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.

为了发现结核分枝杆菌酪蛋白水解蛋白酶（ClpP1P2）的新型抑制剂，采用了虚拟高通量筛选和体外测定的组合策略，并使用了一种新的吡咯化合物1-（2-氯-6-氟苄基）- 2，发现5-二甲基-4-（（（苯乙基氨基）甲基）-1H-吡咯-3-羧酸酯对MIC _37表现出对H ₃₇ Ra的抑制作用。为了更有效抗结核剂抑制ClpP1P2肽酶的发现结核分枝杆菌，一系列吡咯衍生物的设计并在此基础上的命中化合物合成。对合成的化合物进行了体外评估  还评估了针对ClpP1P2肽酶和抗结核活性的研究。最有前途的化合物2-（4-溴苯基）-N -（（1-（2-氯-6-氟苯基）-2，5-二甲基-1H-吡咯基）甲基）乙烷-1-胺盐酸盐7d，乙基4- （（（（4-溴苯乙基）氨基）甲基] -2,5-二甲基-1-苯基-1H-吡咯-3-羧酸盐酸盐13i，乙基1-（4-氯苯基）-4-（（（（2-氟苯乙基）氨基）甲基）-2-甲基-5-苯基-1H-吡咯-3-羧酸盐盐酸盐13n表现出良好的抗分枝杆菌活性，其MIC值为5 µM，针对Mtb H ₃₇ Ra。