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benzoxazoles

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Description

Benzoxazoles are a class of heterocyclic compounds containing a benzene ring fused to an oxazole ring. They have been extensively studied for their diverse biological activities and applications in various fields, including medicinal chemistry, materials science, and organic electronics.'

1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5. [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]

benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton. [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]

Cross-References

ID SourceID
PubMed CID9228
CHEMBL ID451894
CHEBI ID38814
SCHEMBL ID7903
MeSH IDM0002373

Synonyms (37)

Synonym
benzooxazole
nsc3982
1-oxa-3-azaindene
usaf ek-5017
wln: t56 bn doj
benzoxazole
1-oxa-3-aza-1h-indene
nsc-3982
273-53-0
nsc 3982
ai3-05743
einecs 205-988-9
inchi=1/c7h5no/c1-2-4-7-6(3-1)8-5-9-7/h1-5
1,3-benzoxazole
benzoxazole, 98%
CHEBI:38814 ,
benzoxazoles
B0095
CHEMBL451894
benzo[d]oxazole
AKOS000119993
A3423
j233y1i55i ,
unii-j233y1i55i
A819031
FT-0622739
PS-3680
SCHEMBL7903
5-bromo-4-chloro-3-indolylb-d-
DTXSID8059768
1,3-benzoxazole #
mfcd00005765
CS-W004722
J-016748
Q761111
H10149
EN300-20396

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Safety and tolerability were assessed by monitoring adverse events, extrapyramidal symptoms (EPS), laboratory values, electrocardiograms, prolactin levels, and weight."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" The most common treatment-emergent adverse events (TEAEs) noted with bifeprunox were gastrointestinal; no clear dose-related trend in the incidence of any TEAE was observed in the bifeprunox groups."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" Bifeprunox appeared to be safe and well tolerated by patients in this 6-week study."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.35
" They are known to distribute to many organs of the body, and while some evidence suggests that these nanoparticles are toxic to cells, the mechanism of their toxicity is not clear."( Cationic nanoparticles induce caspase 3-, 7- and 9-mediated cytotoxicity in a human astrocytoma cell line.
Bexiga, MG; Dawson, KA; Fenaroli, F; Lynch, I; Salvati, A; Simpson, JC; Varela, JA; Wang, F, 2011
)
0.37
"The misassembly of soluble proteins into toxic aggregates, including amyloid fibrils, underlies a large number of human degenerative diseases."( AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin.
Alhamadsheh, MM; Baranczak, A; Chan, WK; Connelly, S; Graef, IA; Kelly, JW; Liedtke, M; Park, MS; Penchala, SC; Powers, ET; Rappley, I; Reixach, N; Vogel, H; Wang, Y; Wilson, IA; Witteles, RM; Zhao, L, 2013
)
0.39
" Seven patients (19%) were withdrawn for adverse effects."( Effect on disability and safety of Tafamidis in late onset of Met30 transthyretin familial amyloid polyneuropathy.
Adams, D; Ducot, B; Lacroix, C; Lozeron, P; Mincheva, Z; Théaudin, M, 2013
)
0.39
" There were a total of 19 adverse events, including four febrile urinary tract infections and three severe diarrhoeas, with faecal incontinence in two."( Effect on disability and safety of Tafamidis in late onset of Met30 transthyretin familial amyloid polyneuropathy.
Adams, D; Ducot, B; Lacroix, C; Lozeron, P; Mincheva, Z; Théaudin, M, 2013
)
0.39
" Adverse events were recorded."( Safety, tolerability, and pharmacokinetics of SMT C1100, a 2-arylbenzoxazole utrophin modulator, following single- and multiple-dose administration to healthy male adult volunteers.
Davies, KE; Robinson, N; Tinsley, J, 2015
)
0.42
" Most adverse events (AEs) were mild/moderate, with no discontinuations due to AEs."( Effects of tafamidis treatment on transthyretin (TTR) stabilization, efficacy, and safety in Japanese patients with familial amyloid polyneuropathy (TTR-FAP) with Val30Met and non-Val30Met: A phase III, open-label study.
Ando, Y; Ikeda, S; Machii, K; Misumi, Y; Morita, H; Obayashi, K; Ohta, M; Sekijima, Y; Takata, A; Ueda, M; Yamashita, T, 2016
)
0.43
" Tafamidis proved safe and well-tolerated."( Monitoring effectiveness and safety of Tafamidis in transthyretin amyloidosis in Italy: a longitudinal multicenter study in a non-endemic area.
Bisogni, G; Calabrese, D; Cavallaro, T; Cortese, A; Fabrizi, GM; Gemelli, C; Gentile, L; Grandis, M; Lozza, A; Luigetti, M; Manganelli, F; Mauro, A; Mazzeo, A; Obici, L; Pareyson, D; Perlini, S; Piscosquito, G; Pradotto, LG; Russo, M; Sabatelli, M; Santoro, L; Schenone, A; Stancanelli, C; Vita, G, 2016
)
0.43
" Adverse events (AEs) were monitored throughout the study."( Safety, Tolerability, and Pharmacokinetics of SMT C1100, a 2-Arylbenzoxazole Utrophin Modulator, following Single- and Multiple-Dose Administration to Pediatric Patients with Duchenne Muscular Dystrophy.
Davies, K; Hughes, I; Layton, G; Muntoni, F; Ricotti, V; Robinson, N; Roper, H; Spinty, S; Tejura, B; Tinsley, J, 2016
)
0.43
" The incidence rates of adverse events and adverse drug reactions in K-877 combination therapy groups were comparable to those in statin-monotherapy groups without any noteworthy event in both studies."( Efficacy and safety of K-877, a novel selective peroxisome proliferator-activated receptor α modulator (SPPARMα), in combination with statin treatment: Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia.
Arai, H; Araki, E; Ishibashi, S; Suganami, H; Yamashita, S; Yokote, K, 2017
)
0.46
"Long-term tafamidis was associated with a favourable safety/tolerability profile, without any unexpected adverse events."( Long-term safety and efficacy of tafamidis for the treatment of hereditary transthyretin amyloid polyneuropathy: results up to 6 years.
Amass, L; Barroso, FA; Ebede, B; Judge, DP; Li, H; Stewart, M; Sultan, MB, 2017
)
0.46
"To verify the superiority of pemafibrate over placebo and the non-inferiority of pemafibrate to the maximum dose of fenofibrate for determining the percent change in fasting serum triglyceride (TG) levels and to investigate safety by assessing the incidence of adverse events (AEs) and adverse drug reactions (ADRs)."( Efficacy and Safety of Pemafibrate Versus Fenofibrate in Patients with High Triglyceride and Low HDL Cholesterol Levels: A Multicenter, Placebo-Controlled, Double-Blind, Randomized Trial.
Arai, H; Araki, E; Ishibashi, S; Suganami, H; Yamashita, S; Yokote, K, 2018
)
0.48
"The favorable safety profile of pemafibrate, with fewer adverse effects on kidney/liver-related laboratory tests and fewer AEs/ADRs, including those leading to treatment discontinuation, over fenofibrate 200 mg/day may justify the use of this novel and potent treatment option for reducing TG levels in a broader range of patients."( Efficacy and Safety of Pemafibrate Versus Fenofibrate in Patients with High Triglyceride and Low HDL Cholesterol Levels: A Multicenter, Placebo-Controlled, Double-Blind, Randomized Trial.
Arai, H; Araki, E; Ishibashi, S; Suganami, H; Yamashita, S; Yokote, K, 2018
)
0.48
"Oral LS-102 produced a pharmacokinetic profile different from AGS IV with higher bioavailability, while the toxic tolerance was similar to previous estimates."( Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).
Chen, L; Chen, TB; Ding, LS; Luo, P; Qing, LS; Sun, WX; Zhang, ZF, 2019
)
0.51
" The incidences of adverse events and adverse drug reactions were 82."( Long-Term Efficacy and Safety of Pemafibrate, a Novel Selective Peroxisome Proliferator-Activated Receptor-α Modulator (SPPARMα), in Dyslipidemic Patients with Renal Impairment.
Arai, H; Araki, E; Ishibashi, S; Of The K-Study Group, OB; Suganami, H; Yamashita, S; Yokote, K, 2019
)
0.51
" Data on patient demographic and clinical characteristics and adverse drug reactions (ADRs) were captured using case-report forms."( Characteristics of Patients with Hereditary Transthyretin Amyloidosis and an Evaluation of the Safety of Tafamidis Meglumine in Japan: An Interim Analysis of an All-case Postmarketing Surveillance.
Ando, Y; Hirano, Y; Ishii, T; Matsumoto, N; Sekijima, Y; Takata, A; Ueda, M, 2020
)
0.56
" Incidence of adverse events in both tafamidis doses were comparable to placebo."( Efficacy and safety of tafamidis doses in the Tafamidis in Transthyretin Cardiomyopathy Clinical Trial (ATTR-ACT) and long-term extension study.
Damy, T; Garcia-Pavia, P; Gundapaneni, B; Hanna, M; Judge, DP; Merlini, G; Patterson, TA; Riley, S; Schwartz, JH; Sultan, MB; Witteles, R, 2021
)
0.62
" Pemafibrate was safe and well-tolerated, with only minor increases in serum creatinine and homocysteine concentrations."( Efficacy and Safety of K-877 (Pemafibrate), a Selective PPARα Modulator, in European Patients on Statin Therapy.
Bogdanski, P; Ceska, R; Ginsberg, HN; Hounslow, NJ; Hovingh, GK; Kalina, A; Libis, RA; Senko, Y; Suganami, H; Supryadkina, TV, 2022
)
0.72
" The most frequently reported treatment-emergent adverse events were headache and skin exfoliation."( Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults.
Fernandez, C; Teper, A; Usansky, H; Yoon, E; Zou, J, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters were estimated by the NON-LIN computer programme using the two-compartment open model."( Pharmacokinetic studies with benoxaprofen in man: prediction of steady-state levels from single-dose data.
Chatfield, DH; Smith, GL; Speirs, CF; Tarrant, ME, 1977
)
0.26
" Application of the assay in a pilot pharmacokinetic study showed significant differences between the kinetics of the two enantiomers."( Pharmacokinetic studies with the lipid-regulating agent beclobrate: enantiospecific assay for beclobric acid using a new fluorescent chiral coupling component (S-FLOPA).
Mayer, S; Mutschler, E; Spahn-Langguth, H, 1991
)
0.28
" Pharmacodynamic analysis offered the results that the dose-normalized biophase levels of CZX were coincident with each other when CZX was given at three different doses under ACH anesthesia at the dose of 80 mg/kg."( Influence of alpha-chloralose on muscle relaxant effect of chlorzoxazone in rats and pharmacodynamic analysis.
Fukuda, T; Fukumori, Y; Kaneko, I; Takeuchi, Y, 1989
)
0.28
" The pharmacokinetic parameters show noteworthy similarities in the three species studied: high bioavailability, extensive biotransformations with small urinary excretion of unmodified drug, total clearance between 40 and 50 mL/h/kg, and peak plasma levels of approximately 200 micrograms/mL."( Pharmacokinetics of flunoxaprofen in rats, dogs, and monkeys.
Bianchi, E; Segre, G; Zanolo, G, 1988
)
0.27
"A clinical study on normal volunteers was performed in order to establish the pharmacokinetic pattern of the non-steroidal antiinflammatory drug S-(+)-2-(4-fluorophenyl-a-methyl-5-benzoxazole-acetic acid (flunoxaprofen, Priaxim, FLU) after oral administration or after transcutaneous absorption."( Pharmacokinetic study in man with the non-steroidal antiinflammatory drug flunoxaprofen. Serum concentration-time profile after oral or topical preparations.
Bareggi, SR; De Angelis, M; Pedrazzini, S, 1988
)
0.27
" Pharmacodynamic analysis offered the results that the dose-normalized biophase levels for each dose obtained from the CER method were coincident with each other and that the logarithmic-logistic function was proven to be of use for the pharmacodynamic modeling which could simply assess the bioavailability."( Pharmacodynamics of chlorzoxazone in rats.
Fukuda, T; Fukumori, Y; Kaneko, I; Takeuchi, Y, 1988
)
0.27
" The plasma levels of the drug after oral administration of a solution best fitted a 2-compartment open pharmacokinetic model, whereas the levels after the solid dosage forms more appropriately fitted the simple 1-compartment open model."( Pharmacokinetic studies of benoxaprofen after therapeutic doses with a review of related pharmacokinetic and metabolic studies.
Carmichael, RH; Nash, JF; Ridolfo, AS; Spradlin, CT, 1980
)
0.26
"The pharmacokinetic profile of benoxaprofene, administered in a single oral dose of 600 mg, has been determined comparatively in 5 normal subjects and 15 patients with renal insufficiency (five of whom were on chronic hemodialysis)."( [Benoxaprofene: pharmacokinetic profile in the normal subject and patients with renal insufficiency; evaluation of anticipated serum levels].
Audhuy, B; Brogard, JM; Spach, MO, 1981
)
0.26
" Single doses of 200 mg and 500 mg resulted in an increase in AUC and Cmax that was less than proportional to the increase in dose."( Human pharmacokinetics and tolerability of L-697,639, a non-nucleoside HIV-1 reverse transcriptase inhibitor.
Au, T; De Lepeleire, I; De Schepper, PJ; Depre, M; Laskin, O; Van Hecken, A; Woolf, E; Yeh, KC, 1994
)
0.29
" These findings warrant further evaluation of their properties in an effort to identify valuable alternatives to Ritonavir as pharmacokinetic enhancers."( Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors.
Baumeister, J; Haché, G; Hallenberger, S; Jonckers, TH; Rouan, MC; Sasaki, JC; Schepens, W, 2012
)
0.38
" SMT C1100 was absorbed rapidly following single and multiple oral doses, with median tmax attained within 2-3."( Safety, tolerability, and pharmacokinetics of SMT C1100, a 2-arylbenzoxazole utrophin modulator, following single- and multiple-dose administration to healthy male adult volunteers.
Davies, KE; Robinson, N; Tinsley, J, 2015
)
0.42
" The method was also assessed for its applicability to pharmacokinetic studies in rats."( Development and validation of a liquid chromatography-tandem mass spectrometry method for the assay of tafamidis in rat plasma: Application to a pharmacokinetic study in rats.
Choi, S; Hyun, HC; Jeong, JW; Kim, HR; Kim, YS; Koo, TS; Lee, JH; Oh, JH, 2017
)
0.46
" The objective of this study was to investigate the intestinal absorption, main pharmacokinetic parameters and acute toxicity of LS-102 in rodents compared with AGS IV."( Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).
Chen, L; Chen, TB; Ding, LS; Luo, P; Qing, LS; Sun, WX; Zhang, ZF, 2019
)
0.51
" The plasma concentrations were detected by a validated UHPLC-MS/MS method, and pharmacokinetic parameters were calculated using a compartmental model."( Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).
Chen, L; Chen, TB; Ding, LS; Luo, P; Qing, LS; Sun, WX; Zhang, ZF, 2019
)
0.51
"Oral LS-102 produced a pharmacokinetic profile different from AGS IV with higher bioavailability, while the toxic tolerance was similar to previous estimates."( Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).
Chen, L; Chen, TB; Ding, LS; Luo, P; Qing, LS; Sun, WX; Zhang, ZF, 2019
)
0.51
" These results, in combination with the reported findings in humans, suggest that the metabolite profile of pemafibrate in plasma was different for rats and monkeys, and that monkeys could be a suitable animal model for further pharmacokinetic studies of pemafibrate in humans."( Pharmacokinetics and metabolism of pemafibrate, a novel selective peroxisome proliferator-activated receptor-alpha modulator, in rats and monkeys.
Kawai, H; Ogawa, SI; Tsunenari, Y; Yamazaki, H, 2019
)
0.51
"The objective of this study was to investigate the pharmacokinetic properties of LS-102 after single-dose, oral administration in beagle dogs by developing and validating an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method."( Determination of a astragaloside IV derivative LS-102 in plasma by ultra-performance liquid chromatography-tandem mass spectrometry in dog plasma and its application in a pharmacokinetic study.
Cheng, Y; Ding, LS; He, Y; Luo, P; Qing, LS; Sun, WX; Xie, J; Zhang, ZF, 2019
)
0.51
" The pharmacokinetic profiles of pemafibrate with virtual administrations of P450 inhibitors and/or disease interactions were generated using a physiologically based pharmacokinetic (PBPK) model previously established for co-administration of pemafibrate with OATP1B1 inhibitors."( Modelled plasma concentrations of pemafibrate with co-administered typical cytochrome P450 inhibitors clopidogrel, fluconazole or clarithromycin predicted by physiologically based pharmacokinetic modelling in virtual populations.
Ogawa, SI; Shimizu, M; Yamazaki, H, 2020
)
0.56
" The resulting optimized compound, BAY1217224, has reached first clinical trials, which have confirmed the desired pharmacokinetic properties."( Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Allerheiligen, S; Gericke, KM; Gnoth, M; Heitmeier, S; Hillig, RC; Hillisch, A; Lienau, P; Puetter, V; Roehrig, S; Schaefer, M; Schulz, S; Tersteegen, A, 2020
)
0.56
" The objective of this analysis was to develop a unified population pharmacokinetic (PK) model of tafamidis, which can describe the PK of various different formulations in healthy subjects as well as patients with TTR amyloidosis, and to understand effects of intrinsic and extrinsic factors on the PK variability."( Population pharmacokinetic modelling and simulation of tafamidis in healthy subjects and patients with transthyretin amyloidosis.
Harnisch, L; Huh, Y; Nicholas, T; Riley, S, 2021
)
0.62
" Elimination half-life of brensocatib ranged from 22 to 28 hours, resulting in ≈2-fold accumulation in maximum plasma concentration and area under the plasma concentration-time curve at steady state."( Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults.
Fernandez, C; Teper, A; Usansky, H; Yoon, E; Zou, J, 2022
)
0.72
" A population pharmacokinetic (PPK) model was developed to characterize brensocatib exposure, determine potential relationships between brensocatib exposure and efficacy and safety measures, and inform dose selection in clinical studies."( Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis.
Chalmers, JD; Fernandez, C; Mange, KC; Rubino, CM; Teper, A; Usansky, H; Zou, J, 2022
)
0.72
" A total of 1284 steady-state brensocatib concentrations from 225 individuals were included in the PPK data set; 241 patients with NCFBE from the phase II study were included in the pharmacodynamic (PD) population for the PK/PD analyses."( Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis.
Chalmers, JD; Fernandez, C; Mange, KC; Rubino, CM; Teper, A; Usansky, H; Zou, J, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" However, once dyskinesia has developed, dopamine agonists administered with l-dopa exacerbate involuntary movements."( The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets.
Jackson, MJ; Jenner, P; McCreary, AC; Rose, S; Tayarani-Binazir, K, 2010
)
0.36
"These results strongly support the favourable benefit-to-risk ratio of K-877 add-on therapy in combination with statin treatment."( Efficacy and safety of K-877, a novel selective peroxisome proliferator-activated receptor α modulator (SPPARMα), in combination with statin treatment: Two randomised, double-blind, placebo-controlled clinical trials in patients with dyslipidaemia.
Arai, H; Araki, E; Ishibashi, S; Suganami, H; Yamashita, S; Yokote, K, 2017
)
0.46
"Targeting mammalian target of rapamycin pathways in combination with PD-1 may result in increased antitumor efficacy in cancer patients."( Programmed cell death-1 (PD-1) checkpoint blockade in combination with a mammalian target of rapamycin inhibitor restrains hepatocellular carcinoma growth induced by hepatoma cell-intrinsic PD-1.
Guo, L; Li, H; Li, X; Liu, S; Ye, Q; Zhang, B; Zhang, J, 2017
)
0.46
" Here, we developed a PBPK model of PMF to capture drug-drug interactions (DDI) incurred by cyclosporine (CsA) and rifampicin (RIF), the two OATP1B inhibitors."( Improved Prediction of the Drug-Drug Interactions of Pemafibrate Caused by Cyclosporine A and Rifampicin via PBPK Modeling: Consideration of the Albumin-Mediated Hepatic Uptake of Pemafibrate and Inhibition Constants With Preincubation Against OATP1B.
Lee, W; Morita, S; Park, JE; Sahi, J; Shitara, Y; Sugiyama, Y; Toshimoto, K, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
"1 Benoxaprofen is a new acidic anti-inflammatory compound which was well absorbed after oral administration to man."( Preliminary studies of absorption and excretion of benoxaprofen in man.
Burt, RA; Chatfield, DH; Goulbourn, RA; Smith, GL, 1977
)
0.26
" Benoxaprofen was well absorbed after oral administration of doses of 1 to 10 mg/kg in all six species."( Disposition and metabolism of benoxaprofen in laboratory animals and man.
Chatfield, DH; Green, JN, 1978
)
0.26
"A study of the effect of crystal size on the bioavailability of benoxaprofen, 2-[4-chlorophenyl]-alpha-methyl-5-benzoxazoleacetic acid, in man is reported."( The effect of crystal size on the bioavailability of benoxaprofen: studies utilizing deuterium labeled drug.
Carmichael, RH; Ridolfo, AS; Thompkins, L; Wolen, RL; Ziege, EA, 1979
)
0.26
" This observation suggests metabolic inversion of R(-)- to S(+)-enantiomer, although the possibilities of stereoselective bioavailability or interaction between the two isomers can not be excluded."( Stereospecific disposition of flunoxaprofen enantiomers in human beings.
Forgione, A; Furlanut, M; Montanari, G; Palatini, P; Pedrazzini, S; Perosa, A, 1988
)
0.27
"The bioavailability of a single 300 mg dose of benoxaprofen was compared after rectal and oral administration in 5 subjects."( The pharmacokinetics and acceptability of benoxaprofen following rectal administration.
Glynne, A; Jones, RW; Waugh, AE; Wild, RN; Woodage, TJ, 1980
)
0.26
"We investigated the usefulness and efficiency of the co-grinding method with D-mannitol to improve the bioavailability of a sparingly water-soluble drug, (+/-)-5-[[2-(2-naphthalenylmethyl)-5-benzoxazolyl]methyl]-2, 4-thiazolidinedione (174), and compared it with those of the single-grinding method."( Improvement of dissolution rate and oral bioavailability of a sparingly water-soluble drug, (+/-)-5-[[2-(2-naphthalenylmethyl)-5-benzoxazolyl]-methyl]- 2, 4-thiazolidinedione, in co-ground mixture with D-mannitol.
Kubo, H; Mizobe, M, 1997
)
0.3
" Bioavailability of a suspension formulation in rats was less than 1%, but increased to approximately 9% when administered as a 20% soybean oil-in-water emulsion."( Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor.
Ficorilli, JV; Fogal, SE; Hauss, DJ; Jayaraj, AA; Keirns, JJ; Price, CA; Roy, T, 1998
)
0.3
" Exemplary oral bioavailability in mice was achieved using the indole central scaffold."( Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.
Anaclerio, B; Crysler, C; Dasgupta, M; Eisennagel, S; Lafrance, L; Leonard, KA; Lu, T; Manthey, C; Markotan, T; Marugán, JJ; Tomczuk, B, 2005
)
0.33
"From metabolic considerations and prediction of an inhibitor-induced conformational change, novel adenosine deaminase (ADA) inhibitors with improved activities and oral bioavailability have been developed on the basis of our originally designed non-nucleoside ADA inhibitors."( Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism.
Inoue, T; Kato, T; Kato, Y; Kinoshita, T; Kuno, M; Nakamura, K; Nakanishi, I; Tanaka, K; Terasaka, T; Tsuji, K, 2005
)
0.33
"We have previously reported on a series of aminobenzisoxazoles as potent, selective, and orally bioavailable factor Xa inhibitors, which culminated in the discovery of razaxaban."( Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Bai, S; Fevig, JM; Han, Q; Knabb, RM; Lam, PY; Luettgen, JM; Quan, ML; Wexler, RR; Wong, PC, 2006
)
0.33
" Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse."( 2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.
Anderson, MS; Chen, Y; Eveland, SS; Gonzalez, S; Guo, Q; Hammond, ML; Hunt, JA; Hyland, SA; Kallashi, F; Milot, DP; Pivnichny, JV; Sinclair, PJ; Sparrow, CP; Tong, X; Wright, SD; Xu, SS, 2010
)
0.84
" PF-8380 has adequate oral bioavailability and exposures required for in vivo testing of autotaxin inhibition."( A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
Beltey, K; Bradshaw-Pierce, E; Cortes-Burgos, L; Gierse, J; Hall, T; Johnston, A; Masferrer, J; Murphy, M; Nemirovskiy, O; Ogawa, S; Pegg, L; Pelc, M; Prinsen, M; Schnute, M; Thorarensen, A; Weinberg, R; Wendling, J; Wene, S; Wittwer, A; Zweifel, B, 2010
)
0.36
" Compound 16b showed potent in vivo efficacy against mice Candida infection models and good bioavailability in rats."( Structure-activity relationships of 1,3-benzoxazole-4-carbonitriles as novel antifungal agents with potent in vivo efficacy.
Achiwa, I; Horiuchi, T; Kanai, K; Kawakami, K; Kobayashi, S; Kuroyanagi, J; Nakamura, K; Takeshita, H; Yoshida, K, 2011
)
0.37
" The pharmaceutical properties (LogD, solubility, liver micrsomal stability (t1/2), plasma stability (t1/2), and apparent permeability) strongly suggested that NK-HDAC-1 might be superior to SAHA in bioavailability and in vivo half-life."( Discovery and extensive in vitro evaluations of NK-HDAC-1: a chiral histone deacetylase inhibitor as a promising lead.
Fang, Q; Feng, C; Gu, G; Guo, W; Hou, J; Li, Z; Lin, J; Liu, P; Liu, R; Shen, J; Shi, YK; Tian, Y; Wang, H; Wang, PG; Yin, Z; Zhang, H, 2012
)
0.38
" In vivo PK studies in dogs demonstrate 55% oral bioavailability and an 7 h half-life."( Novel benzoxazole inhibitors of mPGES-1.
Berlioz, F; Demian, D; Hoffmaster, K; Kablaoui, N; Moore, WM; Nugent, RA; Patel, S; Shao, J; Vazquez, ML, 2013
)
0.39
" When dosed as a nasal spray in rabbits, 3 was rapidly absorbed and showed good intranasal bioavailability (42%)."( The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Civiello, RL; Conway, CM; Cook, DA; Davis, CD; Degnan, AP; Dubowchik, GM; Han, X; Jiang, XJ; Macci, R; Macor, JE; Mathias, NR; Moench, P; Pin, SS; Schartman, R; Signor, LJ; Thalody, G; Tora, G; Whiterock, V; Xu, C, 2013
)
0.39
" The oral bioavailability of AG10, combined with additional desirable drug-like features, makes it a very promising candidate to treat TTR amyloid cardiomyopathy."( AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin.
Alhamadsheh, MM; Baranczak, A; Chan, WK; Connelly, S; Graef, IA; Kelly, JW; Liedtke, M; Park, MS; Penchala, SC; Powers, ET; Rappley, I; Reixach, N; Vogel, H; Wang, Y; Wilson, IA; Witteles, RM; Zhao, L, 2013
)
0.39
" Our results identify hepatic uptake as an important determinant of the bioavailability of LPA and bioactive lysophospholipid mimetics and suggest a mechanism to explain changes in circulating LPA levels that have been associated with liver dysfunction in humans."( Mechanism of rapid elimination of lysophosphatidic acid and related lipids from the circulation of mice.
Dong, A; Graf, GA; Morris, AJ; Mueller, P; Panchatcharam, M; Salous, AK; Smyth, SS; Sunkara, M; Wang, Y, 2013
)
0.39
" Liver microsomal clearances and in vivo clearances were moderate in rats and dogs consistent with the moderate bioavailability observed in both species."( Characterization of preclinical in vitro and in vivo ADME properties and prediction of human PK using a physiologically based pharmacokinetic model for YQA-14, a new dopamine D3 receptor antagonist candidate for treatment of drug addiction.
Li, J; Li, Z; Liu, F; Lu, C; Xiong, S; Yang, C; Zhang, Z; Zhuang, X, 2014
)
0.4
"4 nM) and high oral bioavailability (F = 52%, mouse)."( Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors.
Adachi, R; Amano, N; Hidaka, K; Ishii, T; Kamaura, M; Kitazaki, T; Kubo, O; Maki, T; Mochida, T; Morimoto, S; Nakakariya, M; Sato, K; Takahagi, H; Takai, T; Takekawa, S; Yoshikawa, T, 2015
)
0.42
" This clinical study in healthy subjects assessed the relative bioavailability of a TAK-117 tablet compared with a capsule formulation (part 1) and the effect of food (part 2) and intragastric pH modulation (part 3) on TAK-117 pharmacokinetics."( Characterizing the Sources of Pharmacokinetic Variability for TAK-117 (Serabelisib), an Investigational Phosphoinositide 3-Kinase Alpha Inhibitor: A Clinical Biopharmaceutics Study to Inform Development Strategy.
Griffin, C; Patel, CG; Patti, M; Rangachari, L; Shou, Y; Venkatakrishnan, K, 2019
)
0.51
" However, its disappointing clinical application is mainly caused by its very low solubility in biologic fluids, resulting in poor bioavailability after oral administration."( Pharmacokinetics Comparison, Intestinal Absorption and Acute Toxicity Assessment of a Novel Water-Soluble Astragaloside IV Derivative (Astragalosidic Acid, LS-102).
Chen, L; Chen, TB; Ding, LS; Luo, P; Qing, LS; Sun, WX; Zhang, ZF, 2019
)
0.51
" These data indicate that the effects of SB on opioid seeking behavior persist beyond the bioavailability of the compound."( Persistent effects of the orexin-1 receptor antagonist SB-334867 on motivation for the fast acting opioid remifentanil.
Aston-Jones, G; James, MH; Mohammadkhani, A; Pantazis, CB, 2020
)
0.56
" Among substituents, a carboxyl group was identified as key for improving the oral bioavailability in cynomolgus monkeys."( The design, synthesis and evaluation of 2-aminobenzoxazole analogues as potent and orally efficacious ChemR23 inhibitors.
Imaizumi, T; Kobayashi, A; Komai, M; Maemoto, M; Otsubo, N; Otsubo, S; Takada, H, 2020
)
0.56
"Despite extensive research on small molecule thrombin inhibitors for oral application in the past decades, only a single double prodrug with very modest oral bioavailability has reached human therapy as a marketed drug."( Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Allerheiligen, S; Gericke, KM; Gnoth, M; Heitmeier, S; Hillig, RC; Hillisch, A; Lienau, P; Puetter, V; Roehrig, S; Schaefer, M; Schulz, S; Tersteegen, A, 2020
)
0.56
" Cabozantinib, an orally bioavailable multikinase inhibitor is now approved by Food and Drug Administration (FDA) for HCC patients."( Cabozantinib-based combination therapy for the treatment of hepatocellular carcinoma.
Calvisi, DF; Che, L; Chen, X; Cigliano, A; Evert, M; Liang, B; Lu, X; Shang, R; Song, X; Utpatel, K; Wang, J; Wang, P; Xu, M; Zhou, Y, 2021
)
0.62
" However, it is disappointing that the in vivo solubility of astragaloside IV and its bioavailability after oral administration are very low."( The Astragaloside IV Derivative LS-102 Ameliorates Obesity-Related Nephropathy.
Li, Z; Liu, Y; Luo, P; Wu, J; Yang, W; Yang, Y, 2022
)
0.72
" Additionally, we used an in silico model to predict the drug-like properties of them to evaluate their bioavailability to the QikProp Properties Predictions."( Biological activity and ADME/Tox prediction of some 2-substituted benzoxazole derivatives.
Ertan-Bolelli, T; Foto, E; Yildiz, I; Zilifdar Foto, F, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" 4 The pharmacokinetic parameters were used to predict steady state plasma levels for various dosage regimens."( Pharmacokinetic studies with benoxaprofen in man: prediction of steady-state levels from single-dose data.
Chatfield, DH; Smith, GL; Speirs, CF; Tarrant, ME, 1977
)
0.26
" 3 Multiple dosing with 25 and 50 mg every 24 h achieved an equilibrium conentration in the plasma after 6-8 days, while dosing with 100 mg every 12 h enabled equilibrium to be reached in 3-6 days."( Preliminary studies of absorption and excretion of benoxaprofen in man.
Burt, RA; Chatfield, DH; Goulbourn, RA; Smith, GL, 1977
)
0.26
"A single daily dose of 600 mg of henoxaprofen has been shown to be more effective than a previously reported dosage regime in patients with rheumatoid arthritis."( Treatment of rheumatoid arthritis with a single daily dose of benoxaprofen.
Huskisson, EC; Scott, J, 1979
)
0.26
" The method also was applicable to chlorzoxazone analysis in a commercial dosage form containing acetaminophen."( Fluorometric determination of chlorzoxazone in tablets and biological fluids.
Chan, CW; Stewart, JT, 1979
)
0.26
" The results obtained in the rat show that S(+)-flunoxaprofen serum levels following the administration of a single oral dose of flunoxaprofen reach about the same values (between 24 and 30 micrograms/ml at 18 h) whichever form was dosed (i."( Stereochemical pharmacokinetics of the 2-arylpropionic acid non-steroidal antiinflammatory drug flunoxaprofen in rats and in man.
De Angelis, M; Forgione, A; Muciaccia, WZ; Pedrazzini, S; Sacchi, C, 1988
)
0.27
" The non-steroid antirheumatic benoxaprofen was used alone in a dosage of a 1 x 600 mg tablet daily."( [Benoxaprofen in the treatment of spondylosis and spondylarthrosis (author's transl)].
Hevelke, G; Schilling, E, 1981
)
0.26
" The plasma levels of the drug after oral administration of a solution best fitted a 2-compartment open pharmacokinetic model, whereas the levels after the solid dosage forms more appropriately fitted the simple 1-compartment open model."( Pharmacokinetic studies of benoxaprofen after therapeutic doses with a review of related pharmacokinetic and metabolic studies.
Carmichael, RH; Nash, JF; Ridolfo, AS; Spradlin, CT, 1980
)
0.26
" Computerized thermography showed that, at a dosage of 600 mg daily, benoxaprofen had a significant antiinflammatory effect; this observation was confirmed by the comparison with indomethacin."( Benoxaprofen--dose-range studies using quantitative thermography.
Bacon, PA; Davies, J; Ring, FJ, 1980
)
0.26
" It appears advisable to reduce the dosage by half only in patients with a Cr clearance of less than 10-20 ml/min/1."( [Benoxaprofene: pharmacokinetic profile in the normal subject and patients with renal insufficiency; evaluation of anticipated serum levels].
Audhuy, B; Brogard, JM; Spach, MO, 1981
)
0.26
" The parent molecule 5a shows potent inhibitory activity in vitro in the nanomolar range against a panel of human breast cancer cell lines, but is inactive (IC50 > 30 microM) against other cell types: activity against the sensitive breast lines MCF-7 and MDA 468 is characterized by a biphasic dose-response relationship."( Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo.
Bradshaw, TD; Fichtner, I; Lelieveld, P; McCall, CJ; Shi, DF; Stevens, MF; Wrigley, S, 1996
)
0.29
" These results indicate that the induction of hyperdiploidy/polyploidy with DES and E2 show sublinear dose-response relationships with likely threshold concentrations in human lymphocytes and that FISH with multiple probes targeting different chromosomes can be used to estimate hyperdiploidy and polyploidy frequencies."( Dose-response studies of the induction of hyperdiploidy and polyploidy by diethylstilbestrol and 17beta-estradiol in cultured human lymphocytes using multicolor fluorescence in situ hybridization.
Eastmond, DA; Hasegawa, L; Metzler, M; Parks, R; Schuler, M, 1998
)
0.3
" To further our understanding of these processes and to discriminate between different PPAR mediated signalling pathways, a proteomic approach has been undertaken to identify changes in protein expression patterns in Sprague Dawley rat liver following dosing with a PPARalpha agonist (Wyeth 14643), a PPARgamma agonist (Troglitazone) and a compound with mixed PPARalpha/gamma agonist activity (SB-219994)."( Protein expression changes in the Sprague Dawley rat liver proteome following administration of peroxisome proliferator activated receptor alpha and gamma ligands.
Bryant, D; Bugelski, P; Camilleri, P; Cutler, P; Hayes, W; Holbrook, JD; Kramer, K; Lord, PG; Man, WJ; White, IR; Wood, J, 2003
)
0.32
" In a dose-response experiment, increases in SPA were correlated with dose of orexin A linearly up to 2 nmol."( Orexin A (hypocretin 1) injected into hypothalamic paraventricular nucleus and spontaneous physical activity in rats.
Kiwaki, K; Kotz, CM; Lanningham-Foster, L; Levine, JA; Wang, C, 2004
)
0.32
" We developed a fast and reliable laboratory screening bioassay for grain crops that includes dose-response considerations as an integral part of the experimental design."( A novel laboratory screening bioassay for crop seedling allelopathy.
Belz, RG; Hurle, K, 2004
)
0.32
" Overall, current data support the hypothesis that a persistent anorectic action contributes to the significant loss of bodyweight observed 24 h following acute dosing with SB-334867."( Anorexia and weight loss in male rats 24 h following single dose treatment with orexin-1 receptor antagonist SB-334867.
Blundell, JE; Halford, JC; Ishii, Y; Jeffrey, P; Johns, A; Porter, R; Rodgers, RJ; Summerfield, S; Upton, N, 2005
)
0.33
" ED50 doses of the pure compounds were estimated in dose-response experiments in Petri dishes, and these turned out to be much higher than the predicted maximum concentrations of DIMBOA, MBOA, and BOA in the soil water following incorporation."( Herbicidal effects of soil-incorporated wheat.
Kudsk, P; Mathiassen, SK; Mogensen, BB, 2006
)
0.33
" The specific inhibitor PF-8380, dosed orally at 30 mg/kg, provided >95% reduction in both plasma and air pouch LPA within 3 h, indicating autotaxin is a major source of LPA during inflammation."( A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
Beltey, K; Bradshaw-Pierce, E; Cortes-Burgos, L; Gierse, J; Hall, T; Johnston, A; Masferrer, J; Murphy, M; Nemirovskiy, O; Ogawa, S; Pegg, L; Pelc, M; Prinsen, M; Schnute, M; Thorarensen, A; Weinberg, R; Wendling, J; Wene, S; Wittwer, A; Zweifel, B, 2010
)
0.36
" Behavioral studies conducted in male, Swiss Webster mice, intraperitoneal or oral dosing with SN79 prior to a convulsive or locomotor stimulant dose of cocaine led to a significant attenuation of cocaine-induced convulsions and locomotor activity."( Synthesis and pharmacological evaluation of 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a cocaine antagonist, in rodents.
Avery, BA; Kaushal, N; Matsumoto, RR; McCurdy, CR; Narayanan, S; Robson, MJ; Vinnakota, H, 2011
)
0.37
" As repeated drug dosing can have differential effects and is more clinically relevant than acute dosing, in the current study we examined the effects of repeated SB-334867 on cocaine self-administration, extinction, and reinstatement to cocaine seeking in Sprague-Dawley rats."( Repeated orexin 1 receptor antagonism effects on cocaine seeking in rats.
Aston-Jones, G; Do, PH; See, RE; Smith, RJ; Zhou, L, 2012
)
0.38
" We tested SB 334867 in three doses (10, 20 and 30 mg/kg), TCS-OX2-29 in two doses (5 and 10 mg/kg) and morphine with highest effective dose based on our dose-response experiment (5 mg/kg)."( The differential effects of OX1R and OX2R selective antagonists on morphine conditioned place preference in naïve versus morphine-dependent mice.
Dehpour, AR; Esmaeili, B; Ghaffarpour, M; Javadi-Paydar, M; Mirbaha, H; Motiei-Langroudi, R; Tabaeizadeh, M; Tahsili-Fahadan, P, 2013
)
0.39
" In a syngeneic mouse model of lymphoid BCR-ABL+ disease, daily oral dosing of MLN0128 rapidly cleared leukemic outgrowth."( Efficacy of the investigational mTOR kinase inhibitor MLN0128/INK128 in models of B-cell acute lymphoblastic leukemia.
Fruman, DA; Janes, MR; Jessen, KA; Li, LS; Lilly, MB; Limon, JJ; Liu, Y; Mallya, S; Martin, MB; Ren, P; Rommel, C; Sender, LS; Shieh, MP; Vu, C, 2013
)
0.39
" Oral dosing in each of the three treatment periods was separated by a washout period of  ≥ 14 days."( The effect of tafamidis on the QTc interval in healthy subjects.
Klamerus, KJ; Moller, R; Riley, S; Wang, R; Watsky, E, 2015
)
0.42
" Systemic exposure reduced upon repeat dosing with steady-state concentrations achieved within 3-5 days of multiple bid dosing."( Safety, tolerability, and pharmacokinetics of SMT C1100, a 2-arylbenzoxazole utrophin modulator, following single- and multiple-dose administration to healthy male adult volunteers.
Davies, KE; Robinson, N; Tinsley, J, 2015
)
0.42
" A dosage (25 mg/kg) was chosen to explore the neuroprotective mechanisms of salviaolate."( Salviaolate Protects Rat Brain from Ischemia-Reperfusion Injury through Inhibition of NADPH Oxidase.
Liu, B; Lou, Z; Luo, XJ; Ma, QL; Peng, J; Peng, JJ; Ren, KD; Ren, X; Tan, B; Yang, J; Yang, ZB, 2015
)
0.42
"TAK-228 pharmacokinetics exhibited dose-dependent increase in exposure when dosed with paclitaxel and no apparent differences when administered with or 24 h after paclitaxel."( TAK-228 (formerly MLN0128), an investigational dual TORC1/2 inhibitor plus paclitaxel, with/without trastuzumab, in patients with advanced solid malignancies.
Burris, HA; Hart, L; Infante, JR; Jones, SF; Kurkjian, CD; Murphy, PB; Neuwirth, R; Pant, S; Patel, CG; Zohren, F, 2017
)
0.46
" An alternative single solid oral dosage formulation (tafamidis 61-mg free acid capsules) was developed and introduced for patient convenience (approved in the United States, United Arab Emirates, and European Union)."( The Bioequivalence of Tafamidis 61-mg Free Acid Capsules and Tafamidis Meglumine 4 × 20-mg Capsules in Healthy Volunteers.
Le, VH; Lockwood, PA; O'Gorman, MT; Patterson, TA; Riley, S; Sultan, MB; Tankisheva, E; Wang, Q, 2020
)
0.56
"An efficient, accurate and sensitive spectrofluorimetric method was developed for analysis of empagliflozin (EGF) in pure form, dosage form and human plasma."( New spectrofluorimetric analysis of empagliflozin in its tablets and human plasma using two level full factorial design.
Abdel Hamid, MA; Ahmed, HM; Batakoushy, HA; Omar, MA, 2020
)
0.56
" Hence, although HSP90 inhibitors show strong inhibition of TSC1/TSC2 null cell line growth in vitro, ganetespib showed little benefit at standard dosage in vivo."( Evaluation of Hsp90 and mTOR inhibitors as potential drugs for the treatment of TSC1/TSC2 deficient cancer.
Bajaj, V; Guo, Y; Kwiatkowski, DJ; Malinowska, IA; Mrozek, EM; Zhang, J, 2021
)
0.62
" This approach was effectively employed to evaluate the content of 6-aminocaproic acid in laboratory prepared dosage form with average percentage recovery of 100."( Benzofurazan -based fluorophore for the spectrofluorimetric determination of 6-Aminocaproic acid: Application to spiked human plasma and urine.
Anwer, EF; Derayea, SM; Nour El-Deen, DAM; Omar, MA, 2022
)
0.72
" A traditional 3 + 3 dose escalation design with 5 dosing cohorts was used."( Phase I dose escalation study of dual PI3K/mTOR inhibition by Sapanisertib and Serabelisib in combination with paclitaxel in patients with advanced solid tumors.
Meissner, T; Rojas-Espaillat, L; Starks, DC; Williams, CB, 2022
)
0.72
" On the other hand, a non-significant dosage of orexin-1 reversed the antidepressant effect of citalopram in the normal and REM sleep-deprived animals."( Synergistic antidepressant effects of citalopram and SB-334867 in the REM sleep-deprived mice: Possible role of BDNF.
Alibeik, H; Bananej, M; Khakpai, F; Saadati, N; Zarrindast, MR, 2022
)
0.72
"Tafamidis meglumine (Vyndaqel) can be dosed at 20 or 80 mg QD."( Tafamidis concentration required for transthyretin stabilisation in cerebrospinal fluid.
Coelho, T; Jaeger, M; Kelly, JW; Powers, ET; Tsai, FJ, 2023
)
0.91
"Tafamidis stabilises TTR in CSF to what is likely a clinically meaningful extent at CSF concentrations achieved by the normal tafamidis dosing regimen."( Tafamidis concentration required for transthyretin stabilisation in cerebrospinal fluid.
Coelho, T; Jaeger, M; Kelly, JW; Powers, ET; Tsai, FJ, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
mancude organic heterobicyclic parent
1,3-benzoxazolesCompounds based on a fused 1,3-oxazole and benzene bicyclic ring skeleton.
[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]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID343680Hexadecane-water distribution coefficient, log D at pH 7.4 by shake-flask technique2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Toward prediction of alkane/water partition coefficients.
AID1887063Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis.
AID1887064Cytotoxicity against human NCI-H522 cells assessed as reduction in cell viability incubated for 3 days by methylene blue staining based analysis2022Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17
Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis.
AID343398Octanol-water distribution coefficient, log D at pH 7.4 by shake-flask technique2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Toward prediction of alkane/water partition coefficients.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,565)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990342 (13.33)18.7374
1990's199 (7.76)18.2507
2000's538 (20.97)29.6817
2010's1141 (44.48)24.3611
2020's345 (13.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.23

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index43.23 (24.57)
Research Supply Index7.92 (2.92)
Research Growth Index4.95 (4.65)
Search Engine Demand Index70.01 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (43.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials100 (3.77%)5.53%
Reviews112 (4.22%)6.00%
Case Studies35 (1.32%)4.05%
Observational7 (0.26%)0.25%
Other2,397 (90.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]