Page last updated: 2024-11-13

chiniofon

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

Description

Hydroxyquinolines: The 8-hydroxy derivatives inhibit various enzymes and their halogenated derivatives, though neurotoxic, are used as topical anti-infective agents, among other uses. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23696930
MeSH IDM0010782

Synonyms (12)

Synonym
hydroxyquinolines
chiniofonum
quiniofon
chiniofonum [inn-latin]
chiniofone [dcit]
98f8y85b6w ,
quiniofon [inn-spanish]
chiniofone
unii-98f8y85b6w
nsc 758879
chiniofon [inn:dcf:nf]
8002-90-2

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In 6 feedlot trials with 1993 cattle in 5 geographic areas, decoquinate fed at this level for 90-120 days had no adverse effects."( Bovine coccidiosis. A review, including field safety studies with decoquinate for prevention.
Fox, JE, 1978
)
0.26
" These findings bring further support to the hypothesis that the toxic and genotoxic effects of benzene are produced by several metabolites acting synergistically."( Genotoxicity of two metabolites of benzene: phenol and hydroquinone show strong synergistic effects in vivo.
Barale, R; Barrai, I; Betti, C; Loprieno, N; Marrazzini, A; Vangelisti, V, 1990
)
0.28
" Adverse effects were mild and did not affect treatment."( A study on the neurotoxicity of broxyquinoline and brobenzoxaldine combination in therapeutic doses.
Bapna, JS; Bosco, B; Chandrasekar, S; Das, AK; Swain, R; Swaminathan, RP; Thombre, DP; Veliath, S, 1986
)
0.27
"The preparation is given of an 111indium-oxine complex that is non toxic and can label reproductively various types of cells."( Measurements of cell-mediated cytotoxicity on target cells labelled with the indium-111-oxine complex.
Czichosz, R; Firket, H; Guillaume, M; Schaaf-Lafontaine, N; Smet-Donnay, M, 1985
)
0.27
"Significant difference in oral LD50 of chinoform in mice was observed between strains C57BL/6 and C3H/He."( Inhibition of gastric emptying by chinoform and its relation to strain differences in acute toxicity of chinoform in mice.
Horiguchi, Y; Takeda, Y; Tohyama, K, 1983
)
0.27
"In all four dose steps, only one adverse event (25 mg; mild skin rash) was considered drug related."( Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein.
Boettcher, MF; Gelfert-Peukert, S; Heinig, R; Kohlsdorfer, C; Ludwig, M; Schaefer, A; Schmeck, C; Weber, O; Wensing, G, 2012
)
0.38
"BAY 60-5521 was clinically safe and well tolerated."( Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein.
Boettcher, MF; Gelfert-Peukert, S; Heinig, R; Kohlsdorfer, C; Ludwig, M; Schaefer, A; Schmeck, C; Weber, O; Wensing, G, 2012
)
0.38
" If formed in vivo, ABAQ may give rise to adverse genotoxic effects."( In vivo genotoxicity of a novel heterocyclic amine, aminobenzoazepinoquinolinone-derivative (ABAQ), produced by the Maillard reaction between glucose and l-tryptophan.
Coulibaly, S; Hasei, T; Kobayashi, S; Nakagama, H; Nishizaki, M; Okazaki, M; Totsuka, Y; Wakabayashi, K; Watanabe, T, 2014
)
0.4
" We found that iOWH032 was generally safe and achieved a mean (± standard deviation) plasma level of 4,270 ng/mL (±2,170) after 3 days of oral dosing."( A Phase 2a randomized, single-center, double-blind, placebo-controlled study to evaluate the safety and preliminary efficacy of oral iOWH032 against cholera diarrhea in a controlled human infection model.
Al-Ibrahim, M; Ambler, G; Chen, WH; Choy, RKM; de Hostos, EL; Dong, SD; Erdem, R; Fraczek, K; Gast, C; Mercer, LD; Raine, M; Tennant, SM, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties."( Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.
Bedard, PW; Clerin, V; Di, L; Huang, A; Janz, K; Kaila, N; Keith, JC; Lowe, M; Moretto, A; Schaub, RG; Shaw, GD; Sushkova, N; Tam, S; Tchernychev, B; Tsao, DH; Wang, Q, 2010
)
0.36
"A combination of allometric scaling of the pharmacokinetics of the CETP-inhibitor BAY 60-5521 with pharmacodynamic studies in CETP-transgenic mice and in human plasma with physiologically-based pharmacokinetic (PBPK) modelling was used to support the selection of the first-in-man dose."( Prediction of a potentially effective dose in humans for BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling.
Bischoff, H; Buehner, K; Hafner, FT; Heinig, R; Li, V; Lustig, K; Schmeck, C; Vakalopoulos, A; Weber, O; Willmann, S, 2012
)
0.38
" A clear pharmacodynamic effect on CETP inhibition and HDL could be demonstrated."( Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein.
Boettcher, MF; Gelfert-Peukert, S; Heinig, R; Kohlsdorfer, C; Ludwig, M; Schaefer, A; Schmeck, C; Weber, O; Wensing, G, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
" aureus but did not show synergy when combined with nafcillin, vancomycin, or rifampin."( Antibacterial activity of coumermycin alone and in combination with other antibiotics.
Chin, NX; Labthavikul, P; Neu, HC, 1984
)
0.27
" Our study suggests that treatment aimed at abrogation of autoimmunity combined with expansion of beta-cell mass constitutes a potential therapeutic approach for treatment of insulin-dependent diabetes mellitus."( Amelioration of diabetes in nonobese diabetic mice with advanced disease by linomide-induced immunoregulation combined with Reg protein treatment.
Clark, A; Gross, DJ; Okamoto, H; Reibstein, I; Slavin, S; van den Brand, J; Weiss, L, 1998
)
0.3
"To investigate the association between vasculopathy and survival during experimental cerebral malaria (ECM), and to determine whether targeting the endothelin-1 (ET-1) pathway alone or in combination with the anti-malaria drug artemether (a semi-synthetic derivative of artemisinin) will improve microvascular hemorrhage and survival."( The novel ETA receptor antagonist HJP-272 prevents cerebral microvascular hemorrhage in cerebral malaria and synergistically improves survival in combination with an artemisinin derivative.
Bruno, FP; Dai, M; Desruisseaux, MS; Freeman, B; Reznik, SE; Shikani, HJ; Stephani, RA; Tanowitz, HB; Weiss, LM, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
" The bioavailability (AUC) of 1 in dogs from capsules containing 2 was also higher than that from PEG 1000-based capsules."( Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions.
Augustine, MA; Bernstein, DF; Mufson, D; Serajuddin, AT; Sheen, PC, 1988
)
0.27
" Pharmacokinetic studies in the dog demonstrated that the compound was well absorbed; the bioavailability was 36% of the dose of 1 mg/kg."( Metabolism of 14C-iodochlorhydroxyquin in the dog and the rat.
Inaba, T; Jurima, M; Kalow, W, 1984
)
0.27
" But the higher bioavailability of zinc in human milk should not only be attributed to the presence of citrate."( [Effect of different concentrations of various zinc complexes (picolinate, citrate, 8-hydroxyquinolate) in comparison with sulfate on zinc supply status in rats].
Kirchgessner, M; Roth, HP, 1983
)
0.27
"In order to investigate the bioavailability and the rate-limiting step of the absorption of roquinimex, an oral solution and a tablet formulation (Linomide(R)) were given to healthy volunteers."( Dissolution rate-limited absorption and complete bioavailability of roquinimex in man.
Gunnarsson, PO; Höglund, P; Nordle, O; Polacek, J; Strandgârden, K; Wännman, H, 1999
)
0.3
" In our study, we explored the role of combinations of hydrophobic ionogenic organic compounds (HIOCs) with copper (Cu2+)for uptake and bioavailability of metals and hydrophobic metal complexes in an in vitro membrane system."( The evaluation of liposome-water partitioning of 8-hydroxyquinolines and their copper complexes.
Escher, BI; Kaiser, SM, 2006
)
0.33
" However, its oral bioavailability was low."( Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.
Bedard, PW; Clerin, V; Di, L; Huang, A; Janz, K; Kaila, N; Keith, JC; Lowe, M; Moretto, A; Schaub, RG; Shaw, GD; Sushkova, N; Tam, S; Tchernychev, B; Tsao, DH; Wang, Q, 2010
)
0.36
" In an attempt to improve the bioavailability and the stability of four of these derivatives, we propose here two different approaches: complexation with β-cyclodextrin derivatives and incorporation of these substances inside antioxidant micelles."( Overcoming instability and low solubility of new cytostatic compounds: a comparison of two approaches.
Bauer-Brandl, A; di Cagno, M; Hlaváč, J; Skalko-Basnet, N; Stein, PC; Styskala, J, 2012
)
0.38

Dosage Studied

ExcerptRelevanceReference
"3 Dose-response curves to the four drugs for tracheal relaxation were almost parallel."( Assessment of the selectivity of OPC-2009, a new beta2-adrenoceptor stimulatn, by the use of the blood-perfused trachea in situ and of the isolated blood-perfused papillary muscle of the dog.
Himori, N; Taira, N, 1977
)
0.26
" The slopes of the salbutamol dose-response curves were flatter than those for isoprenaline and noradrenaline; the slopes of the procaterol dose-response curves were flatter than those for salbutamol."( Comparative study of chronotropic and inotropic responses to 5-(-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrade (procaterol), salbutamol, noradrenaline and isoprenaline in the dog heart.
Chiba, S,
)
0.13
"Clinically used dosage regimen of nitroxoline, three times 100 mg daily, was proved to be inappropriate because the successfulness of medical treatment was rarely sufficient."( Appropriate nitroxoline dosage regimen design.
Bremsak, F; Karba, R; Kozjek, F; Mrhar, A, 1979
)
0.26
" Quinoline did, however, induce a potent mitogenic response in the rat liver between 24 and 48 hr after oral dosing of 200-500 mg/kg."( Quinoline: unscheduled DNA synthesis and mitogenesis data from the rat liver in vivo.
Ashby, J; Bandara, L; Lefevre, PA; Mohammed, R, 1989
)
0.28
" There was no ideal "gold standard" to which our imaging results could be compared, but we used a combination of biopsy findings, clinical impressions, and changes in renal function after pulsing with steroids and/or decreasing CYS dosage as the basis for our diagnoses."( Evaluation of the utility of indium-111 oxine platelet imaging in renal transplant patients on cyclosporine.
Darcourt, J; Koyle, MA; Marcus, CS; Vivian, M, 1986
)
0.27
" The use of 99Tcm is scintigraphically more advantageous and, with the dosage required, the absorbed radiation dose to the red bone marrow is three times lower than with 111In granulocytes."( 99Tcm-labelled HSA-nanocolloid versus 111In oxine-labelled granulocytes in detecting skeletal septic process.
de Schrijver, M; Fridrich, R; Streule, K, 1988
)
0.27
"The physicochemical properties of the base and hydrochloride salt of the poorly water-soluble drug alpha-pentyl-3-(2-quinolinylmethoxy) benzenemethanol (REV 5901) were investigated in order to select an appropriate form of the drug for dosage form development."( Preformulation study of a poorly water-soluble drug, alpha-pentyl-3-(2-quinolinylmethoxy)benzenemethanol: selection of the base for dosage form design.
Augustine, MA; Bernstein, DF; Mufson, D; Serajuddin, AT; Sheen, PC, 1986
)
0.27
" Dose-response curves were generated using such proinflammatory materials as formyl-methionyl-leucyl-phenylalanine, lipopolysaccharide, activated serum, trypsin, glycogen, and acetic acid."( Labeling of peripheral blood polymorphonuclear leukocytes with indium-111: a new method for the quantitation of in-vivo accumulation of PMNLs in rabbit skin.
Barnes, B; Lazarus, GS; Wahba, AV, 1984
)
0.27
" Dose-response analysis demonstrated that a Linomide blood level of 50-100 microM is optimal for such chemoprevention."( Antiangiogenic treatment with linomide as chemoprevention for prostate, seminal vesicle, and breast carcinogenesis in rodents.
Isaacs, JT; Joseph, IB; Vukanovic, J, 1996
)
0.29
" In spite of selection of favourable prognosis patients and an optimal daily dosing schedule, linomide was not an effective treatment in renal cell carcinoma."( EORTC phase II study of daily oral linomide in metastatic renal cell carcinoma patients with good prognostic factors.
de Mulder, PH; de Wit, R; Fosså, SD; Paridaens, R; Pawinsky, A; Stoter, G; Svedberg, A; van Oosterom, AT, 1997
)
0.3
"L-W rats with small induced P-SV tumors were treated with a recommended dosage of linomide (100 mg/kg BW/day) by the intraperitoneal and oral routes."( Effects of linomide on advanced prostate-seminal vesicle cancers in Lobund-Wistar rats.
Pollard, M, 1998
)
0.3
" The dosage of linomide used showed evidence of toxicity."( Effects of linomide on advanced prostate-seminal vesicle cancers in Lobund-Wistar rats.
Pollard, M, 1998
)
0.3
" DCITC attenuated the maximal (-)-isoprenaline-mediated relaxation of a phenylephrine contracted aorta in a concentration-dependent manner and shifted the dose-response curves for (-)-isoprenaline to the right."( Irreversible binding of a carbostyril-based agonist and antagonist to the beta-adrenoceptor in DDT1 MF-2 cells and rat aorta.
Baker, SP; Dennis, DM; Deyrup, MD; Gelband, CH; Greco, PG; Otero, DH, 1998
)
0.3
" Furthermore, bropirimine was most efficacious when dosing was begun 5-10 days after injection of myelin basic protein, the protein isolated from the central nervous system and used for inducing EAE in our model."( Pharmacology of the biological response modifier bropirimine (PNU-54461) on experimental autoimmune encephalomyelitis (EAE) in mice.
Brideau, RJ; Buxser, SE; Chapman, DL; Decker, DE; Dunn, CJ; Galinet, LA; Ready, KA; Vroegop, SM, 1999
)
0.3
" The duration and dosage of Linomide required to obtain these effects is similar to those required for EAE inhibition."( Inhibition of autoimmune disease by the immunomodulator linomide correlates with the ability to activate macrophages.
Andersson, M; Björk, A; Brunmark, C; Dahlén, E; Dawe, K; Hedlund, G; Tellander, AC, 2000
)
0.31
" The activity of each of the three compounds increased in a dose-response manner."( Lytic activity of l-menthol derivatives against the snow blight disease fungus, Micronectriella nivalis.
Hyakumachi, M; Kawazoe, H; Miyazawa, M; Sumi, Y, 2003
)
0.32
", 30- to 60-fold more potent than linomide) in these assays and its lack of a proinflammation in the Beagle-dog, ABR-215050 (tasquinimod), Figure 1, was characterized for dose-response ability to inhibit the growth of a series of four additional human and rodent prostate cancer models in mice."( Identification of ABR-215050 as lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer.
Björk, A; Dalrymple, SL; Garrison, JB; Isaacs, JT; Kyprianou, N; Leanderson, T; Olsson, A; Pili, R; Qian, DZ, 2006
)
0.33
" The applicability of the method was demonstrated by successful determination of AZD1152 and hQPA in human plasma and in plasma, brain, liver, kidney and ileum samples from mice dosed with AZD1152."( Simultaneous determination of AZD1152 (prodrug) and AZD1152-hydroxyquinazoline pyrazol anilide by reversed phase liquid chromatography.
Beijnen, JH; Pluim, D; Schellens, JH; van Tellingen, O, 2009
)
0.35
" A high content of Al(30) nanoclusters in PACl improves the removal efficiency over broader dosage and pH range."( Polyaluminum chloride with high Al30 content as removal agent for arsenic-contaminated well water.
Casentini, B; Furrer, G; Masion, A; Mertens, J; Pöthig, R; Wehrli, B, 2012
)
0.38
"Ferron dosage ([Ferron]) is key to ferron-timed spectrophotometry (ferron assay)."( An important improvement in Ferron-timed spectrophotometry.
Chang, F; Ren, Y; Shi, Q; Zhang, J, 2013
)
0.39
"8, but display excellent solubility at low pH, suggesting that oral dosing may be possible."( Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
Barlow, DJ; Benoni, G; Bompiani, KM; Caglič, D; Dickerson, TJ; Houseknecht, KL; Krutein, MC; Lairson, LL; Pelletier, JC; Reitz, AB; Smith, GR, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,742)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990865 (49.66)18.7374
1990's251 (14.41)18.2507
2000's258 (14.81)29.6817
2010's291 (16.70)24.3611
2020's77 (4.42)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials51 (2.80%)5.53%
Reviews69 (3.78%)6.00%
Case Studies72 (3.95%)4.05%
Observational1 (0.05%)0.25%
Other1,630 (89.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]