Page last updated: 2024-12-06

timegadine

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

Description

timegadine: first source states that SR 1368 is synonym for cpd; SR 1368 is a different cpd in Chemline; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68902
CHEMBL ID276368
SCHEMBL ID187366
MeSH IDM0092840

Synonyms (29)

Synonym
71079-19-1
sr-1368
timegadine
1-cyclohexyl-2-(2-methyl-4-quinolyl)-3-(2-thiazolyl)guanidine
guanidine, n-cyclohexyl-n'-(2-methyl-4-quinolinyl)-n''-2-thiazolyl-
timegadina [inn-spanish]
brn 5619706
timegadine [inn]
n-cyclohexyl-n'-(2-methyl-4-quinolinyl)-n''-2-thiazolylguanidine
timegadinum [inn-latin]
einecs 275-184-0
guanidine, 1-cyclohexyl-2-(2-methyl-4-quinolyl)-3-(2-thiazolyl)-
CHEMBL276368
2-cyclohexyl-1-(2-methylquinolin-4-yl)-3-(1,3-thiazol-2-yl)guanidine
A23740
1xr74j44ul ,
unii-1xr74j44ul
timegadinum
timegadina
SCHEMBL187366
timegadine [who-dd]
DTXSID90221282
CS-0018104
HY-100125
sr1368
A17108
Q27253081
1-cyclohexyl-3-(2-methylquinolin-4-yl)-2-(thiazol-2-yl)guanidine
AKOS040740386

Research Excerpts

Overview

Timegadine is a tri-substituted guanidine derivative. It inhibits both arachidonate cyclo-oxygenase and lipoxygen enzyme activity.

ExcerptReferenceRelevance
"Timegadine is a tri-substituted guanidine derivative which inhibits both arachidonate cyclo-oxygenase and lipoxygenase activity. "( Timegadine: more than a non-steroidal for the treatment of rheumatoid arthritis. A controlled, double-blind study.
Andersen, RB; Egsmose, C; Lund, B, 1988
)
3.16

Dosage Studied

ExcerptRelevanceReference
" Detailed studies in adjuvant arthritic rats showed: (a) long dosing regimen with timegadine inhibited primary and secondary lesions, leukocytosis and hyperfibrinogemia, (b) timegadine was significantly active in reducing the severity of the already established disease, (c) a short course of dosing with timegadine at the time of adjuvant injection permanently prevented the development of secondary lesions."( An unusual profile of activity of a new basic anti-inflammatory drug, timegadine.
Arrigoni-Martelli, E; Binderup, L; Bramm, E, 1981
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID185018Minimum effective dose against adjuvant arthritis on prophylactic dosing (peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID194117Average percent inhibition (arthritis score=3) of the swelling of both injected and non injected paw was measured1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID185017Minimum effective dose against adjuvant arthritis on administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID228185Effective dose against analgesic activity (peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID134741Lethal dose in mice determined by Litchfield and Wilcoxon methods after peroral administration.1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID134594Lethal dose in mice(peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID76028Inhibitory effect on platelet aggregation induced by Arachidonic acid (AA) in guinea pigs ex vivo at a dose of 1 mg/Kg after 1 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID191307Total score is the sum of scores obtained in the adjuvant arthritis, acute toxicity, carrageenan edema, and prostaglandin synthetase assay1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID184641Lethal dose in rats(peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID184793Toxic score (3) was measured as lethal dose in orally administered mice1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID192836Tested for inhibition in the rat paw not injected with carrageenan.1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID192835Tested for inhibition in the rat paw injected with carrageenan.1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID176610In vitro vasodilatory activity in isolated rat aorta1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID185019Minimum effective dose against adjuvant arthritis on therapeutic dosing (peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID76031Inhibitory effect on platelet aggregation induced by Arachidonic acid (AA) in guinea pigs ex vivo at a dose of 3.2 mg/Kg after 1 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID165617In vitro antiplatelet activity against arachidonic acid induced malondialdehyde production1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID192837Percent inhibition of carrageenan paw edema in rat, administered orally at a dose of one tenth of oral lethal dose in mice1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID160890Inhibition of prostaglandin synthetase in bovine seminal vesicle microsomes using Beckman liquid scintillation counter at 10 e-5 M1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID178375Effective dose against carrageenan edema(peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID155220Inhibitory concentration against PG synthetase1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID185020Minimum effective dose is the lowest dose preventing any futher increase in body temperature1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID178376Effective dose against gastroulcerogenic activity (peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
AID178378Effective dose against nystatin edema(peroral administration)1980Journal of medicinal chemistry, Jan, Volume: 23, Issue:1
Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-199019 (90.48)18.7374
1990's2 (9.52)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)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 (%)
Trials2 (9.52%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (90.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]