Journal of Medicinal Chemistry p. 121 - 125 (1984)
Update date:2022-08-23
Topics:
Musser, John H.
Brown, Richard E.
Loev, Bernard
Bailey, Kevin
Jones, Howard
et al.
A series of new 2-(2,3-dihydro-2-oxo-1,3,4-oxadiazol-5-yl) benzo heterocycles has been prepared.These compounds were tested as inhibitors of antigen-induced release of histamine (AIR) in vitro from rat peritoneal mast cells (RMC) and as inhibitors of IgE-mediated rat passive cutaneous anaphylaxis in the rat (PCA).Most of this new class of antiallergic agents showed good activity in the RMC assay.The most potent compound, 3-chloro-2-(2,3-dihydro-2-oxo-1,3,4-oxadiazol-5-yl)benzothiophene (6t), with an I50 value of 0.2 μM, is 15 times more potent than disodium cromoglycate (DSCG) in the RMC assay.Many compounds were orally active in the PCA test, and several of these compounds showed higher potency when given in this way to that shown by DSCG when given intraperitoneally.
View MoreHEZE KINGVOLT CHEMICAL CO., LTD
Contact:86-573-82118911
Address:Juancheng Industry Park
Jinan Jiaquan Chemical Co.,Ltd
Contact:+86-531-62318366
Address:Room 502 of Yidonghuayuan No.601 Huaxin Road Licheng District Jinan China
Contact:86-0510-85133006
Address:hubin road NO157
Hebei Tianxiang Biological & Pharmaceutical Co., Ltd
Contact:86-0312-6615158
Address:No 42 fazhan street qingyuan county
zhuzhou zhongle chemical co. ltd.
Contact:+86-0731 28228409
Address:Zhuzhou, Hunan, China
Doi:10.1039/d0gc03188g
(2021)Doi:10.1021/ol025844x
(2002)Doi:10.1016/j.ejmech.2015.10.034
(2015)Doi:10.1039/d0sc02386h
(2020)Doi:10.1016/j.ejmech.2020.112991
(2021)Doi:10.1039/b413488e
(2005)