6-(4-羧甲基氧苯基)-4,5-二氢-3(2H)-哒嗪酮的一些酰胺衍生物的合成及血管舒张活性。

Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)-pyridazinone.

机构信息

University Institute of Pharmaceutical Sciences, Panjab University, Sector 14, Chandigarh 160014, India.

出版信息

Eur J Med Chem. 2009 Nov;44(11):4441-7. doi: 10.1016/j.ejmech.2009.06.006. Epub 2009 Jun 13.

DOI:10.1016/j.ejmech.2009.06.006

PMID:19589624

Abstract

Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)-pyridazinone are reported. An effect of substitution at 2-position of pyridazinone ring on vasodilatory potential has also been explored. The most active compound 6-[4-(2-oxo-2-pyrrolidin-1-yl-ethoxy)phenyl]-2-(4-fluorophenyl)-4,5-dihydropyridazin-3(2H)-one (11) exhibited vasodilating activity in nanomolar range (IC(50)=0.051 microM).

摘要

报道了一些 6-(4-羧甲基苯氧基)-4,5-二氢-3(2H)-哒嗪酮的酰胺衍生物的合成及其血管舒张活性。还探讨了哒嗪酮环 2 位取代对血管舒张潜能的影响。最活跃的化合物 6-[4-(2-氧代-2-吡咯烷-1-基-乙氧基)苯基]-2-(4-氟苯基)-4,5-二氢哒嗪-3(2H)-酮（11）在纳摩尔范围内表现出血管舒张活性（IC50=0.051μM）。