776-24-9Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel pyrrole derivatives as potential ClpP1P2 inhibitor against Mycobacterium tuberculosis
Liu, Pingxian,Yang, Yang,Ju, Yuan,Tang, Yunxiang,Sang, Zitai,Chen, Lijuan,Yang, Tao,An, Qi,Zhang, Tianyu,Luo, Youfu
, p. 422 - 432 (2018/07/14)
In an effort to discover novel inhibitors of M. tuberculosis Caseinolytic proteases (ClpP1P2), a combination strategy of virtual high-throughput screening and in vitro assay was employed and a new pyrrole compound, 1-(2-chloro-6-fluorobenzyl)-2, 5-dimethyl-4-((phenethylamino)methyl)-1H-pyrrole-3-carboxylate was found to display inhibitory effects against H37Ra with an MIC value of 77 μM. In order for discovery of more potent anti-tubercular agents that inhibit ClpP1P2 peptidase in M. tuberculosis, a series of pyrrole derivatives were designed and synthesized based on this hit compound. The synthesized compounds were evaluated for in vitro studies against ClpP1P2 peptidase and anti-tubercular activities were also evaluated. The most promising compounds 2-(4-bromophenyl)-N-((1-(2-chloro-6-fluorophenyl)-2, 5-dimethyl-1H- pyrrolyl)methyl)ethan-1-aminehydrochloride 7d, ethyl 4-(((4-bromophenethyl) amino) methyl)-2,5-dimethyl-1-phenyl-1H-pyrrole-3-carboxylate hydrochloride 13i, ethyl 1-(4-chlorophenyl)-4-(((2-fluorophenethyl)amino)methyl)-2-methyl-5-phenyl-1H-pyrrole-3-carboxylate hydrochloride 13n exhibited favorable anti-mycobacterial activity with MIC value at 5 μM against Mtb H37Ra, respectively.
Synthesis, structure, and fluorescence of isomeric indolizinediones. Carbonyl-bridged isodipyrrinones
Boiadjiev, Stefan E.,Lightner, David A.
, p. 553 - 565 (2007/10/03)
In "one-pot" reactions, pyrrole-α- and β-aldehydes condense readily with 4-ethyl-3-methyl-3-pyrrolin-2-one to give isodipyrrinone analogs, which undergo intramolecular cyclization when the pyrrolealdehyde possesses an α or β-CO2R group. The res
