Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides as inotropic agents.
We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit hearts. Several compounds were developed from and showed favorable activities compared with the standard drug milrinone. Compound 4l was the most potent with an increased stroke volume of 11.78 ± 0.18% (milrinone 6.36 ± 0.13%) at 1 × 10(-4) M in our in-vitro study. The chronotropic effects of compounds having inotropic effects were also evaluated.
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji, 133000, PR China.
Tianyi
T
Zhang
Liangpeng
L
Sun
Xuekun
X
Liu
Xun
X
Cui
Huri
H
Piao
D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects*
D000081:Acetamides; D002316:Cardiotonic Agents