Bioorganic and Medicinal Chemistry Letters p. 2338 - 2342 (2012)
Update date:2022-09-26
Topics:
Sun, Xicheng
Qiu, Jian
Strong, Sarah A.
Green, Louis S.
Wasley, Jan W.F.
Blonder, Joan P.
Colagiovanni, Dorothy B.
Stout, Adam M.
Mutka, Sarah C.
Richards, Jane P.
Rosenthal, Gary J.
The enzyme S-nitrosoglutathione reductase (GSNOR) is a member of the alcohol dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, gastrointestinal, and cardiovascular systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently in clinical development for acute asthma. We describe here the synthesis and structure-activity relationships (SAR) of novel pyrrole based analogs of N6022 focusing on carboxamide modifications on the pendant N-phenyl moiety. We have identified potent and novel GSNOR inhibitors that demonstrate efficacy in an ovalbumin (OVA) induced asthma model in mice.
View MoreCangzhou Senary Chemical Science-tech Co., Ltd
Contact:+86-317-3563899, 3563699
Address:168 Jinde Road, Cangzhou, Hebei, China
WuHan rongfashun BioChemical co., LTD
Contact:02788866139
Address:No.95 LuoYu Road,Wuhan
Shouguang Haogang Chemical Co., Ltd.
Contact:86-0536-5672678
Address:Bohai Chemical Industrial Park,
Hangzhou Gangjin Chemical Co.,Ltd.
Contact:+86-571-85109780
Address:707 Zhejiang Minhang Bldg., No.290 Zhongshan North Road, Hangzhou 310003, China
qingdao goldenchem imp and exp co.,ltd.
Contact:532-55579246
Address:no.62 ,haier road laoshan distirct
Doi:10.1557/mrs2001.14
(1938)Doi:10.1016/S0040-4020(01)86133-0
(1988)Doi:10.1002/recl.19881071205
(1988)Doi:10.13005/ojc/330361
(2017)Doi:10.1021/ja00127a028
(1995)Doi:10.1007/s10870-016-0667-6
(2016)