20948-68-9Relevant academic research and scientific papers
Synthesis of 2-(2,3-Dihydro-2-oxo-1,3,4-oxadiazolyl-5-yl) Benzo Heterocycles. A Novel Series of Orally Active Antiallergic Agents
Musser, John H.,Brown, Richard E.,Loev, Bernard,Bailey, Kevin,Jones, Howard,et al.
, p. 121 - 125 (1984)
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.
Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile
Jiang, Hai-Xia,Zhuang, Dao-Min,Huang, Ying,Cao, Xing-Xin,Yao, Jian-Hua,Li, Jing-Yun,Wang, Jian-Yong,Zhang, Chen,Jiang, Biao
, p. 3446 - 3458 (2014/05/20)
A novel series of trifluoromethyl indole derivatives have been designed, synthesized and evaluated for anti-HIV-1 activities in MT-2 cells. The hydrophobic constant, acute toxicity, carcinogenicity and mutagenicity were predicted. Trifluoromethyl indoles 10i and 10k showed extremely promising activities against WT HIV-1 with IC50 values at the low nanomolar level, similar to efavirenz, better than nevirapine, and also possessed higher potency towards the drug-resistant mutant strain Y181C than nevirapine. Preliminary SAR and docking studies of detailed binding mode provided some insights for discovery of more potent NNRTIs. the Partner Organisations 2014.
