367500-94-5Relevant articles and documents
Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents
Wang, Apeng,Lv, Kai,Li, Linhu,Liu, Hongtao,Tao, Zeyu,Wang, Bin,Liu, Mingliang,Ma, Chao,Ma, Xican,Han, Bing,Wang, Aoyu,Lu, Yu
, p. 715 - 725 (2019/06/24)
A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates. Compounds 15b and 15d display good safety and pharmacokinetic profiles, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists
Xue, Yu,Tang, Jingshu,Ma, Xiaozhuo,Li, Qing,Xie, Bingxue,Hao, Yuchen,Jin, Hongwei,Wang, Kewei,Zhang, Guisen,Zhang, Liangren,Zhang, Lihe
, p. 94 - 108 (2016/04/05)
Human α7 nicotinic acetylcholine receptor (nAChR) is a promising therapeutic target for the treatment of schizophrenia accompanied with cognitive impairment. Herein, we report the synthesis and agonistic activities of a series of indolizine derivatives targeting to α7 nAChR. The results show that all synthesized compounds have affinity to α7 nAChR and some give strong agonistic activity, particularly most active agonists show higher potency than control EVP-6124. The docking and structure-activity relationship studies provide insights to develop more potent novel α7 nAChR agonists.
Chemical compounds
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, (2008/06/13)
The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.