title: Synthesis of new functionalized 3-substituted [1,2,4]triazolo [4,3-a]pyrimidine derivatives: potential antihypertensive agents.
abstract: A convenient synthesis of a series of thiosemicarbazide, 1,3,4-oxadiazole, 1,3,4-thiadiazole, thiazole, 1,2,4-triazole, pyrazole and dioxoisoindoline derivatives incorporating 1,2,4-triazolo[4,3-a]pyrimidine via the reaction of the readily accessible 1,5-dihydro-5-oxo-1.7-diphenyl-1,2.4-triazolo[4,3-a]pyrimidine-3-carbohydrazide (2) with the appropriate reagents is described. The newly synthesized compounds were found to possess antihypertensive and diuretic activities compared to captopril and furosemide as reference controls, respectively.
authors.affiliation: Applied Organic Chemistry Department, National Research Center, Cairo, Egypt. kornykhlil@yahoo.com
authors.forename: Korany A
authors.initials: KA
authors.lastname: Ali
authors.forename: Eman A
authors.initials: EA
authors.lastname: Ragab
authors.forename: Thoray A
authors.initials: TA
authors.lastname: Farghaly
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Abdalla
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001794:Blood Pressure / Q000187:drug effects; D004195:Disease Models, Animal; D004231:Diuresis / Q000187:drug effects; D004232:Diuretics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D008401:Gas Chromatography-Mass Spectrometry; D006973:Hypertension / Q000188:drug therapy / Q000503:physiopathology; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D011918:Rats, Inbred SHR; D017550:Spectroscopy, Fourier Transform Infrared; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000959:Antihypertensive Agents; D004232:Diuretics; D011743:Pyrimidines; D014230:Triazoles; C045575:1,2,4-triazole