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 Source | ID |
|---|---|
| PubMed CID | 68902 |
| CHEMBL ID | 276368 |
| SCHEMBL ID | 187366 |
| MeSH ID | M0092840 |
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.
| Excerpt | Reference | Relevance |
|---|---|---|
| "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
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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 ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID185018 | Minimum effective dose against adjuvant arthritis on prophylactic dosing (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID194117 | Average percent inhibition (arthritis score=3) of the swelling of both injected and non injected paw was measured | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID185017 | Minimum effective dose against adjuvant arthritis on administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID228185 | Effective dose against analgesic activity (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID134741 | Lethal dose in mice determined by Litchfield and Wilcoxon methods after peroral administration. | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID134594 | Lethal dose in mice(peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID76028 | Inhibitory 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 administration | 1994 | Journal 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. |
| AID191307 | Total score is the sum of scores obtained in the adjuvant arthritis, acute toxicity, carrageenan edema, and prostaglandin synthetase assay | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID184641 | Lethal dose in rats(peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID184793 | Toxic score (3) was measured as lethal dose in orally administered mice | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID192836 | Tested for inhibition in the rat paw not injected with carrageenan. | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID192835 | Tested for inhibition in the rat paw injected with carrageenan. | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID176610 | In vitro vasodilatory activity in isolated rat aorta | 1994 | Journal 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. |
| AID185019 | Minimum effective dose against adjuvant arthritis on therapeutic dosing (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID76031 | Inhibitory 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 administration | 1994 | Journal 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. |
| AID165617 | In vitro antiplatelet activity against arachidonic acid induced malondialdehyde production | 1994 | Journal 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. |
| AID192837 | Percent inhibition of carrageenan paw edema in rat, administered orally at a dose of one tenth of oral lethal dose in mice | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID160890 | Inhibition of prostaglandin synthetase in bovine seminal vesicle microsomes using Beckman liquid scintillation counter at 10 e-5 M | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID178375 | Effective dose against carrageenan edema(peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID155220 | Inhibitory concentration against PG synthetase | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID185020 | Minimum effective dose is the lowest dose preventing any futher increase in body temperature | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID178376 | Effective dose against gastroulcerogenic activity (peroral administration) | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Basic antiinflammatory compounds. N,N',N''-Trisubstituted guanidines. |
| AID178378 | Effective dose against nystatin edema(peroral administration) | 1980 | Journal 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 19 (90.48) | 18.7374 |
| 1990's | 2 (9.52) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (9.52%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 19 (90.48%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||