25627-87-6Relevant academic research and scientific papers
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.
Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase
Dumea, Carmen,Belei, Dalila,Ghinet, Alina,Dubois, Jolle,Farce, Amaury,Bcu, Elena
, p. 5777 - 5781 (2015/01/08)
The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3 ± 0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.
