Design, Synthesis And Chemical Stability Of Indolizine Derivatives For Antihypertensive Activity.

[摘要] In the present work we have synthesized the substituted 2- Phenyl indolizine (1a-f) by the reaction of2-methylpyridine with α-haloaryl ketones produced substituted 2-phenyl indolizine. In the next step 2- substituted indolizine undergo Vilsmeyer reaction to produce substituted 2-phenylindolizine-3-carbaldehydeand this treated with hydralazine to form the derivatives (3a-f). Synthesized compounds were subjected tochemical hydrolysis at pH 1.2, 6.8 and 7.4 and all the compounds have shown significant stability.IR, NMR andMass spectroscopy techniques used to confirm the structure of final derivatives. All the synthesizedcompounds were tested for antihypertensive activity by non-invasive blood pressure (NIBP) measurements(tail-cuff method) in rats. Almost all the tested compounds displayed considerable decrease in the bloodpressure as compared to control. Compounds showed significant antihypertensive activity comparable to thestandard drug hydralazine.

[学科分类] 工程和技术（综合）

[关键词] Indolizine;prodrugs;antihypertensive activity;hydralazine