Synthesis and platelet aggregation inhibitory activity of 4,5-bis(substituted)-1,2,3-thiadiazoles
| Autor: | Davey J. Williams, David C. Zimmermann, Edward W. Thomas, Edward E. Nishizawa |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
chemistry.chemical_classification
Ketone Platelet Aggregation Stereochemistry Hydrazone Biological activity In vitro chemistry.chemical_compound Structure-Activity Relationship chemistry Thiadiazoles Fibrinolytic Agents Drug Discovery Antithrombotic Molecular Medicine Humans Phenols Collagen Benzene |
| Zdroj: | Journal of medicinal chemistry. 28(4) |
| ISSN: | 0022-2623 |
| Popis: | Routine screening of compounds for inhibition of collagen-induced platelet aggregation in vitro revealed 4,5-bis-(4-methoxyphenyl)-1,2,3-thiadiazole (2) was active and it represents the first example of a 1,2,3-thiadiazole with possible antithrombotic activity. In order to develop a structure-activity relationship for this heterocycle, a number of new 4(5)-mono- and -disubstituted 1,2,3-thiadiazoles were synthesized. These were tested in our screen and a number of additional active compounds were found. The most active compounds (2, 5a, 5b, and 6c) were those in which the heterocycle was substituted with benzene rings possessing para electron-donating groups. |
| Databáze: | OpenAIRE |
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