Cardiotonic agents. 6. Synthesis and inotropic activity of 2,4-dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-3H-pyrazol-3-ones: ring-contracted analogues of imazodan (CI-914) |
| |
Authors: | I Sircar G C Morrison S E Burke R Skeean R E Weishaar |
| |
Institution: | Department of Chemistry, Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48105. |
| |
Abstract: | A series of 2,4-dihydro-5-4-(1H-imidazol-1-yl)phenyl]-3H-pyrazol-3-ones was synthesized and evaluated for positive inotropic activity. Only compounds with two small alkyl groups at C-4 showed significant activity. The structure-activity relationships for optimal inotropic activity are presented and compared with those of the 4,5-dihydro-3(2H)-pyridazinone series. The phosphodiesterase inhibitory activity is also reported and correlated with the substitution pattern at C-4 in the pyrazolone ring. |
| |
Keywords: | |
|
|