kaox/Kst ratio using CYPMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1592386Electrochemical behavior of the compound assessed as redox potential corrected toward saturated Ag/AgCl reference electrode by differential pulse voltammetry
AID1264028Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 1 mM after 2 hrs by MTS assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID762874Antioxidant activity assessed as hydroxyl radical scavenging activity at 1 mM after 5 mins by ESR spectroscopy analysis2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and electrochemical and biological studies of novel coumarin-chalcone hybrid compounds.
AID406772DPPH radical scavenging activity at 10 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Efficient synthesis and neuroprotective effect of substituted 1,3-diphenyl-2-propen-1-ones.
AID1374850Neuroprotective activity against tetracycline removal-induced cytotoxicity in human MC65 cells assessed as reduction in oxidative stress at 32 uM after 48 hrs by DCFH-DA dye based fluorescence assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Design and characterization of bivalent compounds as potential neuroprotectants for Alzheimer's disease: Impact of the spacer on biological activity.
AID459653Cytotoxicity against human SH-SY5Y cells assessed as plasma membrane damage at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID341426Antioxidant activity against tert-butyl hydroperoxide-induced ROS evoked cell death in human SH-SY5Y cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
AID504306Antioxidant activity assessed as hydroxyl radical scavenging activity by chemiluminescence analysis2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Antioxidant and anti-inflammatory phenylpropanoid derivatives from Calamus quiquesetinervius.
AID264483Inhibition of peroxynitrite-induced death of mixed cortical cells of E15 Sprague-Dawley rat embryo at 10 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID286756Antioxidant activity assessed as DPPH reducing activity at 0.5 mM after 60 mins2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.
AID1493977Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID1269946Antioxidant activity assessed as DPPH radical scavenging activity incubated for 20 mins by spectrophotometry analysis2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
An appraisal on recent medicinal perspective of curcumin degradant: Dehydrozingerone (DZG).
AID1320874Inhibition of human recombinant MAOA using p-tyramine as substrate incubated for 15 mins by fluorimetric method2016European journal of medicinal chemistry, Oct-04, Volume: 121New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
AID1320862Antioxidant activity assessed as AAPH free radical scavenging activity measured every min during 240 mins by fluorescein-based oxygen radical absorption capacity assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Do cinnamylideneacetophenones have antioxidant properties and a protective effect toward the oxidation of phosphatidylcholines?
AID1592388Cytotoxicity against human SH-SY5Y cells assessed as cell metabolic activity at 10 uM incubated for 24 hrs by MTT assay relative to control
AID1503623Antioxidant activity assessed as DPPH radical scavenging activity incubated for 60 mins under dark condition by spectrophotometry2017European journal of medicinal chemistry, Dec-01, Volume: 141Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
AID497110Antioxidant activity assessed as ABTS free radical scavenging activity at 100 uM after 12 hrs2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
AID668901Cytotoxicity against mouse RAW264.7 cells at 50 uM by MTT assay2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages.
AID1325286Antioxidant activity assessed as ferric ion reducing activity by measuring Fe2+ levels using fe3+-TPTZ at 375 ug/ml after 30 mins by FRAP assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID469411Neuroprotective activity against rotenone/oligomycin A-treated human SH-SY5Y cells assessed as cytoprotection at 1 uM pretreated 24 hrs before rotenone/oligomycin A challenge2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1428597Antioxidant activity assessed as ABTS radical scavenging activity incubated for 10 mins under dark condition2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID289269Reduction of hydroxyl radical activity at 0.1 mM in presence of 33 nM DMSO2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents.
AID639371Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as LDH release at 30 uM incubated for 24 hrs before H2O2 challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1581651Antioxidant activity assessed as ABTS radical scavenging activity at 75 uM measured after 5 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1624743Antioxidant activity assessed as inhibition of linoleic acid peroxidation activity at 10 uL2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
New Quinolylnitrones for Stroke Therapy: Antioxidant and Neuroprotective ( Z)- N- tert-Butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine Oxide as a New Lead-Compound for Ischemic Stroke Treatment.
AID613906Antioxidant activity in human SH-SY5Y cells assessed as decrease of tert-butyl hydroperoxide-induced ROS production at 20 uM after 24 hrs using DCFH-DA by fluorescence assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer's disease.
AID303036Antioxidant activity assessed as hydroxyl radical scavenging activity at 0.1 mM2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues.
AID731499Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2013Journal of natural products, Jan-25, Volume: 76, Issue:1
Neolignanamides, lignanamides, and other phenolic compounds from the root bark of Lycium chinense.
AID1581665Antioxidant activity assessed as increase in total ferric ion reducing activity at 30 uM using FeCl3.H2O and TPTZ incubated for 60 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1306593Antioxidant activity in HMEC1 assessed as inhibition of cell induced LDL oxidation by measuring TBARS level at 10 uM relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID445118Antioxidant activity assessed as DPPH free radical scavenging activity within 1 mins2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and antioxidant properties of dendritic polyphenols.
AID1678097Antioxidant activity assessed as superoxide anion radical scavenging activity incubated for 40 mins by spectrophotometric method2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID334586Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by spectrophotometry2002Journal of natural products, May, Volume: 65, Issue:5
2,3,4-Trimethyl-5,7-dihydroxy-2,3-dihydrobenzofuran, a novel antioxidant, from Penicillium citrinum F5.
AID1729063Antioxidant activity assessed as ferric ion reducing activity by measuring absorbance at 10 uM measured after 40 mins by FRAP assay (Rvb = 0.11 +/- 0.02 No_unit)2021European journal of medicinal chemistry, Mar-05, Volume: 213A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities.
AID247576In vitro inhibitory concentration against lipid peroxidation (LPO)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Nitrone derivatives of trolox as neuroprotective agents.
AID639372Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 0.1 uM treated 24 hrs before rotenone/oligomycin A challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1242920Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 240 mins by spectrophotometric analysis relative to control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.
AID1810884Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins by spectrophotometric analysis
AID220030Antioxidant activity in bovine heart mitochondria using iron(II) / dihydroxy fumaric acid (DHF)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Long-chain-substituted uric acid and 5,6-diaminouracil derivatives as novel agents against free radical processes: synthesis and in vitro activity.
AID1424235Antioxidant activity assessed as alkoxyl radical scavenging activity by measuring rate constant by ESR spin trapping method2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID1348942Antioxidant activity assessed as DPPH radical scavenging activity after 20 mins by spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1143749Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 3 uM preincubated for 24 hrs before rotenone-oligomycin addition measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID548351Neuroprotective activity against rotenone and oligomycin-induced mitochondrial oxidative stress in human SH-SY5Y cells assessed as LDH release at 3 uM after 24 hrs using DCFH-DA fluorescent dye2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1242922Antioxidant activity in rat brain assessed as inhibition of MDA production at 10 uM by TBARS assay relative to control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.
AID1083333Antiviral activity against Human coxsackievirus B4 infected human HeLa cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1515594Antioxidant activity in rat hepatic microsomes assessed as reduction in ferrous salt/ascorbic acid-induced lipid peroxidation of membrane lipids by measuring TBARS level after 45 mins by spectrophotometric method2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Optimizing the Pharmacological Profile of New Bifunctional Antihyperlipidemic/Antioxidant Morpholine Derivatives.
AID1892584Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM incubated for 30 mins by DPPH assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID399080Antioxidant activity assessed as DPPH scavenging activity2005Journal of natural products, Nov, Volume: 68, Issue:11
Free-radical-scavenging and xanthine oxidase inhibitory constituents from Stereospermum personatum.
AID683740Antioxidant activity assessed as Fe3+/ascorbic acid-induced hydroxyl radical scavenging activity at 0.1 mM after 30 mins2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Α-aryl-N-alkyl nitrones, as potential agents for stroke treatment: synthesis, theoretical calculations, antioxidant, anti-inflammatory, neuroprotective, and brain-blood barrier permeability properties.
AID1392707Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation after 48 hrs by thioflavin T-based fluorometric assay
AID635124Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2011Bioorganic & medicinal chemistry letters, Dec-15, Volume: 21, Issue:24
Inhibitory activity of novel kojic acid derivative containing trolox moiety on melanogenesis.
AID382324Antioxidant activity assessed as inhibition of AAPH-induced peroxidation of DOPC liposome after 80 mins by thiocyanate method2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Carboxymethylated pyridoindole antioxidants as aldose reductase inhibitors: Synthesis, activity, partitioning, and molecular modeling.
AID1703579Antioxidant activity assessed as radical scavenging activity measured after 30 mins by microplate reader based DPPH assay2020European journal of medicinal chemistry, Oct-01, Volume: 203Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile.
AID736838Antioxidant activity in mouse HT22 cells assessed as prevention of glutamate-induced GSH depletion at 25 uM2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship study of vitamin k derivatives yields highly potent neuroprotective agents.
AID1581667Antioxidant activity assessed as increase in total ferric ion reducing activity at 150 uM using FeCl3.H2O and TPTZ incubated for 60 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1603219Antioxidant activity assessed as DPPH radical scavenging activity at 5 uM relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID1372031Antioxidant activity assessed as rate constant for singlet oxygen scavenging activity in ethanol-water (1:1 v/v) mixture using phosphorescence-based single-photon-counting method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID639370Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as LDH release at 10 uM incubated for 24 hrs before H2O2 challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1326566Antioxidant activity in Salmonella typhimurium TA102 harboring hysG428 mutant assessed as inhibition of t-BuO2H-dependant mutant formation at 0.3 uM preincubated with compound followed by t-BuO2H addition after 48 hrs by Ames test2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1330215Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by spectrophotometric analysis2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Synthesis and biological assessment of novel N-(hydroxy/methoxy)alkyl β-enaminone curcuminoids.
AID310683Antioxidant activity assessed as DPPH free radical scavenging activity2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antioxidant properties of substituted 3-benzylidene-7-alkoxychroman-4-ones.
AID1249973Antioxidant activity assessed as DPPH radical scavenging activity at 0.3 to 10 uM incubated for 30 mins at 37 degC2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.
AID402581Inhibition of H2O2-stimulated ROS production in human skin fibroblast assessed as DCF-fluorescence at 100 uM after 4 hrs by DCFH-DA assay relative to control2004Journal of natural products, Jun, Volume: 67, Issue:6
Hyperjovinols A and B: Two new phloroglucinol derivatives from Hypericum jovis with antioxidant activity in cell cultures.
AID450087Antioxidant activity assessed as DMPD radical scavenging activity2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Antioxidant activity of 5,10-dihydroindeno[1,2-b]indoles containing substituents on dihydroindeno part.
AID1293542Neuroprotective activity against H2O2-induced neuronal cell death in human SH-SY5Y cells assessed as cell viability at 100 uM pretreated for 12 hrs followed by H2O2 addition measured after 3 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Neuroprotective oleanane triterpenes from the roots of Bupleurum chinense.
AID469405Neuroprotective activity against human SH-SY5Y cells assessed as protection reduction in H2O2-induced LDH release at 3 uM after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID538078Antioxidant activity assessed as DPPH radical scavenging activity2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
abeo-abietanes from Teucrium polium roots as protective factors against oxidative stress.
AID1480863Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 25 uM pretreated for 30 mins followed by glutamate challenge measured after 6 hrs by DCFH-DA probe based 2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1348940Antioxidant activity assessed as DPPH radical scavenging activity at 30 uM after 20 mins by spectrophotometric method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID1294642Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by microplate reader method2016European journal of medicinal chemistry, May-23, Volume: 114Novel benzylidenephenylpyrrolizinones with pleiotropic activities potentially useful in Alzheimer's disease treatment.
AID1493749Antioxidant activity assessed as total antioxidant capacity after 90 mins by phosphomolybdenum method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID1480874Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as increase in glutathione level at 25 to 100 uM pretreated for 30 mins followed by glutamate challenge measured after 10 hrs2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID310685Antioxidant activity at 100 ug by ferric reducing antioxidant power assay2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antioxidant properties of substituted 3-benzylidene-7-alkoxychroman-4-ones.
AID1324201Antioxidant activity assessed as superoxide radical scavenging activity measured every 30 secs for 6 mins in presence of superoxide generator pyrogallol2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID218997Oxidation was assessed indirectly by measuring bovine serum albumin(BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 500 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID1581652Antioxidant activity assessed as ABTS radical scavenging activity at 150 uM measured after 5 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID668899Inhibition of nitrite level in LPS-induced mouse RAW264.7 cells at 50 uM by Griess assay relative to LPS treated control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages.
AID1382552Antioxidant activity assessed as inhibition of DPPH radical generation after 30 mins2018European journal of medicinal chemistry, Mar-25, Volume: 148Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.
AID1651392Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as cell viability at 50 uM preincubated for 1 hr followed by H2O2 addition and measured after 4 hrs by CCK8 assay (Rvb = 61.14 +/- 1.05%)2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Isolation of triterpenoid saponins from Medicago sativa L. with neuroprotective activities.
AID1202555Antioxidant activity assessed as inhibition of ABTS free radical scavenging activity after 10 mins by spectrophotometry relative to control2015European journal of medicinal chemistry, , Volume: 96Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
AID1713229Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 6.3 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1348946Antiproliferative activity against NHDF at 30 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID537007Antioxidant activity in mouse ScGT1 cells assessed as inhibition of ROS formation at 1 uM after 3 hrs by TBARS assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Parallel synthesis, evaluation, and preliminary structure-activity relationship of 2,5-diamino-1,4-benzoquinones as a novel class of bivalent anti-prion compound.
AID1349623Antioxidant activity assessed as DPPH radical scavenging activity at 25 ug/ml after 1 hr
AID1610483Antioxidant activity assessed as decrease in ABTS radical cation scavenging activity every 1 min for 6 mins by UV-Vis spectrophotometric analysis2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.
AID227423In vitro percentage inhibition of glycation-induced fluorescence changes of BSA at 1 mM concentration2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
AID1300890Antioxidant activity of the compound after 90 mins by phosphomolybdenum assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.
AID1152631Antioxidant activity assessed as DPPH free radical scavenging activity after 60 mins by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Synthesis and radical scavenging activity of phenol-imidazole conjugates.
AID597264Antioxidant activity against AAPH-induced lipid peroxidation assessed as linoleic acid oxidation to diene hydroperoxide at 0.1 mM by UV-visible spectrophotometry2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Synthesis, in silico docking experiments of new 2-pyrrolidinone derivatives and study of their anti-inflammatory activity.
AID1713239Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 1.6 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID566095Antioxidant activity assessed as protection against APPH-induced linoleic acid lipid peroxidation 0.1 mM2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
One-pot microwave assisted synthesis under green chemistry conditions, antioxidant screening, and cytotoxicity assessments of benzimidazole Schiff bases and pyrimido[1,2-a]benzimidazol-3(4H)-ones.
AID248217In vitro inhibitory concentration against peroxynitrite (ONOO-): using pyrogallol red bleaching assay2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Nitrone derivatives of trolox as neuroprotective agents.
AID604217Antioxidant activity assessed as inhibition of ABTS free radicals after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID218994Oxidation was assessed indirectly by measuring bovine serum albumin thiol protection by using Ellman''s test at 500 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID1859608Antioxidant activity assessed as FRAP radical activity at 50 uM by FRAP assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1702531Neuroprotective activity against H2O2-induced cell injury in rat PC12 cells assessed as cell viability preincubated for 2 hrs followed by H2O2 addition and measured after 24 hrs by MTT assay (Rvb = 53.8 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID548350Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 100 uM after 24 hrs by UV-vis spectroscopy2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID676991Antioxidant activity assessed as inhibition of linoleic acid peroxidation at 100 uM by AAPH assay by UV spectrometry2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis of sulfur containing dihydro-pyrrolo derivatives and their biological evaluation as antioxidants.
AID668898Inhibition of nitrite level in LPS-induced mouse RAW264.7 cells at 5 uM by Griess assay relative to LPS treated control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages.
AID1326575Cytotoxicity against mouse LMTK cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1326579Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID451368Antioxidant activity assessed as inhibition of H2O2-induced bovine serum albumin oxidation after 10 mins by spectrophotometry2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Antioxidant efficacy of iridoid and phenylethanoid glycosides from the medicinal plant Teucrium chamaedris in cell-free systems.
AID1256884Hepatotoxicity in human HepG2 cells assessed as cell viability at 512 uM after 24 hrs by MTT assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1320875Inhibition of human recombinant MAOB using p-tyramine as substrate incubated for 15 mins by fluorimetric method2016European journal of medicinal chemistry, Oct-04, Volume: 121New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
AID639460Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 3 mM after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1743177Antioxidant activity assessed as ABTS radical scavenging activity measured after 1 hr by UV-vis spectrophotometric method2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID1610482Inhibition of equine serum BuChE at 20 uM using butyrylcholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method relative to control2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.
AID1713225Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 100 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1465116Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.
AID380429Cytotoxicity against human BT549 cells upto 48 uM2006Journal of natural products, Mar, Volume: 69, Issue:3
Schisandrene, a dibenzocyclooctadiene lignan from Schisandra chinensis: structure-antioxidant activity relationships of dibenzocyclooctadiene lignans.
AID264482Inhibition of hydrogen peroxide-induced death of mixed cortical cells of E15 Sprague-Dawley rat embryo at 10 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID42807Inhibition of [Fe(2+)]/ascorbate-induced oxidation of bovine heart membranes(antioxidant BHMLO)1999Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
Novel esters and amides of nonsteroidal antiinflammatory carboxylic acids as antioxidants and antiproliferative agents.
AID619932Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 12 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1525516Antioxidant activity in human M17 cell lysate assessed as trolox equivalents of ABTS radical scavenging activity incubated up to 10 mins2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID1713234Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 50 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID735814Antioxidant activity assessed as concentration required to 50 % ABTS radical scavenging activity absorbance at 734 nm2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Dorsamin-A's, glycerolipids carrying a dehydrophenylalanine ester moiety from the seed-eating larvae of the bruchid beetle Bruchidius dorsalis.
AID1418625Antioxidant activity assessed as ABTS radical scavenging activity incubated for 10 mins in dark2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Resveratrol-maltol hybrids as multi-target-directed agents for Alzheimer's disease.
AID774816Antioxidant activity assessed as ABTS radical scavenging activity after 6 mins2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antioxidant activity of novel Mannich base of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan.
AID1589465Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 30 mins under dark condition by spectrophotometry2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID234581Inhibition time for 20 uM during peroxidation of methyl linoleate / DMVN in TBA /methanol medium at 40 degree Centigrade1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Long-chain-substituted uric acid and 5,6-diaminouracil derivatives as novel agents against free radical processes: synthesis and in vitro activity.
AID1465115Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment.
AID264486Viability of rotifers against doxorubicin toxicity at 10 uM2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID1293536Neuroprotective activity against H2O2-induced neuronal cell death in human SH-SY5Y cells assessed as cell viability at 25 uM pretreated for 12 hrs followed by H2O2 addition measured after 3 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Neuroprotective oleanane triterpenes from the roots of Bupleurum chinense.
AID402580Inhibition of H2O2-stimulated ROS production in human skin fibroblast assessed as DCF-fluorescence at 10 uM after 4 hrs by DCFH-DA assay relative to control2004Journal of natural products, Jun, Volume: 67, Issue:6
Hyperjovinols A and B: Two new phloroglucinol derivatives from Hypericum jovis with antioxidant activity in cell cultures.
AID633132Antioxidant activity in Wistar rat erythrocytes assessed as prolongation of initial inhibition period-lag phase of AAPH-induced hemolysis at 100 uM preincubated for 30 mins before induction measured up to 5 hrs by spectrophotometry2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
(2-Benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl)-acetic acid: an aldose reductase inhibitor and antioxidant of zwitterionic nature.
AID426427In vivo antiinflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip administered simultaneously with carrageenan measured after 3.5 hrs2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.
AID180509Tested in vitro for the inhibition of iron-dependent lipid peroxidation against rat brain homogenates, by malondialdehyde (MDA) formation assay1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia.
AID1256879Inhibition of human plasmatic BChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1743181Antioxidant activity in human erythrocytes assessed as protection against AAPH-induced hemolysis at 400 uM preincubated for 20 mins followed by AAPH addition and measured after 2 hrs by spectrophotometric method relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID619940Antioxidant activity assessed as ferric to ferrous reduction at 10 ug/ml by FRAP assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1357813Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as cell viability at 12.5 uM pre-incubated for 1 hr followed by H2O2 addition and measured after 4 hrs by MTT assay relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID551408Antioxidant activity assessed as trolox equivalents of peroxyl radical scavenging activity by ORAC assay2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Synthesis, structure, theoretical and experimental in vitro antioxidant/pharmacological properties of α-aryl, N-alkyl nitrones, as potential agents for the treatment of cerebral ischemia.
AID1633206Antioxidant activity assessed as AAPH radical scavenging activity preincubated for 15 mins with fluorescein before AAPH addition and recorded every 2 mins for 160 mins by ORAC-FL assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID1659477Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM relative to control2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID1592383Antioxidant activity assessed as DPPH radical scavenging activity measured after 45 mins by UV-Visible spectrophotometric based assay
AID736282Antioxidant activity assessed as reduction of Cu2+ to Cu+ measured as copper (I) level at 1 uM measured for 1 hr2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Scopoletin and scopolin isolated from Artemisia iwayomogi suppress differentiation of osteoclastic macrophage RAW 264.7 cells by scavenging reactive oxygen species.
AID1234558Antioxidant activity in rat liver microsomes assessed as reduction in iron-ascorbic acid-induced lipid peroxidase activity after 30 mins by TBARS assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis of (2-amino)ethyl derivatives of quercetin 3-O-methyl ether and their antioxidant and neuroprotective effects.
AID184561Inhibition of [Fe(2+)]/ascorbate-induced lipid peroxidation at 10e-5 M in rat brain homogenate1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
Benzoselenazolinone derivatives designed to be glutathione peroxidase mimetics feature inhibition of cyclooxygenase/5-lipoxygenase pathways and anti-inflammatory activity.
AID1678098Antioxidant activity in rat brain homogenate assessed as inhibition of FeCl3/ascorbic acid-induced lipid peroxidation by measuring MDA level at 100 uM after 30 mins by thiobarbituric acid based spectrophotometric method relative to control2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID1851307Antioxidant activity assessed as DPPH radical scavenging activity by DPPH assay2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Biocatalytic synthesis and evaluation of antioxidant and antibacterial activities of hydroxyequols.
AID1326583Cytotoxicity against hamster AG17-1 cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1782120Antioxidant activity assessed as DPPH radical scavenging activity measured for 60 mins by spectrophotometric analysis2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Investigation on the solid-phase synthesis of silybin prodrugs and their timed-release.
AID230361Reducing activity to scavenge 10 uM 1, 1-diphenylpicrylhydrazyl (DPPH)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Long-chain-substituted uric acid and 5,6-diaminouracil derivatives as novel agents against free radical processes: synthesis and in vitro activity.
AID1267383Antioxidant activity assessed as ABTS radical scavenging activity after 30 mins2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents.
AID1356533Antioxidant activity assessed as DPPH radical scavenging activity incubated for 10 mins under dark condition2018Journal of natural products, 08-24, Volume: 81, Issue:8
A Bioactive Resveratrol Trimer from the Stem Bark of the Sri Lankan Endemic Plant Vateria copallifera.
AID1143539Antioxidant activity assessed as ABTS radical scavenging activity after 16 hrs by spectrophotometric analysis2014European journal of medicinal chemistry, Jun-23, Volume: 81Thiaflavan scavenges radicals and inhibits DNA oxidation: a story from the ferrocene modification.
AID1071850Antioxidant activity assessed as riboflavin/EDTA-induced superoxide anion radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1322939Antioxidant activity of the compound assessed as DPPH radical scavenging activity at 50 uM after 60 mins by spectrophotometric method2016European journal of medicinal chemistry, Oct-04, Volume: 121Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.
AID745286Antioxidant activity against AAPH-induced lipid peroxidation at 100 uM by UV spectrophotometry2013European journal of medicinal chemistry, May, Volume: 63Analysis of the antioxidant properties of differently substituted 2- and 3-indolyl carbohydrazides and related derivatives.
AID497111Antioxidant activity assessed as DPPH free radical scavenging activity after 1 hr2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
AID228563Krel expressed as Ki with respect to Ktrolox2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Imidazolopyrazinones as potential antioxidants.
AID257307Hydroxyl radical scavenging activity of Cudriana tricuspidata extracts2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Antioxidant and cytotoxic activities of xanthones from Cudrania tricuspidata.
AID196392Compound was evaluated for its inhibitory concentration against X/XO- induced oxidative neuronal damage in primary cultured rat cortical cells2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Synthesis and evaluation of 4-hydroxyphenylacetic acid amides and 4-hydroxycinnamamides as antioxidants.
AID257904Activity against hydrogen peroxide induced DNA damage in Jurkat T cells2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Chroman/catechol hybrids: synthesis and evaluation of their activity against oxidative stress induced cellular damage.
AID459655Cytotoxicity against human Caco-2 cells assessed as plasma membrane damage at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1194494Antioxidant activity assessed as ferric-reducing antioxidant power after 20 mins at 50 degC by UV spectrophotometry2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities.
AID469406Neuroprotective activity against human SH-SY5Y cells assessed as protection reduction in H2O2-induced LDH release at 10 uM after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID619933Antioxidant activity assessed as inhibition of linoleic acid lipid peroxidation at 100 ug/ml measured after 18 hrs by ferric thiocynate method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1581661Antioxidant activity assessed as increase in total ferric ion reducing activity at 150 uM using FeCl3.H2O and TPTZ incubated for 5 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID609920Antioxidant activity against AAPH-induced linoleic acid peroxidation at 100 uM by UV spectrophotometry analysis2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities.
AID427136Antioxidant activity assessed as ABTS radical scavenging activity after 6 mins by cation decolorization assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
p-Terphenyls from the fruiting bodies of Paxillus curtisii and their antioxidant properties.
AID471738Antioxidant activity assessed as inhibition of lipid peroxidation at 100 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of modified homo-N-nucleosides from the reactions of mesityl nitrile oxide with 9-allylpurines and their influence on lipid peroxidation and thrombin inhibition.
AID1730600Antioxidant activity assessed as ABTS radical scavenging activity incubated for 2 to 6 mins under dark condition2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID639457Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 0.1 uM after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID604210Antioxidant activity assessed as inhibition of DPPH free radicals at 0.01 mM after 30 mins by UV-visible spectrophotometer analysis relative to control2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents.
AID1324202Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins in dark2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Synthesis and anti-inflammatory activity of paeonol analogues in the murine model of complete Freund's adjuvant induced arthritis.
AID235284Free radical scavenging assessed as ABTS (2,2'-azinobis-(3-ethyl benz) thiazoline-6-sulfonic acid) color change2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Novel 3-O-acyl mesquitol analogues as free-radical scavengers and enzyme inhibitors: synthesis, biological evaluation and structure-activity relationship.
AID1428598Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM incubated for 24 hrs under dark condition by thioflavin-T based fluorometric assay relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID490419Cytoprotective activity against UV-induced LDL oxidation in HMEC1 cells at 10 uM after 6 hrs by MTT assay2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antioxidant activity evaluation of a syringic hydrazones family.
AID1293535Neuroprotective activity against H2O2-induced neuronal cell death in human SH-SY5Y cells assessed as cell viability at 50 uM pretreated for 12 hrs followed by H2O2 addition measured after 3 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
Neuroprotective oleanane triterpenes from the roots of Bupleurum chinense.
AID1743178Antioxidant activity assessed as AAPH scavenging activity by measuring residual fluorescence at 10 uM measured at 1 min interval for 30 mins by ORAC fluorescein assay relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID536050Antioxidant activity assessed as protection against UV/H2O2-induced thymidine degradation in 12.5 mM phosphate buffer at 100 uM by competitive immuno-enzymatic assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Synthesis and antioxidant properties of pulvinic acids analogues.
AID469409Neuroprotective activity against rotenone/oligomycin A-treated human SH-SY5Y cells assessed as cytoprotection at 0.1 uM pretreated 24 hrs before rotenone/oligomycin A challenge2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID442293Inhibition of peroxynitrite-induced 3-nitrotyrosin formation by HPLC2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis, anti-HCV, antioxidant, and peroxynitrite inhibitory activity of fused benzosuberone derivatives.
AID774814Antioxidant activity in KM mouse liver microsomes assessed as inhibition of lipid peroxidation after 60 mins2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antioxidant activity of novel Mannich base of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan.
AID1474957Antioxidant activity assessed as ABTS radical scavenging activity at 2 mg/ml incubated for 2 hrs in dark by spectrophotometric analysis (Rvb = 1 to 9%)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID490946Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 60 mins2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID1163382Antioxidant activity assessed as inhibition of lipid peroxidation at 100 uM by spectrophotometry2014European journal of medicinal chemistry, Oct-30, Volume: 86Novel semicarbazides and ureas of primaquine with bulky aryl or hydroxyalkyl substituents: synthesis, cytostatic and antioxidative activity.
AID1424233Antioxidant activity assessed as hydroxyl radical scavenging activity by measuring rate constant using UV irradiation by ESR spin trapping method2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID295041Inhibition of Xanthine oxidase2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID567049Antioxidant activity assessed as inhibition of heme protein-dependent lipid peroxidation at 1 mM2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.
AID469407Neuroprotective activity against human SH-SY5Y cells assessed as protection reduction in H2O2-induced LDH release at 30 uM after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID648156Antioxidant activity assessed as DPPH free radical scavenging activity by UV-Vis spectrophotometry2012European journal of medicinal chemistry, Apr, Volume: 50Novel molecular combination deriving from natural aminoacids and polyphenols: Design, synthesis and free-radical scavenging activities.
AID1406254Inhibition of human AChE using acetylthiocholine iodide as substrate assessed as residual activity at 10 uM preincubated for 5 mins followed by substrate addition and measured for 1 min by Ellman's assay relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID264480Hydroxyl radical scavenging activity by ABTS competition assay per 30 mins at 1 umol/mL2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID1418624Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM after 24 hrs by thioflavin-T fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Resveratrol-maltol hybrids as multi-target-directed agents for Alzheimer's disease.
AID1474955Antioxidant activity assessed as ABTS radical scavenging activity at 0.5 mg/ml incubated for 2 hrs in dark by spectrophotometric analysis (Rvb = 1 to 9 %)2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Stereoselective synthesis of enantiopure N-substituted pyrrolidin-2,5-dione derivatives by 1,3-dipolar cycloaddition and assessment of their in vitro antioxidant and antibacterial activities.
AID1729052Antioxidant activity in Swiss mouse brain cerebral tissue assessed as inhibition of SNP-induced lipid peroxidation by measuring TBARS level at 10 uM incubated for 1 hr relative to control2021European journal of medicinal chemistry, Mar-05, Volume: 213A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities.
AID1493966Antiproliferative activity against human A549 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID1810883Antioxidant activity of compound assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every 2 mins for 90 mins by ORAC fluorescein assay
AID1589463Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM incubated for 30 mins under dark condition by spectrophotometry2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID1326570Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1436063Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as increase in cell viability at 100 uM pretreated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID1480865Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 100 uM pretreated for 30 mins followed by glutamate challenge measured after 6 hrs by DCFH-DA probe based2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID453103Antioxidant activity assessed as inhibition of peroxynitrite-mediated 3-nitrotyrosine formation by HPLC2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Synthesis, tautomerism, and antimicrobial, anti-HCV, anti-SSPE, antioxidant, and antitumor activities of arylazobenzosuberones.
AID1331319Antioxidant activity assessed as ABTS free radical scavenging activity at 10 uM2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID377070Antioxidant activity assessed as DPPH radical scavenging activity studied at DPPH to compound ratio of 52005Journal of natural products, Feb, Volume: 68, Issue:2
Identification of radical scavenging compounds in Rhaponticum carthamoides by means of LC-DAD-SPE-NMR.
AID1511012Antioxidant activity assessed as H2O2 radical scavenging activity2019European journal of medicinal chemistry, Oct-15, Volume: 180Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
AID1515596Inhibition of SQS in rat liver microsomes assessed as reduction in [3H]FPP conversion to squalene preincubated for 10 mins followed by [3H]FPP addition and measured after 10 mins by scintillation counting method2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Optimizing the Pharmacological Profile of New Bifunctional Antihyperlipidemic/Antioxidant Morpholine Derivatives.
AID668900Cytotoxicity against mouse RAW264.7 cells at 5 uM by MTT assay2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages.
AID436306Antioxidant activity assessed as AAPH radical scavenging activity2008Journal of natural products, Nov, Volume: 71, Issue:11
Monodictyochromes A and B, dimeric xanthone derivatives from the marine algicolous fungus Monodictys putredinis.
AID1083331Antiviral activity against Feline coronavirus infected feline kidney crandell cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID257306Superoxide radical scavenging activity of Cudriana tricuspidata extracts2005Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
Antioxidant and cytotoxic activities of xanthones from Cudrania tricuspidata.
AID1318720Antioxidant activity assessed as DPPH free radical scavenging activity at 10 uM after 30 mins by UV-spectrophotometric method relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121A series of pyrido[2,3-b]pyrazin-3(4H)-one derivatives as aldose reductase inhibitors with antioxidant activity.
AID379313Antioxidant scavenging activity against 2,2'-azobis-amidinopropane-induced peroxyl radicals assessed as total oxyradical scavenging capacity2000Journal of natural products, Mar, Volume: 63, Issue:3
Evaluation of the total peroxyl radical-scavenging capacity of flavonoids: structure-activity relationships.
AID1436862Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 240 mins by UV spectrophotometer relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis and structure-activity relationship studies of phenolic hydroxyl derivatives based on quinoxalinone as aldose reductase inhibitors with antioxidant activity.
AID1300893Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins under dark conditions2016European journal of medicinal chemistry, Jul-19, Volume: 117Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.
AID490947Inhibition of soybean LOX at 100 uM2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID196890Effect on in vitro myocardial electrical activity (arrhythmia score) at 5 uM2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Novel potent inhibitors of lipid peroxidation with protective effects against reperfusion arrhythmias.
AID1581660Antioxidant activity assessed as increase in total ferric ion reducing activity at 75 uM using FeCl3.H2O and TPTZ incubated for 5 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID333771Induction of HIF1beta protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis2004Journal of natural products, Dec, Volume: 67, Issue:12
Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
AID1083329Antiviral activity against Unidentified Influenza A virus (H1N2) infected MDCK cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID286755Antioxidant activity assessed as DPPH reducing activity at 0.5 mM after 20 mins2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.
AID196224Relative efficacy gives an indication of the percent of viable cells (Rat cerebellar granule cells) at the maximal efficacious concentration of 77.8 uM2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
AID1755234Antagonist activity at human H3 receptor by TR-FRET assay
AID1277565Antioxidant activity assessed as suppression of H2O2/cobalt2+-mediated hydroxyl radical formation by luminol-based fluorescence assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Synthesis and biological evaluation of novel orally available 1-phenyl-6-aminouracils containing dimethyldihydrobenzofuranol structure for the treatment of allergic skin diseases.
AID1071845Antioxidant activity assessed as H2O2-induced hydroxyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1327544Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent at 10 uM preincubated for 30 mins followed by AAPH addition measured evey 60 secs for 60 cycles by ORAC-FL assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease.
AID1434538Antioxidant activity assessed as inhibition of ferrous chloride-induced lipid peroxidation at 50 uM preincubated for 24 hrs followed by ferrous chloride addition relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl)methanone derivatives.
AID736290Ratio of trolox EC50 to compound EC50 for ABTS free radical scavenging activity2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Antioxidant and anti-inflammatory meroterpenoids from the brown alga Cystoseira usneoides.
AID1318719Antioxidant activity assessed as DPPH free radical scavenging activity at 50 uM after 30 mins by UV-spectrophotometric method relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121A series of pyrido[2,3-b]pyrazin-3(4H)-one derivatives as aldose reductase inhibitors with antioxidant activity.
AID1071848Antioxidant activity assessed as t-butylhyroperoxide-induced alkylperoxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1728603Antioxidant activity assessed as H2O2 radical scavenging activity in pH 7.4 buffer at 1 to 30 uM measured after 24 hrs by quantichrom-peroxide assay kit based method2021European journal of medicinal chemistry, Feb-15, Volume: 212ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker.
AID1325288Antioxidant activity assessed as ferric ion reducing activity by measuring Fe2+ levels using fe3+-TPTZ at 1500 ug/ml after 30 mins by FRAP assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID1238057Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins under dark conditions2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Nitric oxide inhibitory activity and antioxidant evaluations of 2-benzoyl-6-benzylidenecyclohexanone analogs, a novel series of curcuminoid and diarylpentanoid derivatives.
AID1372029Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced super-oxide anion scavenging activity by measuring Kaox/Kst ratio using CYPMPO spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1083330Antiviral activity against Unidentified Influenza A virus (H1N2) infected MDCK cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID289270Reduction of hydroxyl radical activity at 1 mM in presence of 33 nM DMSO2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents.
AID1071841Antioxidant activity assessed as DMSO/H2O2-induced methyl radical scavenging activity by ESR spin trapping method2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1257005Antioxidant activity assessed as DPPH scavenging activity at 10 to 60 ug/ml after 30 mins2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease.
AID1071746Antioxidant activity against AAPH-induced lipid peroxidation assessed as inhibition of conjugated diene hydroperoxide production at 100 uM2014European journal of medicinal chemistry, Mar-03, Volume: 74Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's
AID1651393Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as cell viability at 100 uM preincubated for 1 hr followed by H2O2 addition and measured after 4 hrs by CCK8 assay (Rvb = 61.14 +/- 1.05%)2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Isolation of triterpenoid saponins from Medicago sativa L. with neuroprotective activities.
AID1581662Antioxidant activity assessed as increase in total ferric ion reducing activity at 30 uM using FeCl3.H2O and TPTZ incubated for 30 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1392706Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM after 48 hrs by thioflavin T-based fluorometric assay relative to control
AID1581655Antioxidant activity assessed as ABTS radical scavenging activity at 150 uM measured after 30 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID639459Neuroprotective activity against rotenone/oligomycin A-induced cell death in human SH-SY5Y cells assessed as LDH release at 1 uM after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1264039Antioxidant activity in human SH-SY5Y cells assessed as reduction of xanthine oxidase-mediated superoxide generation preincubated for 1 hr followed by xanthine oxidase challenge for 1 hr by MitoSOX staining-based fluorescence analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1493750Antioxidant activity assessed as ferric ion reducing activity using using Fe3+-TPTZ after 30 mins by FRAP assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID1357815Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as cell viability at 50 uM pre-incubated for 1 hr followed by H2O2 addition and measured after 4 hrs by MTT assay relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.
AID1534715Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalents after 150 mins2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of isoprenylation-resveratrol dimer derivatives against Alzheimer's disease.
AID1702443Neuroprotective activity against H2O2-induced cell injury in rat PC-12 cells assessed as increase in cell viability causing decrease in LDH content preincubated for 2 hrs followed by H2O2 addition and measured after 24 hrs by LDH assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID295042Inhibition of COX12007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID286757Antioxidant activity assessed as DMSO hydroxyl radical scavenging activity at 0.1 mM2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.
AID378807Antioxidant activity assessed as inhibition of hydroxyl radical generation by fluorescence spectroscopy2006Journal of natural products, Oct, Volume: 69, Issue:10
Antioxidative phenolics from the fresh leaves of Ternstroemia japonica.
AID1075986Neuroprotective activity against Abeta1-42 peptide-induced neurotoxicity in rat C6 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID619943Antioxidant activity assessed as ferric to ferrous reduction activity at 40 ug/ml by FRAP assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID452852Antioxidant activity assessed as hydroxyl radical scavenging activity at 100 uM2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID1594788Neuroprotective activity in human SH-SY5Y cells assessed as reduction in H2O2-induced cell damage by measuring cell viability level at 50 uM by MTT assay (Rvb = 67.95%)2019Journal of natural products, 06-28, Volume: 82, Issue:6
Guaiane-Type Sesquiterpenoids from the Roots of Daphne genkwa and Evaluation of Their Neuroprotective Effects.
AID1713233Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 100 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1167300Antioxidant activity assessed as DPPH radical scavenging activity incubated at room temperature for 20 mins by UV-visible spectrophotometry2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Design, synthesis and exploring the quantitative structure-activity relationship of some antioxidant flavonoid analogues.
AID1264036Neuroprotective activity against Fenton reagent-induced ROS generation-stimulated cytotoxicity in human SH-SY5Y cells assessed as cell viability at 1 mM after 2 hrs by MTS assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID277125Cytotoxicity against microglial cells at 10 uM2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent.
AID1575654Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins under dark condition by spectrophotometric analysis2019MedChemComm, May-01, Volume: 10, Issue:5
Synthesis of novel vanillin derivatives: novel multi-targeted scaffold ligands against Alzheimer's disease.
AID1315210Antioxidant activity of the compound assessed as inhibition of fenton reaction-induced DNA strand cleavage of plasmid pcDNA Hismyc B4 after 1 hr by ethidium bromide staining-based agarose gel electrophoresis2016European journal of medicinal chemistry, Oct-04, Volume: 121Multi-target screening mines hesperidin as a multi-potent inhibitor: Implication in Alzheimer's disease therapeutics.
AID639365Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as LDH release at 1 uM incubated for 24 hrs before H2O2 challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1428599Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation incubated for 24 hrs under dark condition by thioflavin-T based fluorometric assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and biological evaluation of deferiprone-resveratrol hybrids as antioxidants, Aβ
AID458693Cytotoxicity against HEK293 cells assessed as cell death at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1592382Cytotoxicity against human HepG2 cells assessed as cell metabolic activity at 10 uM incubated for 48 hrs by resazurin assay relative to control
AID1892588Antioxidant activity in rat brain homogenate assessed as inhibition of lipid peroxidation by measuring MDA concentration at 5 uM by TBARS assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID625358Antioxidant activity assessed as DPPH free radical scavenging activity at 100 uM2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of (2,5-dihydro-1H-pyrrol-1-yl)-2H-chromen-2-ones as free radical scavengers.
AID1493752Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID619939Antioxidant activity assessed as superoxide radical scavenging activity after 40 mins by Zhishen's method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1729059Antioxidant activity in Swiss mouse brain cerebral tissue assessed as inhibition of sodium azide-induced reactive species production by measuring fluorescence unit at 10 uM by DCHF-DA dye based spectrofluorimetric method (Rvb = 139 +/- 26.8 U)2021European journal of medicinal chemistry, Mar-05, Volume: 213A greener protocol for the synthesis of phosphorochalcogenoates: Antioxidant and free radical scavenging activities.
AID1300891Antioxidant activity of the compound after 30 mins by FRAP assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties.
AID1083342Antiviral activity against Punta Toro virus infected Hela cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1424253Antioxidant activity assessed as effect on linolenic acid autooxidation in presence of 0.015 M SDS based micellar systems2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID1480869Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 25 uM pretreated for 30 mins followed by glutamate challenge after 10 hrs by DCFH-DA probe based FACS ana2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1872744Antioxidant activity assessed as DPPH radical scavenging activity measured after 30 mins2022European journal of medicinal chemistry, Apr-05, Volume: 233Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
AID736486Antioxidant activity assessed as inhibition of ABTS radical formation for 15 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Exploring nature profits: development of novel and potent lipophilic antioxidants based on galloyl-cinnamic hybrids.
AID537161Antioxidant activity assessed as DPPH radical scavenging activity after 270 mins by least-square analysis2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID1306600Cytotoxicity against HMEC1 assessed as cell viability at 10 uM after 24 hrs by MTT assay in absence of oxidized LDL2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1418623Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation after 24 hrs by thioflavin-T fluorescence assay2018Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22
Resveratrol-maltol hybrids as multi-target-directed agents for Alzheimer's disease.
AID1331320Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID1480870Neuroprotective activity against glutamate-induced neuronal cell death in mouse HT22 cells assessed as intracellular reactive oxygen species level at 50 uM pretreated for 30 mins followed by glutamate challenge after 10 hrs by DCFH-DA probe based FACS ana2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID1293785Antioxidant activity assessed as ABTS free radical scavenging activity after 1 min by spectrophotometry2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling.
AID1242921Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 240 mins by spectrophotometric analysis relative to control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.
AID1326578Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability at 300 uM after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1083336Antiviral activity against Human parainfluenza virus 3 infected Vero cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID227421In vitro percentage inhibition of formation of DNPH-reactive carbonyl groups in BSA exposed to fructose at 1 mM concentration2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
AID469410Neuroprotective activity against rotenone/oligomycin A-treated human SH-SY5Y cells assessed as cytoprotection at 0.3 uM pretreated 24 hrs before rotenone/oligomycin A challenge2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1264025Neuroprotective activity against Fenton reagent-induced ROS generation in human ARPE19 cells assessed as increase in GSH level at 1 mM after 2 hrs by DTNB method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1424252Antioxidant activity assessed as effect on linolenic acid autooxidation in presence of 0.5 M SDS based micellar systems2017European journal of medicinal chemistry, Jun-16, Volume: 133Free radicals and polyphenols: The redox chemistry of neurodegenerative diseases.
AID1143748Neuroprotective activity in human SH-SY5Y cells assessed as protection against rotenone-oligomycin-induced toxicity at 1 uM preincubated for 24 hrs before rotenone-oligomycin addition measured after 24 hrs by lactate dehydrogenase release assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.
AID427666Antioxidant activity assessed as superoxide anion radical scavenging activity by spectrophotometry2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Potential antioxidants and tyrosinase inhibitors from synthetic polyphenolic deoxybenzoins.
AID1228330Antioxidant activity assessed as inhibition of AAPH-induced crocin oxidation at 5 to 500 uM in lipophilic medium containing linoleic acid by crocin bleaching assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Interaction of α-Hexylcinnamaldehyde with a Biomembrane Model: A Possible MDR Reversal Mechanism.
AID1083348Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 1 X 10'-5 M2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1846106Antioxidant activity assessed as trolox equivalent of ABTS radical cation scavenging activity measured for 15 mins by spectrophotometeric analysis2021European journal of medicinal chemistry, Apr-05, Volume: 215A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease.
AID1083332Antiviral activity against Respiratory syncytial virus infected human HeLa cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1581663Antioxidant activity assessed as increase in total ferric ion reducing activity at 75 uM using FeCl3.H2O and TPTZ incubated for 30 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID625354Antioxidant activity assessed as hydroxyl radical scavenging activity at 100 uM after 30 mins2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
Synthesis and biological evaluation of (2,5-dihydro-1H-pyrrol-1-yl)-2H-chromen-2-ones as free radical scavengers.
AID333770Induction of HIF1alpha protein in human T47D cells under normoxic condition at 100 uM after 4 hrs by Western blot analysis2004Journal of natural products, Dec, Volume: 67, Issue:12
Hypoxia-inducible factor-1 activation by (-)-epicatechin gallate: potential adverse effects of cancer chemoprevention with high-dose green tea extracts.
AID1306598Antiangiogenic activity in HMEC1 assessed as inhibition of oxidized LDL induced tube formation measured as residual tube at 10 uM after 18 hrs by calcein staining based fluorescence microscopy2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1377506Antioxidant activity assessed as ABTS radical scavenging activity after 30 mins2017European journal of medicinal chemistry, Sep-29, Volume: 138A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
AID344045Antioxidant activity assessed as ABTS radical scavenging activity after 12 hrs2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Cyathuscavins A, B, and C, new free radical scavengers with DNA protection activity from the Basidiomycete Cyathus stercoreus.
AID320331Antioxidant activity in human MCF7 cells by FRAP test2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and protective effects of coumarin derivatives against oxidative stress induced by doxorubicin.
AID537162Antioxidant activity assessed as ratio of IC50 for DPPH radical scavenging activity to concentration of DPPH2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID1581653Antioxidant activity assessed as ABTS radical scavenging activity at 30 uM measured after 30 mins by spectrophotometric assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID462445Antioxidant activity against AAPH-induced lipid peroxidation in unilamellar DOPC liposomes after 80 mins by thiocyanate reagent method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
AID1743180Antioxidant activity in human erythrocytes assessed as protection against AAPH-induced hemolysis at 50 uM preincubated for 20 mins followed by AAPH addition and measured after 2 hrs by spectrophotometric method relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID310684Antioxidant activity in Wistar rat brain assessed as inhibition of lipid peroxidation2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antioxidant properties of substituted 3-benzylidene-7-alkoxychroman-4-ones.
AID1435200Antioxidant activity assessed as ABTS radical scavenging activity after 1 min2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
New insights into highly potent tyrosinase inhibitors based on 3-heteroarylcoumarins: Anti-melanogenesis and antioxidant activities, and computational molecular modeling studies.
AID548352Neuroprotective activity against rotenone and oligomycin-induced mitochondrial oxidative stress in human SH-SY5Y cells assessed as LDH release at 10 uM after 24 hrs using DCFH-DA fluorescent dye2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID1248049Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation after 3 hrs by TBA-MDA test2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Synthesis, electronic properties, antioxidant and antibacterial activity of some new benzimidazoles.
AID1385652Neuroprotective activity against glutamate-induced cell death in mouse HT22 cells assessed as cell viability at 12.5 uM pretreated for 2 hrs followed by glutamate-challenge and measured after 20 hrs by MTT assay (Rvb = 23 +/- 3.57%)2018Journal of natural products, 08-24, Volume: 81, Issue:8
Targeted Isolation of Neuroprotective Dicoumaroyl Neolignans and Lignans from Sageretia theezans Using in Silico Molecular Network Annotation Propagation-Based Dereplication.
AID1743176Antioxidant activity assessed as trolox equivalent of ABTS radical scavenging activity measured after 1 hr by UV-vis spectrophotometric method2020European journal of medicinal chemistry, Dec-15, Volume: 208Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation.
AID447535Antioxidant activity assessed as DPPH free radical scavenging activity by UV spectroscopic method2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles.
AID1071851Antioxidant activity assessed as H2O2-induced hydroxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1406256Selectivity ratio of IC50 for human AChE to IC50 for human BChE2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID1436861Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 240 mins by UV spectrophotometer relative to control2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis and structure-activity relationship studies of phenolic hydroxyl derivatives based on quinoxalinone as aldose reductase inhibitors with antioxidant activity.
AID427134Protection against ferrous and hydrogen peroxide-induced single strand breakage of pBR322 DNA at 50 uM after 30 mins using ethium bromide staining2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
p-Terphenyls from the fruiting bodies of Paxillus curtisii and their antioxidant properties.
AID1564984Antioxidant activity in human SH-SY5Y cells assessed as inhibition of t-BuOOH-induced intracellular oxidative stress by measuring ROS level at 100 uM preincubated for 24 hrs followed by t-BuOOH addition and measured after 30 mins by DCFH-DA dye-based fluo2019European journal of medicinal chemistry, Nov-15, Volume: 182Novel multi target-directed ligands targeting 5-HT
AID1382555Protection against CoCl2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 36 hrs followed by CoCl2 addition measured after 12 hrs by MTT assay (Rvb = 51.2%)2018European journal of medicinal chemistry, Mar-25, Volume: 148Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.
AID1762405Inhibition of equine serum BuChE using butyrylcholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method2021European journal of medicinal chemistry, Jun-05, Volume: 218Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
AID548354Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as LDH release at 100 uM after 24 hrs by UV-vis spectroscopy in presence of calcium channel blocker nimodipine2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases.
AID598279Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties.
AID218993Oxidation was assessed indirectly by measuring bovine serum albumin thiol protection by using Ellman''s test at 1 mM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID1678473Antioxidant activity assessed as ferric ion reducing activity using FeCl3.H2O and TPTZ incubated for 30 mins by FRAP assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-
AID1194493Antioxidant activity assessed as ABTS radical scavenging activity incubated for 6 mins2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities.
AID1327543Reactive carbonyl species trapping activity of compound assessed as MDA adduct formation at 10 mM preincubated for 24 hrs with MDA measured after 1 hr by LCMS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease.
AID264481Radical reducing potency by ABTS cation radical reduction assay per 30 mins at 1 umol/mL2006Journal of medicinal chemistry, May-04, Volume: 49, Issue:9
Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.
AID1179728Antioxidant activity assessed as reduction in mouse CRL2181 cells-mediated human LDL oxidation by measuring TBARS level at 10 uM after 18 hrs2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID1678474Antioxidant activity assessed as DPPH free radical scavenging activity after 5 mins by microplate reader based assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-
AID1257020Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 100 uM2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Synthesis and biological evaluation of new C-10 substituted dithranol pleiotropic hybrids.
AID295043Inhibition of COX22007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID1238058Antioxidant activity incubated at 50 degC for 20 mins by FRAP assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Nitric oxide inhibitory activity and antioxidant evaluations of 2-benzoyl-6-benzylidenecyclohexanone analogs, a novel series of curcuminoid and diarylpentanoid derivatives.
AID1603216Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID1655202Antioxidant activity in pH 7.4 PBS assessed as H2O2 radical scavenging activity2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
AID619937Antioxidant activity assessed as residual DPPH radical scavenging activity after 30 mins by spectrophotometric analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Isoeugenol-based novel potent antioxidants: synthesis and reactivity.
AID1493967Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A green multicomponent synthesis of tocopherol analogues with antiproliferative activities.
AID469412Neuroprotective activity against rotenone/oligomycin A-treated human SH-SY5Y cells assessed as cytoprotection at 3 uM pretreated 24 hrs before rotenone/oligomycin A challenge2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID248216In vitro inhibitory concentration against Total peroxyl radical-trapping antioxidant parameter(TRAP)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Nitrone derivatives of trolox as neuroprotective agents.
AID1762407Antioxidant activity assessed as trolox equivalent of ABTS radical cation scavenging activity incubated for 24 hrs by UV-Vis spectrophotometric analysis2021European journal of medicinal chemistry, Jun-05, Volume: 218Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.
AID1810909Inhibition of human BChE using butyrylthiocholine iodide as substrate at 10 uM incubated for 20 mins followed by substrate addition by Ellman's method
AID1331318Antioxidant activity assessed as inhibition of peroxyl radical-induced oxidation at 10 uM by ORAC assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID1326564Genotoxicity in Salmonella typhimurium TA102 harboring hysG428 mutant assessed as frequency of reversion from histidine auxotrophy to prototrophy at 30 mM after 48 hrs by Ames test (Rvb = 209 +/- 10 No _unit)2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1592384Antioxidant activity assessed as ABTS radical scavenging activity measured after 15 mins by UV-Visible spectrophotometric based assay
AID1083353Antioxidant activity assessed as DPPH radical scavenging activity at 5 X 10'-5 M after 20 min2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1436102Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 1262,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies.
AID234579Inhibition time for 20 uM during peroxidation of liposomal suspension of dilinoleoylphosphatidylcholine (DPLC) indicated by DMVN at 40 degree Centigrade1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Long-chain-substituted uric acid and 5,6-diaminouracil derivatives as novel agents against free radical processes: synthesis and in vitro activity.
AID1311888Antioxidant activity against human SH-SY5Y cells assessed as amyloid beta (1 to 42)-induced ROS production preincubated for 1 day prior H2O2 treatment at 1.25 uM by DCFH-DA-based fluorescence analysis relative to control2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, and evaluation of Trolox-conjugated amyloid-β C-terminal peptides for therapeutic intervention in an in vitro model of Alzheimer's disease.
AID1678102Antioxidant activity assessed as DPPH radical scavenging activity at 1 uM relative to control2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID451361Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by spectrophotometry2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Antioxidant efficacy of iridoid and phenylethanoid glycosides from the medicinal plant Teucrium chamaedris in cell-free systems.
AID295045Inhibition of horseradish peroxidase2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID1325289Antioxidant activity assessed as ferric ion reducing activity by measuring Fe2+ levels using fe3+-TPTZ at 3000 ug/ml after 30 mins by FRAP assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID457183Antioxidant activity assessed as superoxide radical scavenging activity by chemiluminescence assay2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Quiquelignan A-H, eight new lignoids from the rattan palm Calamus quiquesetinervius and their antiradical, anti-inflammatory and antiplatelet aggregation activities.
AID1348945Antiproliferative activity against human MCF7 cells at 30 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Trisubstituted barbiturates and thiobarbiturates: Synthesis and biological evaluation as xanthine oxidase inhibitors, antioxidants, antibacterial and anti-proliferative agents.
AID639461Antioxidant activity in human SH-SY5Y cells assessed as sequestering of rotenone/oligomycin A-induced mitochondrial free radicals at 0.3 uM after 120 mins by DCFH-DA assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID628336Antioxidant activity in rat hepatic microsomes assessed as inhibition of lipid peroxidation by spectrophotometric analysis2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Novel benzoxazine and benzothiazine derivatives as multifunctional antihyperlipidemic agents.
AID1326567Antioxidant activity in Salmonella typhimurium TA102 harboring hysG428 mutant assessed as inhibition of t-BuO2H-dependant mutant formation at 3 uM preincubated with compound followed by t-BuO2H addition after 48 hrs by Ames test2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID490421Cytotoxicity against HMEC1 cells after 6 hrs by MTT assay2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antioxidant activity evaluation of a syringic hydrazones family.
AID1678100Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM relative to control2020Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.
AID762877Antioxidant activity assessed as trolox equivalents of peroxyl radical scavenging activity at 0.3 to 2 uM preincubated for 15 mins by ORAC assay relative to control2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and electrochemical and biological studies of novel coumarin-chalcone hybrid compounds.
AID450085Antioxidant activity assessed as DPPH radical scavenging activity2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Antioxidant activity of 5,10-dihydroindeno[1,2-b]indoles containing substituents on dihydroindeno part.
AID1581666Antioxidant activity assessed as increase in total ferric ion reducing activity at 75 uM using FeCl3.H2O and TPTZ incubated for 60 mins by FRAP assay relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 1871-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
AID1325284Antioxidant activity assessed as DPPH radical scavenging activity incubated in dark for 30 mins2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Antioxidant and anti-inflammatory neolignans from the seeds of hawthorn.
AID401040Antioxidant activity against cupric ion-induced lipid peroxidation in human LDL by TBA assay1998Journal of natural products, May, Volume: 61, Issue:5
Isolation, identification, and antioxidant activity of three stilbene glucosides newly extracted from vitis vinifera cell cultures
AID490945Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 20 mins2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological screening of some novel amidocarbamate derivatives of ketoprofen.
AID286754Antioxidant activity assessed as DPPH reducing activity at 0.1 mM after 60 mins2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.
AID1659476Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM relative to control2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID295044Inhibition of 3alphaHSD2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).
AID1918880Antioxidant activity assessed as inhibition of ABTS radical scavenging activity measured upto 6 mins2022Journal of natural products, 12-23, Volume: 85, Issue:12
Bioactive Arylnaphthalide Lignans from
AID469413Neuroprotective activity against human SH-SY5Y cells assessed as cytoprotection at 0.1 uM coincubated with rotenone/oligomycin A measured after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID1264040Antioxidant activity in human ARPE19 cells assessed as reduction of xanthine oxidase-mediated superoxide generation preincubated for 1 hr followed by xanthine oxidase challenge for 1 hr by MitoSOX staining-based fluorescence analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Orally Bioavailable Metal Chelators and Radical Scavengers: Multifunctional Antioxidants for the Coadjutant Treatment of Neurodegenerative Diseases.
AID1327545Metal chelating activity of compound assessed as compound-Cu2+ complex formation at 200 uM after 10 mins in presence of CuSO4.5H2O by complexometric indicator murexide based UV-Vis spectrophotometric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer's disease.
AID1704055Antioxidant activity assessed as radical scavenging activity measured after 30 mins by DPPH assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, inhibitory activity and in silico docking of dual COX/5-LOX inhibitors with quinone and resorcinol core.
AID1179763Ratio of compound IC50 to trolox IC50 for DPPH radical scavenging activity after 30 mins by spectrophotometry2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Phenylpropanoid acid esters from Korean propolis and their antioxidant activities.
AID1372030Antioxidant activity assessed as relative scavenging rate constant for photolysis-induced singlet oxygen scavenging activity by measuring Kaox/Kst ratio using 4-HO-TEMP spin trap by ESR spectroscopic method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Resveratrol analogues like piceatannol are potent antioxidants as quantitatively demonstrated through the high scavenging ability against reactive oxygen species and methyl radical.
AID1256117Metal chelating activity assessed as inhibition of Fe2+-ferrozine complex formation after 10 mins2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
AID1809146Antioxidant activity assessed as ABTS radical scavenging activity2021Bioorganic & medicinal chemistry letters, 11-15, Volume: 52Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity.
AID288847Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins2007Journal of natural products, Jun, Volume: 70, Issue:6
Cyathusals A, B, and C, antioxidants from the fermented mushroom Cyathus stercoreus.
AID459649Cytotoxicity against human MRC5 cells assessed as cell death at 60 uM after 7 days by LDH assay2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Exploring a synthetic organoselenium compound for antioxidant pharmacotherapy--toxicity and effects on ROS-production.
AID1075993Antioxidant activity assessed as inhibition of ABTS radical cation formation after 15 mins by ABTS radical scavenging method2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1709279Neuroprotective activity against H2O2-induced cytotoxicity in rat PC12 cells assessed as increase in cell viability at 100 uM preincubated for 2 hrs followed by H2O2 addition and measured after 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1713227Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 25 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID427137Antioxidant activity assessed as superoxide radical anion scavenging activity after 30 mins by xanthine/xanthine oxidase method2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
p-Terphenyls from the fruiting bodies of Paxillus curtisii and their antioxidant properties.
AID738172Inhibition of PMA induced ROS generation in human HL60 cells assessed as inhibition of ROA mediated oxidation of DCFH2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Cytotoxicity and modulation of cancer-related signaling by (Z)- and (E)-3,4,3',5'-tetramethoxystilbene isolated from Eugenia rigida.
AID736826Neuroprotective activity in mouse HT22 cells assessed as prevention from tBuOOH-induced oxidative cell death after 3 hrs by MTS assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Structure-activity relationship study of vitamin k derivatives yields highly potent neuroprotective agents.
AID1713232Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 0.8 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID427665Antioxidant activity assessed as DPPH radical scavenging activity incubated at 40 degC in dark after 30 mins2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Potential antioxidants and tyrosinase inhibitors from synthetic polyphenolic deoxybenzoins.
AID1179731Cytoprotection in mouse CRL2181 cells assessed as reduction in UV-oxidized LDL-induced cytotoxicity by measuring cell viability at 1 uM after 24 hrs by MTT assay relative to untreated control2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.
AID490418Cytoprotective activity against copper-induced LDL oxidation in HMEC1 cells at 10 uM after 6 hrs by MTT assay2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and antioxidant activity evaluation of a syringic hydrazones family.
AID451363Antioxidant activity assessed as inhibition of lipid peroxidation after 60 mins by TBARS assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Antioxidant efficacy of iridoid and phenylethanoid glycosides from the medicinal plant Teucrium chamaedris in cell-free systems.
AID548182Antioxidant activity assessed as ABTS radical scavenging activity2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Benzophenones and biflavonoids from Rheedia edulis.
AID450089Antioxidant activity assessed as hydrogen peroxide radical scavenging activity2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Antioxidant activity of 5,10-dihydroindeno[1,2-b]indoles containing substituents on dihydroindeno part.
AID1603217Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM relative to control2019Bioorganic & medicinal chemistry, 04-15, Volume: 27, Issue:8
Designing of acyl sulphonamide based quinoxalinones as multifunctional aldose reductase inhibitors.
AID1892590Antioxidant activity in rat brain homogenate assessed as inhibition of lipid peroxidation by measuring MDA concentration at 50 uM by TBARS assay relative to control2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Novel Hydroxychalcone-Based Dual Inhibitors of Aldose Reductase and α-Glucosidase as Potential Therapeutic Agents against Diabetes Mellitus and Its Complications.
AID1543565Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as cell viability at 10 uM measured after 24 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease.
AID1083343Antiviral activity against Vesicular stomatitis virus infected Hela cells assessed as inhibition of virus-induced cytopathicity2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 20, Issue:2
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity.
AID1071849Antioxidant activity assessed as AAPH-induced alkoxyl radical scavenging activity by ESR spin trapping method relative to CYPMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1326563Genotoxicity in Escherichia coli PQ37 expressing lacZ gene assessed as ratio of inducible beta-galactosidase activity to alkaline phosphatase activity at 3 mM after 2 hrs by SOS-chromotest relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Antioxidant and antitumor activity of trolox, trolox succinate, and α-tocopheryl succinate conjugates with nitroxides.
AID1594823Antioxidant activity assessed as DPPH radical scavenging activity2019Journal of natural products, 06-28, Volume: 82, Issue:6
Konamycins A and B and Rubromycins CA1 and CA2, Aromatic Polyketides from the Tunicate-Derived Streptomyces hyaluromycini MB-PO13
AID1713231Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 1.6 uM measured after 2 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and in vitro, ex-vivo and in vivo activity of hybrid compounds linking a potent ROS and RNS scavenger activity with diverse substrates addressed to pass across the blood-brain barrier.
AID1071847Antioxidant activity assessed as DMSO/H2O2-induced methyl radical scavenging activity by ESR spin trapping method relative to DMPO2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
A multiple free-radical scavenging (MULTIS) study on the antioxidant capacity of a neuroprotective drug, edaravone as compared with uric acid, glutathione, and trolox.
AID1306591Antioxidant activity assessed as inhibition of DPPH free radical scavenging activity by EPR spectrophotometry2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.
AID1730599Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins under dark condition2021European journal of medicinal chemistry, Mar-05, Volume: 213Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID377071Antioxidant activity assessed as DPPH radical scavenging activity studied at DPPH to compound ratio of 22005Journal of natural products, Feb, Volume: 68, Issue:2
Identification of radical scavenging compounds in Rhaponticum carthamoides by means of LC-DAD-SPE-NMR.
AID1299566Antioxidant activity assessed as ABTS free radical scavenging activity after 6 mins by ABTS free radical decolorization assay2016Journal of natural products, Feb-26, Volume: 79, Issue:2
Cystoseira usneoides: A Brown Alga Rich in Antioxidant and Anti-inflammatory Meroditerpenoids.
AID195017LPO-lowering activity was estimated by the IC50 value of compound in rat liver microsomal lipid peroxidation1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
AID1322937Antioxidant activity of the compound assessed as time required to induce AAPH-mediated linoleic acid peroxidation (Rvb = 40 to 60 mins)2016European journal of medicinal chemistry, Oct-04, Volume: 121Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1802996AChE Inhibition Bioassay from Article 10.3109/14756366.2010.529806: \\Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.\\2011Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 26, Issue:4
Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,487)

TimeframeStudies, This Drug (%)All Drugs %
pre-199021 (1.41)18.7374
1990's244 (16.41)18.2507
2000's555 (37.32)29.6817
2010's586 (39.41)24.3611
2020's81 (5.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.27

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.27 (24.57)
Research Supply Index7.35 (2.92)
Research Growth Index5.72 (4.65)
Search Engine Demand Index34.82 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.27)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (1.04%)5.53%
Reviews18 (1.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (0.06%)0.25%
Other1,506 (97.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase IIb Open-label, Multi-centre, Extension Study to Explore the Long-term Safety and Efficacy of KH176 in Subjects With a Genetically Confirmed Mitochondrial DNA tRNALeu(UUR) m.3243A>G Mutation Who Have Completed the KHENERGYZE Study KH176-202. [NCT04604548]Phase 215 participants (Anticipated)Interventional2021-08-09Active, not recruiting
An Exploratory, Double-blind, Randomized, Placebo-controlled, Single-center, Two-way Cross-over Study With KH176 in Patients With the Mitochondrial DNA tRNALeu(UUR) m.3243A>G Mutation and Clinical Signs of Mitochondrial Disease [NCT02909400]Phase 220 participants (Actual)Interventional2016-09-30Completed
A Phase I, Randomized, Double Blind, Placebo-controlled, Dose-escalating Clinical Trial With KH176 [NCT02544217]Phase 132 participants (Actual)Interventional2015-05-31Completed
A Phase IIb Double-blind, Randomised, Placebo-controlled, Multi-centre, Confirmative Three-way Cross-over Study on Cognitive Function With Two Doses of KH176 in Subjects With a Genetically Confirmed Mitochondrial DNA tRNALeu(UUR) m.3243A>G Mutation. [NCT04165239]Phase 227 participants (Actual)Interventional2019-10-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02544217 (118) [back to overview]Accumulation Factor (Racc) of KH176 Over 7 Days: MAD Group
NCT02544217 (118) [back to overview]Accumulation Factor (Racc) of KH183 (Active Metabolite of KH176): MAD Group
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration Versus Time Curve (AUClast) of KH176: SAD Group
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration Versus Time Curve (AUClast) of KH183: SAD Group
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero Until Infinity (AUCl0-inf) of KH176: SAD
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero Until Infinity (AUCl0-inf) of KH183: SAD
NCT02544217 (118) [back to overview]KH173 + KH183: Percentage of Administered Dose Excreted in Urine: MAD
NCT02544217 (118) [back to overview]KH176 + KH183: Percentage of Administered Dose Excreted in Urine: SAD
NCT02544217 (118) [back to overview]KH176: Percentage of Administered Dose Excreted in Urine: MAD
NCT02544217 (118) [back to overview]KH176: Percentage of Administered Dose Excreted in Urine: SAD
NCT02544217 (118) [back to overview]KH183: Percentage of Administered Dose Excreted in Urine: MAD
NCT02544217 (118) [back to overview]KH183: Percentage of Administered Dose Excreted in Urine: SAD
NCT02544217 (118) [back to overview]Maximum Concentration (Cmax) of KH176: SAD Group
NCT02544217 (118) [back to overview]Maximum Concentration (Cmax) of KH183 Over 24 Hours: SAD
NCT02544217 (118) [back to overview]Terminal Elimination Half-life (T1/2) of KH176 Over 24 Hours: SAD
NCT02544217 (118) [back to overview]Terminal Elimination Half-life (T1/2) of KH183: SAD
NCT02544217 (118) [back to overview]Time to Maximum Concentration (Tmax) of KH176 Over 24 Hours: SAD
NCT02544217 (118) [back to overview]Time to Reach Peak Plasma Concentration (Tmax) of KH183: SAD
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration-time Curve (AUCtau) of KH176: MAD Group:
NCT02544217 (118) [back to overview]Area Under the Plasma Concentration-time Curve During a Dose Interval (AUCtau) of KH183 (Active Metabolite of KH176): MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Alanine Aminotransferase. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Alkaline Phosphatase. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Aspartate Aminotransferase. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Bicarbonate. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Calcium (Corrected for Albumin). MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Chloride. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Cholesterol. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Creatine Kinase. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Creatinine. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Fasting Glucose. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Gamma GT. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: High Density Lipoproteins. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Human Serum Albumin. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Lactate. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Lipase. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Low Density Lipoproteins. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Phosphate. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Potassium. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Sodium. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Thyroid-stimulating Hormone. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Thyroxine (T4). MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Total Bilirubin. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Total Protein. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Triglycerides. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Trilodothyronine (T3). MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Urea. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Time Point: Uric Acid. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: (Fasting) Glucose. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Alanine Aminotransferase. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Alkaline Phosphatase. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Aspartate Aminotransferase. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Bicarbonate. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Calcium (Corrected for Albumin). SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Chloride. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Cholesterol. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Creatinine Kinase. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Creatinine. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Gamma-GT. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: High Density Lipoproteins. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Human Serum Albumin. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Lactate. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Lipase. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Low Density Lipoproteins. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Phosphate. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Potassium. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Sodium. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Thyroid-stimulating Hormone. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Thyroxine (T4). SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Total Bilirubin. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Total Protein. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Triglycerides. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Triiodothyronine (T3). SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Urea. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Uric Acid. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Basophils. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Basophils. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Eosinophils. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Eosinophils. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Erythrocyte Sedimentation Rate (SAD Group)
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Erythrocyte Sedimentation Rate MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hematocrit MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hematocrit SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hemoglobin. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Lymphocytes. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Lymphocytes. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Haemoglobin Concentration. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Haemoglobin. SAD
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Hemoglobin Concentration - SAD
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Hemoglobin. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Volume - SAD
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Volume. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Monocytes. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Monocytes. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Neutrophils. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Neutrophils. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Red Blood Cell Count. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Red Blood Cell Count. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Thrombocytes. MAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: Thrombocytes. SAD Group
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: White Blood Cell Count. MAD
NCT02544217 (118) [back to overview]Change From Baseline in Hematology Laboratory Test Results by Timepoint: White Blood Cell Count. SAD Group
NCT02544217 (118) [back to overview]MAD: Change From Baseline in ECG Results by Time Point: Corrected QT Interval According to Barret's Formaula (QTcB)
NCT02544217 (118) [back to overview]MAD: Change From Baseline in ECG Results by Time Point: P Wave-Q Wave Interval (PQ Interval)
NCT02544217 (118) [back to overview]MAD: Change From Baseline in ECG Results by Time Point: QT Interval
NCT02544217 (118) [back to overview]MAD: Change From Baseline in ECG Results by Time Point: QTcF
NCT02544217 (118) [back to overview]MAD: Change From Baseline in ECG Results by Time Point: the Interval That Denotes Depolarization of the Ventricles, Between the Beginning of the Q Wave and the End of the S Wave (QRS Interval)
NCT02544217 (118) [back to overview]Maximum Concentration (Cmax) of KH176: MAD
NCT02544217 (118) [back to overview]Maximum Concentration (Cmax) of KH183 (Active Metabolite of KH176): MAD Group
NCT02544217 (118) [back to overview]Pharmacodynamics of KH176
NCT02544217 (118) [back to overview]Phospholipidosis
NCT02544217 (118) [back to overview]Relationship to Study Drug and Severity of Treatment-emergent Adverse Events
NCT02544217 (118) [back to overview]SAD: Change From Baseline in ECG Results by Time Point: PQ Interval
NCT02544217 (118) [back to overview]SAD: Change From Baseline in ECG Results by Time Point: QRS Interval
NCT02544217 (118) [back to overview]SAD: Change From Baseline in ECG Results by Time Point: QT Interval
NCT02544217 (118) [back to overview]SAD: Change From Baseline in ECG Results by Time Point: QTcB Interval
NCT02544217 (118) [back to overview]SAD: Change From Baseline in ECG Results by Timepoint: Corrected QT Interval According to Fridericia's Formula (QTcF)
NCT02544217 (118) [back to overview]Time to Maximum Concentration (Tmax) of KH176 at Day 1, Day 7: MAD Group
NCT02544217 (118) [back to overview]Time to Maximum Concentration (Tmax) of KH183 (Active Metabolite of KH176): MAD Group

Accumulation Factor (Racc) of KH176 Over 7 Days: MAD Group

Plasma concentrations of KH176 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d.. Racc was calculated as follows: AUCtau day 7/ AUCtau day 1. (NCT02544217)
Timeframe: Pre-dose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

Interventionratio (Geometric Mean)
Racc Dose 100mg2.52
Racc- Dose 200mg2.65
Racc - Dose 400mg2.17

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Accumulation Factor (Racc) of KH183 (Active Metabolite of KH176): MAD Group

Plasma concentrations of KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d.: Accumulation factor was calculated as follows: AUCtau day 7/ AUCtau day 1. (NCT02544217)
Timeframe: Predose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

Interventionratio (Geometric Mean)
Racc Dose 100mg1.86
Racc- Dose 200mg1.32
Racc - Dose 400mg1.19

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Area Under the Plasma Concentration Versus Time Curve (AUClast) of KH176: SAD Group

Plasma concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionh*ng/mL (Geometric Mean)
SAD Group I 10mg75
SAD Group II 30mg389
SAD Group I 100mg1310
SAD Group II 300mg6320
SAD Group I 800mg21000
SAD Group II 2000mg61200
Group I 100mg + Food1650

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Area Under the Plasma Concentration Versus Time Curve (AUClast) of KH183: SAD Group

Plasma concentrations of KH183 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food) , 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionh*ng/mL (Geometric Mean)
SAD Group I 10mg151
SAD Group II 30mg547
SAD Group I 100mg1810
SAD Group II 300mg4830
SAD Group I 800mg11700
SAD Group II 2000mg23900
Group I 100mg + Food1590

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Area Under the Plasma Concentration-time Curve From Time Zero Until Infinity (AUCl0-inf) of KH176: SAD

Plasma concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food) , 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionh*ng/mL (Geometric Mean)
SAD Group I 10mg0
SAD Group II 30mg474
SAD Group I 100mg1540
SAD Group II 300mg7500
SAD Group I 800mg25800
SAD Group II 2000mg79100
Group I 100mg + Food1970

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Area Under the Plasma Concentration-time Curve From Time Zero Until Infinity (AUCl0-inf) of KH183: SAD

Plasma concentrations of KH183 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food) , 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionh*ng/mL (Geometric Mean)
SAD Group I 10mg234
SAD Group II 30mg881
SAD Group I 100mg2690
SAD Group II 300mg6690
SAD Group I 800mg18700
SAD Group II 2000mg41300
Group I 100mg + Food2410

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KH173 + KH183: Percentage of Administered Dose Excreted in Urine: MAD

Urine concentrations of KH176 and KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: Day 7 Post dose

Interventionpercentage of dose excreted (Geometric Mean)
MAD Group Dose 100mg20.7
MAD Group - Dose 200mg17.4
MAD Group - Dose 400mg19.0

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KH176 + KH183: Percentage of Administered Dose Excreted in Urine: SAD

Urine concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: 24 hours post-dose

Interventionpercentage of dose excreted (Geometric Mean)
SAD Group I 10mg14.4
SAD Group II 30mg17.2
SAD Group I 100mg15.8
SAD Group II 300mg13.4
SAD Group I 800mg14.8
SAD Group II 2000mg15.9

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KH176: Percentage of Administered Dose Excreted in Urine: MAD

Urine concentrations of KH176 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: Day 7 post dose

Interventionpercentage of dose excreted (Geometric Mean)
MAD Group Dose 100mg14.9
MAD Group - Dose 200mg13.4
MAD Group - Dose 400mg14.0

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KH176: Percentage of Administered Dose Excreted in Urine: SAD

Urine concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: 24 hours post-dose

Interventionpercentage of dose excreted (Geometric Mean)
SAD Group I 10mg9.71
SAD Group II 30mg10.5
SAD Group I 100mg10.4
SAD Group II 300mg9.53
SAD Group I 800mg10.9
SAD Group II 2000mg12.4

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KH183: Percentage of Administered Dose Excreted in Urine: MAD

Urine concentrations of KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: Post dose Day 7

Interventionpercentage of dose excreted (Geometric Mean)
MAD Group Dose 100mg5.30
MAD Group - Dose 200mg3.79
MAD Group - Dose 400mg4.85

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KH183: Percentage of Administered Dose Excreted in Urine: SAD

Urine concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: 24 hours post-dose

Interventionpercentage of dose excreted (Geometric Mean)
SAD Group I 10mg4.56
SAD Group II 30mg6.42
SAD Group I 100mg5.18
SAD Group II 300mg3.81
SAD Group I 800mg3.86
SAD Group II 2000mg3.33

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Maximum Concentration (Cmax) of KH176: SAD Group

Plasma concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionng/mL (Geometric Mean)
SAD Group I 10mg12.9
SAD Group II 30mg56.2
SAD Group I 100mg167
SAD Group II 300mg766
SAD Group I 800mg2170
SAD Group II 2000mg5990
Group I 100mg + Food165

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Maximum Concentration (Cmax) of KH183 Over 24 Hours: SAD

Plasma concentrations of KH183 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food) , 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionng/mL (Geometric Mean)
SAD Group I 10mg14.2
SAD Group II 30mg49.4
SAD Group I 100mg168
SAD Group II 300mg497
SAD Group I 800mg1100
SAD Group II 2000mg1780
Group I 100mg + Food117

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Terminal Elimination Half-life (T1/2) of KH176 Over 24 Hours: SAD

Plasma concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionhours (Geometric Mean)
SAD Group I 10mg0
SAD Group II 30mg10.3
SAD Group I 100mg9.10
SAD Group II 300mg9.64
SAD Group I 800mg9.80
SAD Group II 2000mg11.5
Group I 100mg + Food9.09

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Terminal Elimination Half-life (T1/2) of KH183: SAD

Plasma concentrations of KH183 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food) , 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionhours (Geometric Mean)
SAD Group I 10mg16.6
SAD Group II 30mg17.8
SAD Group I 100mg15.4
SAD Group II 300mg14.3
SAD Group I 800mg17.2
SAD Group II 2000mg18.9
Group I 100mg + Food14.9

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Time to Maximum Concentration (Tmax) of KH176 Over 24 Hours: SAD

Plasma concentrations of KH176 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionhours (Geometric Mean)
SAD Group I 10mg1.03
SAD Group II 30mg1.03
SAD Group I 100mg0.931
SAD Group II 300mg1.10
SAD Group I 800mg1.36
SAD Group II 2000mg0.931
Group I 100mg + Food2.45

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Time to Reach Peak Plasma Concentration (Tmax) of KH183: SAD

Plasma concentrations of KH183 were analysed after single dose administration of doses 10mg, 30mg, 100mg (with and without food), 300mg, 800mg, 2000mg b.i.d. (NCT02544217)
Timeframe: Pre-dose (5 min before dosing) and 0.5, 1, 1.5, 2, 3, 6, 8, 12, and 24 hours post-dose

Interventionng/mL (Geometric Mean)
SAD Group I 10mg1.32
SAD Group II 30mg1.46
SAD Group I 100mg1.32
SAD Group II 300mg1.31
SAD Group I 800mg1.61
SAD Group II 2000mg1.57
Group I 100mg + Food2.45

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Area Under the Plasma Concentration-time Curve (AUCtau) of KH176: MAD Group:

Plasma concentrations of KH176 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: Pre-dose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionh*ng/mL (Geometric Mean)
Day 1Day 7
AUCtau - Dose 200mg22505960
AUCtau - Dose 400mg689014900
AUCtau Dose 100mg10902760

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Area Under the Plasma Concentration-time Curve During a Dose Interval (AUCtau) of KH183 (Active Metabolite of KH176): MAD Group

Plasma concentrations of KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: Predose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionh*ng/mL (Geometric Mean)
Day 1Day 7
AUCtau - Dose 200mg16802220
AUCtau - Dose 400mg36004270
AUCtau Dose 100mg7021310

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Alanine Aminotransferase. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III25.30.0-1.81.3
MAD Group IV21.3-0.32.36.3
MAD Group V20.5-1.30.34.8
Placebo22.32.02.82.3

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Alkaline Phosphatase. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III66.07.313.09.0
MAD Group IV67.32.05.010.8
MAD Group V55.31.56.09.8
Placebo52.31.83.33.3

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Aspartate Aminotransferase. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III20.3-2.0-1.01.5
MAD Group IV21.5-5.0-2.81.3
MAD Group V18.5-2.5-0.39.8
Placebo23.0-1.7-1.52.8

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Bicarbonate. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III27.53-0.38-1.10-1.18
MAD Group IV25.532.201.421.68
MAD Group V28.530.10-0.55-0.32
Placebo27.230.030.47-0.27

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Calcium (Corrected for Albumin). MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III2.2780.1050.1270.087
MAD Group IV2.3100.0830.0830.083
MAD Group V2.2650.0480.1000.045
Placebo2.3230.0680.0880.055

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Chloride. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III103.8-2.5-3.5-2.0
MAD Group IV101.5-2.0-2.0-2.3
MAD Group V102.0-1.5-2.8-2.0
Placebo102.2-1.5-2.2-1.3

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Cholesterol. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III192.820.032.39.3
MAD Group IV191.08.82.58.0
MAD Group V203.513.513.39.8
Placebo177.819.724.3-5.5

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Creatine Kinase. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III129.5-48.5-50.827.0
MAD Group IV192.3-68.8-83.8-7.5
MAD Group V146.5-58.0-68.0150.5
Placebo229.8-106.5-123.542.2

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Creatinine. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III0.9100.0950.0050.008
MAD Group IV0.9600.1220.122-0.020
MAD Group V0.9130.1650.1330.017
Placebo0.8970.0570.0530.007

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Fasting Glucose. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III89.0-6.8-6.5-2.2
MAD Group IV85.52.8-9.52.0
MAD Group V89.8-6.8-7.0-10.8
Placebo87.21.5-3.50.0

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Gamma GT. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III15.50.50.81.3
MAD Group IV18.30.30.3-0.5
MAD Group V20.52.01.81.8
Placebo21.50.70.0-0.8

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: High Density Lipoproteins. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III51.0-1.0-5.0-2.5
MAD Group IV61.0-3.0-7.81.3
MAD Group V53.5-1.5-3.57.5
Placebo66.8-2.5-7.0-2.2

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Human Serum Albumin. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventiong/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III43.33.35.32.8
MAD Group IV45.53.83.53.0
MAD Group V42.81.34.03.3
Placebo44.71.53.81.7

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Lactate. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III8.630.983.132.75
MAD Group IV7.002.232.301.08
MAD Group V7.231.181.836.63
Placebo9.125.931.23-0.12

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Lipase. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III26.5-1.8-0.33.5
MAD Group IV26.50.01.317.3
MAD Group V32.826.050.5-2.8
Placebo34.21.21.0-1.8

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Low Density Lipoproteins. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III114.117.933.28.1
MAD Group IV112.94.91.46.9
MAD Group V127.09.03.5-1.5
Placebo93.318.825.6-1.9

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Phosphate. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III0.9780.1020.052-0.030
MAD Group IV1.0330.0030.000-0.010
MAD Group V0.9200.015-0.0200.053
Placebo1.000-0.005-0.002-0.002

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Potassium. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III4.200.450.070.25
MAD Group IV4.350.330.150.45
MAD Group V4.400.100.250.25
Placebo4.320.520.150.30

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Sodium. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III143.8-0.5-3.0-1.5
MAD Group IV141.3-1.50.8-0.3
MAD Group V141.00.81.02.0
Placebo142.0-1.0-0.50.2

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Thyroid-stimulating Hormone. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
InterventionmU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III1.410.110.280.16
MAD Group IV1.480.090.45-0.15
MAD Group V1.200.480.750.05
Placebo1.580.250.850.05

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Thyroxine (T4). MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionng/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III1.200.050.120.12
MAD Group IV1.250.020.070.03
MAD Group V1.200.050.230.12
Placebo1.070.030.170.10

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Total Bilirubin. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III0.500.380.33-0.02
MAD Group IV0.550.050.03-0.08
MAD Group V0.630.200.180.08
Placebo0.650.130.08-0.05

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Total Protein. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day1), Day 3, Day 8, FU (one week after last dosing)

,,,
Interventiong/L (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III65.34.07.05.0
MAD Group IV67.32.34.34.8
MAD Group V63.82.56.04.0
Placebo66.01.74.81.8

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Triglycerides. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III140.314.817.816.0
MAD Group IV83.535.546.80.5
MAD Group V114.030.569.020.3
Placebo90.214.828.3-8.0

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Trilodothyronine (T3). MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionpg/mL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III3.35-0.05-0.320.30
MAD Group IV3.35-0.280.10-0.05
MAD Group V3.30-0.15-0.130.18
Placebo3.08-0.15-0.050.18

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Urea. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III24.86.05.82.3
MAD Group IV28.02.8-0.5-0.5
MAD Group V29.82.00.5-0.5
Placebo30.22.5-1.0-0.3

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Change From Baseline in Chemistry Laboratory Test Results by Time Point: Uric Acid. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline, Day 3, Day 8, FU (one week after last dosing)

,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III5.650.500.280.08
MAD Group IV4.930.58-0.020.55
MAD Group V5.400.750.150.22
Placebo5.25-0.07-0.63-0.05

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: (Fasting) Glucose. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food78.83.36.3
Group I Placebo85.0-1.0-0.2
Group I Placebo + Food84.04.02.0
Group II Placebo86.81.25.5
SAD Group I 100mg77.87.07.3
SAD Group I 10mg84.82.0-0.3
SAD Group I 800mg87.00.5-1.3
SAD Group II 2000mg95.5-2.3-1.5
SAD Group II 300mg86.3-1.00.5
SAD Group II 30mg88.5-2.06.3

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Alanine Aminotransferase. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food15.01.51.8
Group I Placebo20.2-1.2-1.0
Group I Placebo + Food19.01.57.5
Group II Placebo17.2-0.35.7
SAD Group I 100mg15.01.31.8
SAD Group I 10mg19.30.82.3
SAD Group I 800mg22.8-2.0-2.3
SAD Group II 2000mg17.80.3-1.0
SAD Group II 300mg19.3-0.36.0
SAD Group II 30mg20.0-1.38.3

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Alkaline Phosphatase. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food62.30.8-0.8
Group I Placebo62.0-0.2-1.5
Group I Placebo + Food54.52.02.0
Group II Placebo64.01.71.7
SAD Group I 100mg66.01.01.5
SAD Group I 10mg66.01.01.8
SAD Group I 800mg53.31.3-2.0
SAD Group II 2000mg49.06.84.3
SAD Group II 300mg68.33.8-1.5
SAD Group II 30mg75.0-1.8-3.8

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Aspartate Aminotransferase. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food18.5-1.00.0
Group I Placebo20.5-2.70.3
Group I Placebo + Food19.5-1.03.5
Group II Placebo16.80.33.3
SAD Group I 100mg18.3-2.50.3
SAD Group I 10mg19.3-0.52.8
SAD Group I 800mg18.8-1.01.3
SAD Group II 2000mg17.00.51.0
SAD Group II 300mg20.8-0.30.5
SAD Group II 30mg17.51.84.8

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Bicarbonate. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food25.930.05-1.23
Group I Placebo25.68-0.05-1.22
Group I Placebo + Food24.901.95-0.55
Group II Placebo25.220.280.97
SAD Group I 100mg24.850.40-0.15
SAD Group I 10mg24.781.05-0.58
SAD Group I 800mg27.05-0.17-2.38
SAD Group II 2000mg26.030.05-0.20
SAD Group II 300mg24.282.351.65
SAD Group II 30mg25.851.180.95

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Calcium (Corrected for Albumin). SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food2.3600.0750.055
Group I Placebo2.3800.0330.010
Group I Placebo + Food2.340-0.005-0.065
Group II Placebo2.3030.0950.062
SAD Group I 100mg2.3730.0580.042
SAD Group I 10mg2.2900.0980.085
SAD Group I 800mg2.3530.078-0.005
SAD Group II 2000mg2.3230.1480.090
SAD Group II 300mg2.3580.085-0.032
SAD Group II 30mg2.2880.0930.073

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Chloride. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food101.5-0.50.0
Group I Placebo102.7-0.5-1.5
Group I Placebo + Food100.52.03.5
Group II Placebo104.0-2.5-3.2
SAD Group I 100mg102.30.0-0.8
SAD Group I 10mg103.8-1.5-2.5
SAD Group I 800mg103.3-1.3-0.8
SAD Group II 2000mg103.8-3.5-3.0
SAD Group II 300mg103.0-2.8-2.3
SAD Group II 30mg104.0-3.5-3.5

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Cholesterol. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food166.55.88.3
Group I Placebo176.04.85.0
Group I Placebo + Food200.512.5-2.5
Group II Placebo151.012.526.3
SAD Group I 100mg146.59.528.3
SAD Group I 10mg146.35.325.3
SAD Group I 800mg212.88.3-13.8
SAD Group II 2000mg174.525.06.8
SAD Group II 300mg167.519.524.3
SAD Group II 30mg149.05.321.5

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Creatinine Kinase. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food81.3-14.818.0
Group I Placebo118.2-34.313.0
Group I Placebo + Food82.5-31.521.5
Group II Placebo78.7-14.016.7
SAD Group I 100mg209.3-97.8-110.0
SAD Group I 10mg181.8-51.0-17.3
SAD Group I 800mg68.5-14.015.8
SAD Group II 2000mg89.5-14.87.0
SAD Group II 300mg82.3-15.56.0
SAD Group II 30mg78.8-12.824.5

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Creatinine. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food0.8630.0380.063
Group I Placebo0.9270.023-0.003
Group I Placebo + Food0.9350.015-0.080
Group II Placebo0.7680.0670.065
SAD Group I 100mg0.8380.0400.088
SAD Group I 10mg0.9030.0800.012
SAD Group I 800mg0.9180.090-0.020
SAD Group II 2000mg0.8380.075-0.017
SAD Group II 300mg0.7350.1150.063
SAD Group II 30mg0.8100.0530.073

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Gamma-GT. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food13.50.81.0
Group I Placebo23.5-0.8-4.0
Group I Placebo + Food29.00.03.5
Group II Placebo19.01.210.0
SAD Group I 100mg12.00.32.5
SAD Group I 10mg24.00.0-1.3
SAD Group I 800mg30.0-0.5-7.3
SAD Group II 2000mg21.33.81.8
SAD Group II 300mg17.31.311.3
SAD Group II 30mg23.00.813.8

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: High Density Lipoproteins. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food45.8-0.31.5
Group I Placebo50.0-2.81.8
Group I Placebo + Food47.02.5-2.0
Group II Placebo49.80.54.5
SAD Group I 100mg40.0-1.37.3
SAD Group I 10mg45.51.06.3
SAD Group I 800mg51.5-3.0-3.0
SAD Group II 2000mg48.010.08.8
SAD Group II 300mg54.52.82.8
SAD Group II 30mg49.5-2.53.0

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Human Serum Albumin. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventiong/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food45.80.005
Group I Placebo46.2-0.30.2
Group I Placebo + Food44.00.50.0
Group II Placebo45.01.72.0
SAD Group I 100mg45.31.51.0
SAD Group I 10mg45.30.32.3
SAD Group I 800mg44.01.50.0
SAD Group II 2000mg44.35.33.5
SAD Group II 300mg46.03.50.5
SAD Group II 30mg45.02.02.0

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Lactate. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food8.330.401.70
Group I Placebo7.98-0.801.05
Group I Placebo + Food9.85-1.05-0.15
Group II Placebo7.281.403.80
SAD Group I 100mg8.10-0.501.93
SAD Group I 10mg8.65-2.082.25
SAD Group I 800mg7.530.78-0.02
SAD Group II 2000mg8.583.254.33
SAD Group II 300mg9.030.880.70
SAD Group II 30mg8.232.103.45

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Lipase. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food31.1-2.5-2.5
Group I Placebo31.0-1.5-1.0
Group I Placebo + Food42.0-0.5-7.0
Group II Placebo34.8-7.5-1.0
SAD Group I 100mg27.31.31.5
SAD Group I 10mg39.0-6.3-4.5
SAD Group I 800mg30.0-1.3-2.0
SAD Group II 2000mg25.5-4.89.3
SAD Group II 300mg33.07.3-5.0
SAD Group II 30mg29.3-1.88.0

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Low Density Lipoproteins. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food103.54.47.2
Group I Placebo111.14.50.3
Group I Placebo + Food134.510.0-8.5
Group II Placebo83.58.317.0
SAD Group I 100mg92.36.418.5
SAD Group I 10mg88.92.913.3
SAD Group I 800mg145.95.7-17.9
SAD Group II 2000mg103.116.71.3
SAD Group II 300mg98.712.814.2
SAD Group II 30mg82.51.49.6

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Phosphate. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food1.105-0.015-0.080
Group I Placebo1.0420.033-0.020
Group I Placebo + Food1.410-0.180-0.395
Group II Placebo0.998-0.0450.030
SAD Group I 100mg1.0230.0450.003
SAD Group I 10mg1.120-0.035-0.077
SAD Group I 800mg1.0880.032-0.090
SAD Group II 2000mg1.128-0.090-0.105
SAD Group II 300mg0.983-0.060-0.070
SAD Group II 30mg1.085-0.133-0.018

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Potassium. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food4.200.150.33
Group I Placebo4.250.170.25
Group I Placebo + Food4.000.250.30
Group II Placebo4.270.170.10
SAD Group I 100mg4.030.300.50
SAD Group I 10mg4.250.070.30
SAD Group I 800mg4.280.120.08
SAD Group II 2000mg4.50-0.10-0.05
SAD Group II 300mg4.33-0.050.10
SAD Group II 30mg4.180.230.20

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Sodium. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmmol/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food140.51.01.8
Group I Placebo141.8-0.2-0.3
Group I Placebo + Food139.52.54.5
Group II Placebo142.5-0.7-1.8
SAD Group I 100mg141.5-0.80.8
SAD Group I 10mg141.5-0.30.0
SAD Group I 800mg142.30.50.5
SAD Group II 2000mg143.3-1.3-2.8
SAD Group II 300mg142.0-1.0-2.0
SAD Group II 30mg142.8-2.0-2.3

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Thyroid-stimulating Hormone. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
InterventionmU/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food1.93-0.42-0.10
Group I Placebo1.45-0.200.08
Group I Placebo + Food2.57-0.54-0.69
Group II Placebo1.260.040.45
SAD Group I 100mg1.500.070.32
SAD Group I 10mg1.14-0.120.10
SAD Group I 800mg1.830.050.17
SAD Group II 2000mg1.59-0.12-0.06
SAD Group II 300mg1.550.460.11
SAD Group II 30mg1.14-0.030.77

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Thyroxine (T4). SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionng/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food1.220.030.10
Group I Placebo1.27-0.050.03
Group I Placebo + Food1.350.05-0.10
Group II Placebo1.220.030.15
SAD Group I 100mg1.25-0.050.07
SAD Group I 10mg1.30-0.080.02
SAD Group I 800mg1.200.050.05
SAD Group II 2000mg1.150.100.13
SAD Group II 300mg1.080.120.22
SAD Group II 30mg1.38-0.080.05

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Total Bilirubin. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food1.100.27-0.10
Group I Placebo0.820.300.13
Group I Placebo + Food0.450.150.10
Group II Placebo0.750.12-0.02
SAD Group I 100mg1.18-0.00-0.18
SAD Group I 10mg1.030.400.05
SAD Group I 800mg0.63-0.030.00
SAD Group II 2000mg0.310.310.21
SAD Group II 300mg0.530.280.20
SAD Group II 30mg0.680.380.13

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Total Protein. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventiong/L (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food66.32.32.3
Group I Placebo67.51.31.5
Group I Placebo + Food66.52.51.0
Group II Placebo65.53.73.3
SAD Group I 100mg65.32.83.3
SAD Group I 10mg67.01.54.0
SAD Group I 800mg66.33.00.0
SAD Group II 2000mg66.09.34.8
SAD Group II 300mg66.06.00.8
SAD Group II 30mg67.33.01.8

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Triglycerides. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food86.37.8-1.8
Group I Placebo72.816.716.5
Group I Placebo + Food92.51.543.5
Group II Placebo88.519.024.5
SAD Group I 100mg72.020.312.5
SAD Group I 10mg57.310.330.8
SAD Group I 800mg76.327.037.8
SAD Group II 2000mg117.0-10.3-16.5
SAD Group II 300mg71.022.537.5
SAD Group II 30mg84.531.047.3

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Triiodothyronine (T3). SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionpg/mL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food3.63-0.25-0.28
Group I Placebo3.65-0.35-0.30
Group I Placebo + Food3.60-0.40-0.30
Group II Placebo3.23-0.100.42
SAD Group I 100mg3.48-0.07-0.13
SAD Group I 10mg3.73-0.22-0.23
SAD Group I 800mg3.18-0.230.05
SAD Group II 2000mg3.33-0.130.20
SAD Group II 300mg3.18-0.230.50
SAD Group II 30mg3.400.050.30

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Urea. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food25.8-0.5-1.5
Group I Placebo27.50.01.2
Group I Placebo + Food38.5-9.0-8.0
Group II Placebo24.70.20.5
SAD Group I 100mg24.00.00.3
SAD Group I 10mg30.0-2.5-0.8
SAD Group I 800mg29.3-1.0-0.3
SAD Group II 2000mg34.8-4.0-6.8
SAD Group II 300mg25.3-0.5-2.3
SAD Group II 30mg26.0-0.32.3

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Change From Baseline in Chemistry Laboratory Test Results by Timepoint: Uric Acid. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of clinical chemistry parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventionmg/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food5.50-0.280.33
Group I Placebo5.52-0.250.28
Group I Placebo + Food5.45-0.600.40
Group II Placebo4.85-0.130.32
SAD Group I 100mg5.48-0.300.35
SAD Group I 10mg5.75-0.280.22
SAD Group I 800mg5.48-0.200.18
SAD Group II 2000mg5.100.150.23
SAD Group II 300mg4.75-0.250.30
SAD Group II 30mg4.80-0.200.40

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Basophils. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III30.07.512.57.5
MAD Group IV34.08.5-6.51.0
MAD Group V20.02.55.02.5
Placebo23.33.34.05.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Basophils. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value ateach timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post-dose)

,,,,,,,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food25.0-2.5-2.5
Group I Placebo23.3-5.00.0
Group I Placebo + Food65.0-20.0-15.0
Group II Placebo25.00.0-1.7
SAD Group I 100mg15.00.07.5
SAD Group I 10mg15.02.55.0
SAD Group I 800mg20.02.520.0
SAD Group II 2000mg22.55.00.0
SAD Group II 300mg32.5-5.0-5.0
SAD Group II 30mg30.0-7.5-5.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Eosinophils. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III212.5-40.0-47.5-27.5
MAD Group IV183.5-31.0-28.531.5
MAD Group V127.57.5-10.0-17.5
Placebo141.7-28.3-22.7-45.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Eosinophils. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food152.5-30.0-42.5
Group I Placebo115.0-5.0-13.3
Group I Placebo + Food650.0-25.0-125.0
Group II Placebo191.7-50.0-58.3
SAD Group I 100mg112.5-15.0-2.5
SAD Group I 10mg110.0-17.5-17.5
SAD Group I 800mg245.0-25.077.5
SAD Group II 2000mg110.0-25.0-20.0
SAD Group II 300mg200.0-37.5-42.5
SAD Group II 30mg137.5-22.5-12.5

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Erythrocyte Sedimentation Rate (SAD Group)

(NCT02544217)
Timeframe: Baseline (pre-dose Day1), 24h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventionmm/hr (Mean)
BaselineChange from BL at 24hChange from BL at FU
Group I 100mg + Food2.51.00.0
Group I Placebo2.30.50.3
Group I Placebo + Food5.0-0.50.0
Group II Placebo2.80.30.3
SAD Group I 100mg2.00.00.5
SAD Group I 10mg1.30.00.8
SAD Group I 800mg7.30.3-2.3
SAD Group II 2000mg4.03.00.5
SAD Group II 300mg3.00.30.0
SAD Group II 30mg1.81.00.5

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Erythrocyte Sedimentation Rate MAD Group

(NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days after last dosing)

,,,
Interventionmm/hr (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III4.02.04.85.0
MAD Group IV3.00.80.81.3
MAD Group V2.00.52.51.0
Placebo2.70.80.32.2

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hematocrit MAD Group

Hematocrit is a measure of the ratio of red blood cells (RBCs) in the blood by volume. Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Intervention% of red cells to volume of whole blood. (Mean)
BaselineChange from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III39.932.673.300.92
MAD Group IV43.401.171.22-0.10
MAD Group V45.100.130.10-1.05
Placebo43.301.701.93-0.75

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hematocrit SAD Group

Hematocrit is a measure of the ratio of red blood cells (RBCs) in the blood by volume. Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24 h postdose, FU (7 days after last dosing)

,,,,,,,,,
Intervention%red cells to the volume of whole blood. (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food42.530.680.55
Group I Placebo43.770.53-0.43
Group I Placebo + Food44.351.90-0.65
Group II Placebo43.130.60-0.65
SAD Group I 100mg42.981.420.10
SAD Group I 10mg43.100.750.85
SAD Group I 800mg44.051.33-1.15
SAD Group II 2000mg41.352.330.07
SAD Group II 300mg44.351.03-2.02
SAD Group II 30mg44.381.95-0.93

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Hemoglobin. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventiong/dL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III13.681.051.350.30
MAD Group IV15.230.420.55-0.05
MAD Group V15.680.170.27-0.38
Placebo14.820.620.75-0.35

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Lymphocytes. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III1627.587.512.5-55.0
MAD Group IV1498.5159.0124.039.0
MAD Group V1750.0390.0237.5262.5
Placebo1508.3215.0283.35.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Lymphocytes. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post dose)

,,,,,,,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food1640.0-70.0-27.5
Group I Placebo1570.0-13.386.7
Group I Placebo + Food2260.0-135.0-190.0
Group II Placebo1748.3-16.7-45.0
SAD Group I 100mg1485.0-27.5127.5
SAD Group I 10mg1655.0-45.0180.0
SAD Group I 800mg1550.0287.5135.0
SAD Group II 2000mg1497.537.5-7.5
SAD Group II 300mg1570.092.5-32.5
SAD Group II 30mg1862.5-172.5-92.5

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Haemoglobin Concentration. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventiong/dL RBC (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III34.280.300.47-0.08
MAD Group IV35.050.050.250.00
MAD Group V34.750.300.500.00
Placebo34.230.080.17-0.22

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Haemoglobin. SAD

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24 h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventionpg/cell (Mean)
Baseline (pre-dose Day 1)Change from BL at 24h - Day 1Change from BL at FU
Group I 100mg + Food29.650.20-0.08
Group I Placebo30.320.08-0.22
Group I Placebo + Food30.250.25-0.15
Group II Placebo29.700.230.05
SAD Group I 100mg30.00-0.15-0.42
SAD Group I 10mg30.780.17-0.28
SAD Group I 800mg30.28-0.25-0.58
SAD Group II 2000mg29.800.330.12
SAD Group II 300mg29.63-0.60-0.28
SAD Group II 30mg30.38-0.08-0.23

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Hemoglobin Concentration - SAD

Erythrocyte mean corpuscular hemoglobin concentration (MCHC) is a measure of the average concentration of hemoglobin per red blood cell. Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24 h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventiong/dL RBC (Mean)
Baseline (pre-dose Day 1)Change from BL at 24h - Day 1Change from BL at FU
Group I 100mg + Food34.680.45-0.20
Group I Placebo34.15-0.070.17
Group I Placebo + Food34.700.10-0.60
Group II Placebo33.980.430.47
SAD Group I 100mg34.53-0.17-0.05
SAD Group I 10mg34.180.000.27
SAD Group I 800mg34.20-0.20-0.13
SAD Group II 2000mg33.250.821.00
SAD Group II 300mg34.33-1.050.30
SAD Group II 30mg34.38-0.270.18

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Hemoglobin. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventionpg/cell (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III29.800.250.400.15
MAD Group IV31.330.230.12-0.20
MAD Group V30.030.450.570.40
Placebo30.470.200.250.02

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Volume - SAD

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24 h post dose, FU (7 days after last dosing)

,,,,,,,,,
InterventionfL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food85.48-0.550.20
Group I Placebo88.750.45-1.10
Group I Placebo + Food87.100.601.10
Group II Placebo87.52-0.38-1.03
SAD Group I 100mg86.930.00-1.25
SAD Group I 10mg90.150.35-1.68
SAD Group I 800mg88.55-0.27-1.45
SAD Group II 2000mg89.73-1.33-2.30
SAD Group II 300mg86.420.85-1.52
SAD Group II 30mg88.350.48-0.92

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Mean Corpuscular Volume. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
InterventionfL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III87.00-0.05-0.100.60
MAD Group IV89.320.52-0.43-0.55
MAD Group V86.430.550.321.22
Placebo89.020.400.280.65

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Monocytes. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III505.075.0137.5-52.5
MAD Group IV424.0-11.576.0-21.5
MAD Group V530.057.527.582.5
Placebo418.31.724.3-43.3

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Monocytes. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days post-dose)

,,,,,,,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food512.5-55.0-110.0
Group I Placebo445.01.7-21.7
Group I Placebo + Food550.0-45.0-20.0
Group II Placebo496.7-81.7-78.3
SAD Group I 100mg397.520.05.0
SAD Group I 10mg407.520.030.0
SAD Group I 800mg462.5-25.00.0
SAD Group II 2000mg470.02.5-47.5
SAD Group II 300mg467.5-62.5-42.5
SAD Group II 30mg455.0-45.0-70.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Neutrophils. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III3077.5-567.5105.0185.0
MAD Group IV2602.5350.0312.5177.5
MAD Group V2935.0437.5537.51010.0
Placebo2483.381.7261.0-75.0

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Neutrophils. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventioncells/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food3192.5-122.5-557.5
Group I Placebo2276.7356.7205.0
Group I Placebo + Food2280.0445.0-205.0
Group II Placebo2296.798.3-16.7
SAD Group I 100mg2380.0272.5255.0
SAD Group I 10mg2117.57.590.0
SAD Group I 800mg2565.0285.0-12.5
SAD Group II 2000mg2360.0440.0-382.5
SAD Group II 300mg2197.5165.0-167.5
SAD Group II 30mg2365.0410.0107.5

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Red Blood Cell Count. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells 10^6/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III4.5880.3130.3850.075
MAD Group IV4.8580.1000.1600.020
MAD Group V5.217-0.017-0.007-0.192
Placebo4.8730.1670.198-0.120

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Red Blood Cell Count. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventioncells 10^6/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food4.9850.1150.050
Group I Placebo4.9470.2000.003
Group I Placebo + Food5.0950.185-0.150
Group II Placebo4.9330.095-0.013
SAD Group I 100mg4.9530.1700.083
SAD Group I 10mg4.7930.0630.185
SAD Group I 800mg4.9730.173-0.053
SAD Group II 2000mg4.6230.3250.125
SAD Group II 300mg5.1370.065-0.147
SAD Group II 30mg5.0300.188-0.052

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Thrombocytes. MAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells 10^3/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III207.315.544.863.8
MAD Group IV211.517.54.85.5
MAD Group V199.827.531.333.8
Placebo206.717.329.521.7

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: Thrombocytes. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h, FU (7 days post-dose)

,,,,,,,,,
Interventioncells 10^3/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food215.80.316.3
Group I Placebo209.50.011.8
Group I Placebo + Food204.54.01.0
Group II Placebo204.04.822.5
SAD Group I 100mg215.83.816.3
SAD Group I 10mg193.08.523.8
SAD Group I 800mg202.322.315.8
SAD Group II 2000mg160.123.021.5
SAD Group II 300mg203.8-14.57.3
SAD Group II 30mg223.02.38.5

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: White Blood Cell Count. MAD

Blood samples were collected from participants at the indicated time points for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each time point are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day 3, Day 8, FU (7 days post dose)

,,,
Interventioncells 10^3/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at Day 3Change from BL at Day 8Change from BL at FU
MAD Group III5.463-0.4350.2230.060
MAD Group IV4.7530.4800.4800.230
MAD Group V5.3780.8950.7951.340
Placebo4.5830.2770.563-0.140

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Change From Baseline in Hematology Laboratory Test Results by Timepoint: White Blood Cell Count. SAD Group

Blood samples were collected from participants at the indicated timepoints for evaluation of hematology parameters. The baseline value at visit and the change from baseline value at each timepoint are reported. The change from baseline value was calculated by subtracting the post-baseline value from the baseline value. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), 24h post dose, FU (7 days after last dosing)

,,,,,,,,,
Interventioncells 10^3/µL (Mean)
Baseline (pre-dose Day 1)Change from BL at 24hChange from BL at FU
Group I 100mg + Food5.535-0.280-0.745
Group I Placebo4.4350.3430.258
Group I Placebo + Food5.8150.220-0.560
Group II Placebo4.773-0.057-0.203
SAD Group I 100mg4.3950.2570.395
SAD Group I 10mg4.313-0.0330.288
SAD Group I 800mg4.8530.5280.215
SAD Group II 2000mg5.1180.655-0.320
SAD Group II 300mg4.4750.160-0.287
SAD Group II 30mg4.8630.160-0.073

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MAD: Change From Baseline in ECG Results by Time Point: Corrected QT Interval According to Barret's Formaula (QTcB)

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. Other ECG recordings will be singlet (one recording of at least 3 complexes) prior to dosing, or around the expected Cmax on Day 1 or 7 for the multiple- dose part. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Follow-up

,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline at 2h - Day 1Change from BL at 24h - Day 1Baseline (pre-dose Day 7)Change from pre-dose Day 7 at 1h - Day 7Change from pre-dose Day 7 at 2h - Day 7Change from pre-dose Day 7 at 4hChange from pre-dose Day 7 BL at 6h - Day 7Change from pre-dose Day 7 at 8h - Day 7Change from pre-dose Day 7 at 12h - Day 7Change from BL at pre-dose Day 2Change from BL at pre-dose Day 3Change from BL at pre-dose Day 4Change from BL at pre-dose Day 5Change from BL at pre-dose Day 6Change from BL at pre-dose Day 7Change from BL at FU
MAD Group III391.33.8-1.0398.3-3.8-5.0-7.85.3-7.04.5-1.06.06.513.85.57.07.8
MAD Group IV381.012.30.3386.5-3.85.8-3.812.5-4.53.00.30.52.010.3-2.35.511.0
MAD Group V384.011.811.5402.0-10.32.5-6.5-1.8-11.5-9.011.520.57.514.013.518.010.5
Placebo385.20.7-5.7378.8-3.51.0-0.55.83.06.7-5.7-8.5-10.2-8.5-10.5-11.33.8

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MAD: Change From Baseline in ECG Results by Time Point: P Wave-Q Wave Interval (PQ Interval)

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation of the PQ interval the average of the 3 recordings will be taken as baseline. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Follow-up

,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline at 2h - Day 1Change from BL at 24h - Day 1Baseline (pre-dose Day 7)Change from pre-dose Day 7 at 1h - Day 7Change from pre-dose Day 7 at 2h - Day 7Change from pre-dose Day 7 at 4hChange from pre-dose Day 7 BL at 6h - Day 7Change from pre-dose Day 7 at 8h - Day 7Change from pre-dose Day 7 at 12h - Day 7Change from BL at pre-dose Day 2Change from BL at pre-dose Day 3Change from BL at pre-dose Day 4Change from BL at pre-dose Day 5Change from BL at pre-dose Day 6Change from BL at pre-dose Day 7Change from BL at FU
MAD Group III185.82.8-5.8191.5-1.0-3.5-9.0-13.0-10.0-24.0-5.86.36.3-2.3-0.35.8-6.8
MAD Group IV160.5-1.5-0.5164.05.5-1.5-1.0-3.50.0-1.5-0.54.59.54.03.03.5-2.5
MAD Group V162.06.02.0167.56.54.00.0-4.5-5.0-4.52.00.07.58.56.05.5-3.5
Placebo171.86.2-6.5178.3-1.7-14.7-14.3-6.7-11.3-4.0-6.5-6.8-3.8-2.25.26.50.5

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MAD: Change From Baseline in ECG Results by Time Point: QT Interval

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. Other ECG recordings will be singlet (one recording of at least 3 complexes) prior to dosing, or around the expected Cmax on Day 1 or 7 for the multiple- dose part. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Follow-up

,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from BL at 2h - Day 1Change from BL at 24h - Day 1Baseline (pre-dose Day 7)Change from pre-dose Day 7 at 1h - Day 7Change from pre-dose Day 7 at 2h - Day 7Change from pre-dose Day 7 at 4hChange from pre-dose Day 7 BL at 6h - Day 7Change from pre-dose Day 7 at 8h - Day 7Change from pre-dose Day 7 at 12h - Day 7Change from BL at pre-dose Day 2Change from BL at pre-dose Day 3Change from BL at pre-dose Day 4Change from BL at pre-dose Day 5Change from BL at pre-dose Day 6Change from BL at pre-dose Day 7Change from BL at FU
MAD Group III410.5-5.5-10.0393.05.00.0-7.0-15.5-18.5-20.0-10.0-10.5-6.0-9.0-16.0-17.5-22.0
MAD Group IV391.5-7.51.0388.5-1.0-10.5-2.0-17.0-1.0-20.01.07.5-3.5-13.0-0.5-3.0-10.5
MAD Group V399.0-4.0-14.5402.00.0-7.5-4.0-16.5-11.0-11.5-14.5-10.06.03.0-4.53.0-23.0
Placebo410.24.2-4.2406.01.0-2.310.7-14.3-3.0-8.7-4.2-6.2-0.21.2-3.8-4.213.2

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MAD: Change From Baseline in ECG Results by Time Point: QTcF

"The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation of the corrected QT intervals the average of the 3 recordings will be taken as baseline. Other ECG recordings will be singlet (one recording of at least 3 complexes) prior to dosing, or around the expected Cmax on Day 1 or 7 for the multiple-dose part.~QTcF is calculated as the quotient between the QT interval in milliseconds and the cube root of the RR interval in seconds, according to Fridericia's formula." (NCT02544217)
Timeframe: Baseline, Day1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7

,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from BL at 2h - Day 1Change from BL at 24h - Day 1Change from BL Day 7 at 1h - Day 7Change from BL Day 7 at 2h - Day 7Change from BL Day 7 at 4hChange from BL Day 7 BL at 6h - Day 7Change from BL Day 7 at 8h - Day 7Change from BL Day 7 at 12h - Day 7Change from BL at pre-dose Day 2Change from BL at pre-dose Day 3Change from BL at pre-dose Day 4Change from BL at pre-dose Day 5Change from BL at pre-dose Day 6Change from BL at pre-dose Day 7Change from BL at FU
MAD Group III397.30.5-4.3-1.3-3.5-7.5-1.8-11.3-4.3-4.30.52.56.0-1.3-1.0-2.3
MAD Group IV384.35.50.5-3.0-0.3-3.82.0-3.8-5.00.52.80.52.5-1.53.04.0
MAD Group V388.57.33.3-6.5-0.8-5.8-7.3-11.0-10.03.310.57.310.87.813.5-0.5
Placebo393.01.7-4.8-2.2-0.33.0-0.50.81.7-4.8-7.5-6.7-5.3-8.2-8.86.7

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MAD: Change From Baseline in ECG Results by Time Point: the Interval That Denotes Depolarization of the Ventricles, Between the Beginning of the Q Wave and the End of the S Wave (QRS Interval)

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. Other ECG recordings will be singlet (one recording of at least 3 complexes) prior to dosing, or around the expected Cmax on Day 1 or 7 for the multiple- dose part. (NCT02544217)
Timeframe: Baseline (pre-dose Day 1), Day1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Follow-up

,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from BL at 2h - Day 1Change from BL at 24h - Day 1Baseline (pre-dose Day 7)Change from BL Day 7 at 1h - Day 7Change from BL Day 7 at 2h - Day 7Change from BL Day 7 at 4hChange from BL Day 7 BL at 6h - Day 7Change from BL Day 7 at 8h - Day 7Change from BL Day 7 at 12h - Day 7Change from BL at pre-dose Day 2Change from BL at pre-dose Day 3Change from BL at pre-dose Day 4Change from BL at pre-dose Day 5Change from BL at pre-dose Day 6Change from BL at pre-dose Day 7Change from BL at FU
MAD Group III99.31.30.399.50.50.50.00.5-3.5-1.50.30.3-0.8-0.8-0.30.30.3
MAD Group IV92.52.02.597.00.01.0-0.5-2.5-0.5-2.02.52.55.02.52.04.50.5
MAD Group V85.56.03.587.55.05.52.53.02.02.03.52.03.52.51.02.0-2.5
Placebo98.5-0.2-0.898.7-0.30.70.70.70.7-2.0-0.8-0.8-0.5-0.5-1.80.2-1.8

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Maximum Concentration (Cmax) of KH176: MAD

Plasma concentrations of KH176 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: pre-dose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionng/mL (Geometric Mean)
Day 1Day 7
Cmax - Dose 200mg313748
Cmax - Dose 400mg13302100
Cmax Dose 100mg184353

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Maximum Concentration (Cmax) of KH183 (Active Metabolite of KH176): MAD Group

Plasma concentrations of KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d.: Cmax was obtained directly from the concentration-time data. (NCT02544217)
Timeframe: Predose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionng/mL (Geometric Mean)
Day 1Day 7
Cmax - Dose 200mg251250
Cmax - Dose 400mg550450
Cmax Dose 100mg99.4152

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Pharmacodynamics of KH176

Change from baseline in biochemistry related to Oxidative Phosphorylation (OXPHOS) (glutathione, lactate); MAD group (NCT02544217)
Timeframe: Day 1, day 7

,,,
Interventionratio GSH/GSSG (Mean)
Ox glutathione (GSH)/Red Glutathati(GSSG) Day 1-0hGSH/GSSG Day 7-0hGSH/GSSG Day 7-3hGSH/GSSG Day 7-6hGSH/GSSG Day 7-12h
MAD Group III87291977910401361
MAD Group IV20831923204521131893
MAD Group V22751918193519931875
Placebo15841694171217181680

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Phospholipidosis

Change from Day 1 to Day 7 in di-docosahexaenoyl (22:6)-bis(monoacylglycerol) phosphate (di-22:6-BMP) and normalized di-22:6-BMP (urine) - MAD (NCT02544217)
Timeframe: Day 1, Day 7

,,,
Interventionng/mL (Mean)
di-22:6-BMP: Change from Day 1 to Day 7Normalized di-22:6-BMP: Change from Day 1 to Day 7
MAD Group III-1.4731.298
MAD Group IV-3.4650.060
MAD Group V-2.6300.337
Placebo-1.5921.780

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Relationship to Study Drug and Severity of Treatment-emergent Adverse Events

(NCT02544217)
Timeframe: 4 months

,,,,,,,,,,,,,
InterventionTEAE (Number)
TEAESerious TEAENot related TEAEUnlikely relatedPossibly relatedRelated
Group I 100mg + Food101000
Group I Placebo504010
Group I Placebo + Food101000
Group II Placebo200200
MAD Group III 200mg901170
MAD Group IV 400mg601140
MAD Group V 800mg1403290
Placebo17031130
SAD Group I 100mg706010
SAD Group I 10mg200200
SAD Group I 800mg000000
SAD Group II 2000mg28000325
SAD Group II 300mg100001
SAD Group II 30mg502300

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SAD: Change From Baseline in ECG Results by Time Point: PQ Interval

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. (NCT02544217)
Timeframe: Pre-dose, Day 1, Day 7

,,,,,,,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline at 1hChange from BL at 2h post doseChange from BL at 4h post doseChange from BL at 6h post doseChange from BL at 8h post doseChange from BLat 12h post doseChange from BL at 24h post doseChange from BL at FU
Group I Placebo + Food177.0-9.0-11.0-5.0-11.0-6.0-9.00.0-16.0
Group II 100mg + Food147.5-3.5-1.0-1.5-1.5-4.0-1.5-2.0-3.5
SAD Group I 100mg155.0-4.0-3.0-3.5-7.5-8.0-6.5-7.0-11.0
SAD Group I 10mg154.5-0.5-3.0-2.0-2.0-6.5-4.0-4.5-5.0
SAD Group I 800mg171.88.88.33.3-3.3-5.3-4.3-4.3-9.8
SAD Group I Placebo195.5-1.21.2-1.5-1.2-3.2-1.8-2.2-5.5
SAD Group II 2000mg176.020.516.010.09.01.00.5-5.5-7.0
SAD Group II 300mg176.54.04.50.0-5.5-8.0-9.5-6.5-3.0
SAD Group II 30mg159.8-1.31.34.80.8-1.3-1.8-4.3-7.3
SAD Group II Placebo165.03.3-0.7-2.3-2.71.0-3.7-3.7-1.3

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SAD: Change From Baseline in ECG Results by Time Point: QRS Interval

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. (NCT02544217)
Timeframe: Pre-dose, Day 1, Day 7

,,,,,,,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline at 1hChange from BL at 2h post doseChange from BL at 4h post doseChange from BL at 6h post doseChange from BL at 8h post doseChange from BL at 12h post doseChange from BL at 24h post doseChange from BL at FU
Group I Placebo + Food95.01.00.00.01.00.00.0-3.0-1.0
Group II 100mg + Food105.50.0-2.0-3.5-1.5-0.5-2.5-1.0-1.5
SAD Group I 100mg106.50.0-2.5-2.0-1.5-2.0-1.5-1.5-2.5
SAD Group I 10mg99.3-1.3-1.3-1.30.81.30.3-1.3-1.3
SAD Group I 800mg104.51.52.52.51.50.02.50.0-3.0
SAD Group I Placebo103.0-0.7-2.0-1.00.3-2.0-0.7-2.7-1.3
SAD Group II 2000mg94.026.020.517.014.513.07.04.0-0.5
SAD Group II 300mg92.53.53.02.03.52.51.01.50.0
SAD Group II 30mg97.80.3-0.3-0.8-0.3-0.8-0.3-2.30.8
SAD Group II Placebo97.01.00.7-0.70.3-1.0-1.7-1.7-0.7

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SAD: Change From Baseline in ECG Results by Time Point: QT Interval

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. (NCT02544217)
Timeframe: Pre-dose, Day 1, Day 7

,,,,,,,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline at 1hChange from BL at 2h post doseChange from BL at 4h post doseChange from BL at 6h post doseChange from BL at 8h post doseChange from BL at 12h post doseChange from BL at 24h post doseChange from BL at FU
Group I Placebo + Food373.0-11.0-2.07.0-14.0-17.0-18.0-3.0-2.0
Group II 100mg + Food396.0-15.516.0-4.0-13.0-9.0-10.0-7.0-1.0
SAD Group I 100mg404.010.59.07.0-3.5-4.0-6.5-4.5-9.0
SAD Group I 10mg393.32.34.83.3-9.8-6.8-2.8-11.8-13.8
SAD Group I 800mg396.3-5.83.3-3.8-19.3-14.8-12.3-10.3-8.3
SAD Group I Placebo400.09.73.09.3-6.7-8.7-8.7-6.7-12.0
SAD Group II 2000mg398.38.84.81.8-4.8-5.3-13.32.3-7.8
SAD Group II 300mg409.0-3.0-2.5-2.0-11.0-16.0-22.5-17.0-12.0
SAD Group II 30mg416.0-8.50.56.0-19.5-18.5-15.5-15.5-12.5
SAD Group II Placebo415.0-4.3-7.3-3.7-16.0-24.0-24.3-23.0-18.3

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SAD: Change From Baseline in ECG Results by Time Point: QTcB Interval

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation the average of the 3 recordings will be taken as baseline. (NCT02544217)
Timeframe: Pre-dose, Day1, Day 7

,,,,,,,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from BL at 1hChange from BL at 2h post doseChange from BL at 4h post doseChange from BL at 6h post doseChange from BL at 8h post doseChange from BL at 12h post doseChange from BL at 24h post doseChange from BL at FU
Group I Placebo + Food367.512.54.59.020.05.017.5-0.59.0
Group II 100mg + Food382.316.010.31.815.55.09.5-2.59.8
SAD Group I 100mg383.8-3.5-10.8-1.50.08.52.83.08.3
SAD Group I 10mg382.0-1.0-4.0-7.311.5-4.8-1.00.04.8
SAD Group I 800mg382.03.09.86.517.88.017.85.3-3.5
SAD Group I Placebo379.31.7-0.55.512.73.07.011.75.3
SAD Group II 2000mg378.539.041.338.541.837.536.015.89.0
SAD Group II 300mg386.31.83.06.014.05.511.51.513.3
SAD Group II 30mg390.5-0.3-6.5-8.34.06.8-2.80.810.8
SAD Group II Placebo385.5-0.7-2.8-1.53.71.23.80.013.0

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SAD: Change From Baseline in ECG Results by Timepoint: Corrected QT Interval According to Fridericia's Formula (QTcF)

The baseline ECG recording consists of a triplicate recording (3 recordings of a least 3 complexes within a 5 minute window) prior to dosing on Day 1. For the evaluation of the corrected QT intervals the average of the 3 recordings will be taken as baseline. Other ECG recordings will be singlet (one recording of at least 3 complexes) prior to dosing. QTcF is calculated as the quotient between the QT interval in milliseconds and the cube root of the RR interval in seconds, according to Fridericia's formula. (NCT02544217)
Timeframe: Baseline, 1, 2, 4, 6, 8, 12, 24 hours, 7 day follow up

,,,,,,,,,
Interventionmsec (Mean)
Baseline (Pre-dose Day 1)Change from baseline (BL)at 1hChange from BL at 2hChange from BL at 4hChange from BL at 6hChange from BL at 8hChange from BL at 12hChange from BL at 24hChange from BL at FU
Group I 100mg + Food386.55.81.80.36.00.53.3-3.86.5
Group I Placebo386.24.00.56.56.2-0.81.85.3-0.3
Group I Placebo + Food369.04.52.58.58.5-2.55.5-1.05.5
Group II Placebo395.0-2.0-4.0-2.2-2.7-7.2-5.2-7.52.8
SAD Group I 100mg390.30.8-4.81.0-1.04.30.00.32.8
SAD Group I 10mg385.8-0.3-1.8-3.84.3-5.5-1.8-4.0-1.3
SAD Group I 800mg386.50.37.83.35.50.88.00.3-5.0
SAD Group II 2000mg385.328.828.526.026.023.319.311.33.3
SAD Group II 300mg393.50.81.53.85.8-1.80.0-4.35.0
SAD Group II 30mg399.3-3.5-4.8-4.3-4.0-1.8-7.3-4.82.8

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Time to Maximum Concentration (Tmax) of KH176 at Day 1, Day 7: MAD Group

Plasma concentrations of KH176 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d. (NCT02544217)
Timeframe: pre-dose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionhours (Geometric Mean)
Day 1Day 7
Tmax - Dose 200mg1.731.86
Tmax - Dose 400mg0.8661.36
Tmax Dose 100mg1.570.931

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Time to Maximum Concentration (Tmax) of KH183 (Active Metabolite of KH176): MAD Group

Plasma concentrations of KH183 were analysed after multiple-dose administration of doses of 100, 200 and 400 mg b.i.d.. tmax was obtained directly from the concentration-time data. (NCT02544217)
Timeframe: Predose at Day 1, 2, 4, 7, and post-dose at Day 1 and Day 7 at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 hours

,,
Interventionhours (Geometric Mean)
Day 1Day 7
Tmax - Dose 200mg1.571.46
Tmax - Dose 400mg1.221.61
Tmax Dose 100mg2.061.19

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