Bioorganic and Medicinal Chemistry Letters p. 2689 - 2692 (2014)
Update date:2022-07-29
Topics:
Kawasaki, Motoji
Fusano, Akira
Nigo, Tomohiro
Nakamura, Shunya
Ito, Mari N.
Teranishi, Yasuhiro
Matsumoto, Satoshi
Toda, Hiroshi
Nomura, Naruaki
Sumiyoshi, Takaaki
A series of 2,3-disubstituted pyridines were synthesized as potential non-emetic PDE4 inhibitors. To decrease brain exposure and minimize emesis, we modified the lipophilic moiety of a series of emetic PDE4 inhibitors and found that introduction of a hydroxy group into the pyridine moiety of the side chain led to non-emetic compounds with preserved PDE4 inhibitory activity. Following optimization at the phenoxy group, we identified compound 1 as a potent non-emetic PDE4 inhibitor. Compound 1 showed significant efficacy in an animal model of asthma without inducing emesis.
View Morewebsite:http://www.mascot-ie.com
Contact:86-519-85010339
Address:B-802,XingBei Building,391#,Tongjiang Middle Road New District,Changzhou,JS,China
Shenyang Mole pharmaceutical Technology Development Co.,Ltd
Contact:+86-24-31204918/13889278616
Address:No.44, wanliutang road, shenhe District of Shenyang
Shandong Yaroma Perfumery Co., Ltd.
Contact:+86- 531- 88024598
Address:7-702 Caizhi Central, 59 Gong Ye South Road, Jinan City,250101, P. R. China
Nantong Auxin Electronic Technology Co., LTD
Contact:86-513-88760026
Address:NO.5-1, Aoxin Road, Haian Hi-tech Development Zone, Jiangsu Province, China
Taixing Joxin Bio-tec Co.,Ltd.
website:http://www.joxbio.com
Contact:86-523-87558858 87612088
Address:No.88, chengdong industrial park
Doi:10.1246/bcsj.38.679
(1965)Doi:10.1055/s-2002-33655
(2002)Doi:10.1515/chempap-2015-0066
(2015)Doi:10.1021/ja00343a006
(1983)Doi:10.1039/a906903h
(2000)Doi:10.1016/S0040-4039(99)02285-6
(2000)