Synthesis and pharmacological activity of 5-substituted-s-triazole-3-thiols.
Two subgroups of 5-substituted triazoles were synthesized: derivatives of 3(3-substituted-amino-2-hydroxypropylthio)-5-substituted-4H-1,2,4- triazole and derivatives of N-substituted amides of 5-substituted-s-(1,2,4-triazole-3)thioglycolic acid. Selected members of the two subseries were tested pharmacologically. The blood pressure lowering effect in anaesthetized normotensive rats was weak to moderate. More pronounced was the inhibitory effect against adrenaline induced human blood platelet aggregation. In experiments on isolated rat heart atria and on isolated rat tail artery the activity of the agents was much weaker than in the case of known beta or alpha adrenoceptor antagonists. Generally, the chance to find a potential antihypertensive agent within the group studied seems to be low. Antiaggregatory activity of the compounds deserves further studies.
Czarnocka-Janowicz
A
A
Department of Organic Chemistry, Medical Academy of Gdańsk, Poland.
Foks
H
H
Nasal
A
A
Petrusewicz
J
J
Damasiewicz
B
B
Radwańska
A
A
Kaliszan
R
R
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis; D001794:Blood Pressure / Q000187:drug effects; D002317:Cardiovascular Agents / Q000138:chemical synthesis*; D004837:Epinephrine / Q000494:pharmacology; D006321:Heart / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis; D051381:Rats; D011919:Rats, Inbred Strains; D013440:Sulfides / Q000138:chemical synthesis / Q000494:pharmacology; D013864:Thioglycolates / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000959:Antihypertensive Agents; D002317:Cardiovascular Agents; D010975:Platelet Aggregation Inhibitors; D013440:Sulfides; D013864:Thioglycolates; D014230:Triazoles; D004837:Epinephrine