Synthesis of certain new 2,4,5(6) trisubstituted-1,2,4-triazolo[1,5-alpha]pyrimidines as potential antihypertensive agents.
A series of 1,2,4-triazolol[1,5-alpha]pyrimidines bearing at position 2, morpholine, piperidine or piperazine moities has been prepared. In addition, ethyl 4-methyl-2-(4-acylpiperazin-1-yl)-1,2,4-triazolo[1, 5-alpha]pyrimidin-7(4H)-one-6-carboxylates 25,26, which have related structure with prazosin, have been synthesized. Ten representative compounds were tested in vitro and in vivo for their antihypertensive activity where compounds 7, 11 and 25 showed promising activity. The detailed synthesis, spectroscopic and biological data are reported.
Bayomi
S M
SM
Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Egypt.
Abdelal
A M
AM
el-Ashry
S M
SM
Ghoneim
O A
OA
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002855:Chromatography, Thin Layer; D004285:Dogs; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013055:Spectrophotometry, Infrared
D000959:Antihypertensive Agents; D011743:Pyrimidines