Synthesis and vasodepressor screen of a series of 2-(2-alkylaminoalkylamido)-3-carbamyl-4-methyl-5-benzylpyrroles.
A series of 2-(2-alkylaminoalkylamido)-3-carbamyl-4-methyl-5-benzylpyrroles was synthesized and screened for vasoactivity. The compounds were administered intraperitoneally as a suspension to approximate the oral route of administration and intravenously when solubilization could be affected with suitable solvents. The most active compound following intravenous or intraperitoneal administration lowered blood pressure 73 and 35.5 mm Hg at doses of 4 mg/kg iv and 100mg/kg ip, respectively. It also exhibited the longest duration of vasodepressor activity (25 min). Several other compounds exhibited vasodepressor activity following intraperitoneal administration. Several hydrochloride salts appeared to be more potent vasoactive agents than the corresponding bases.
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006439:Hemodynamics / Q000187:drug effects*; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D008297:Male; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000959:Antihypertensive Agents; D011758:Pyrroles; D008012:Lidocaine