|
|||||
|
|
The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors |
|
| Authors: | Ting Pauline C Kuang Rongze Wu Heping Aslanian Robert G Cao Jianhua Kim David W Lee Joe F Schwerdt John Zhou Gang Wainhaus Samuel Black Todd A Cacciapuoti Anthony McNicholas Paul M Xu Yiming Walker Scott S |
| Affiliation: | a Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA b Department of Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA c Department of Biological Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | A structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one 1 has resulted in the identification of 2-(3,5-difluorophenyl)-4-(3-fluorocyclopentyloxy)-5-[4-(isopropylsulfonyl)piperazin-1-yl]-pyridazin-3(2H)-one 11c as a β-1,3-glucan synthase inhibitor. Compound 11c exhibited significant efficacy in an in vivo mouse model of Candida glabrata infection. |
| Keywords: | Glucan synthase inhibitor |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |