title: Antihypertensive thiadiazoles. 1. Synthesis of some 2-aryl-5-hydrazino-1,3,4-thiadiazoles with vasodilator activity.
abstract: Some 2-aryl-5-hydrazino-1,3,4-thiadiazoles have been synthesized and screened for antihypertensive activity. In general, compounds with a 2-substituted phenyl ring had higher activity than their 3- or 4-substituted counterparts or those containing heteroaryl groups. The 2-methylphenyl and 2-ethylphenyl derivatives 7 and 18 were the most potent members of the series. Preliminary studies indicated that the hypotensive action of these compounds was due to a direct relaxant effect on vascular smooth muscle.
authors: Department of Medicinal Chemistry, Reckitt and Colman plc, Kingston-upon-Hull, United Kingdom.
authors: S
authors: S
authors: Turner
authors: M
authors: M
authors: Myers
authors: B
authors: B
authors: Gadie
authors: A J
authors: AJ
authors: Nelson
authors: R
authors: R
authors: Pape
authors: J F
authors: JF
authors: Saville
authors: J C
authors: JC
authors: Doxey
authors: T L
authors: TL
authors: Berridge
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001794:Blood Pressure / Q000187:drug effects; D003655:Decerebrate State; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D006973:Hypertension / Q000503:physiopathology; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000959:Antihypertensive Agents; D006834:Hydrazines; D013830:Thiadiazoles