synthesis of potent inhibitors of β-ketoacyl-acyl carrier protein synthase iii as potential antimicrobial agents合成的抑制剂β-ketoacyl-acyl载体蛋白合酶iii作为潜在的抗菌药物.pdfVIP

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synthesis of potent inhibitors of β-ketoacyl-acyl carrier protein synthase iii as potential antimicrobial agents合成的抑制剂β-ketoacyl-acyl载体蛋白合酶iii作为潜在的抗菌药物.pdf

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synthesis of potent inhibitors of β-ketoacyl-acyl carrier protein synthase iii as potential antimicrobial agents合成的抑制剂β-ketoacyl-acyl载体蛋白合酶iii作为潜在的抗菌药物

Molecules 2012, 17, 4770-4781; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of Potent Inhibitors of β-Ketoacyl-Acyl Carrier Protein Synthase III as Potential Antimicrobial Agents Yan Liu 1,2, Wu Zhong 2,*, Rui-Juan Li 1,2 and Song Li 2 1 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mail: liuyanbtnet@163.com (Y.L.) 2 Laboratory of Computer-Aided Drug Design Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China * Author to whom correspondence should be addressed; E-Mail: zhongwu@; Tel.: +86-10-66-931-634; Fax: +86-10-68-240-321. Received: 26 December 2011; in revised form: 11 April 2012 / Accepted: 16 April 2012 / Published: 25 April 2012 Abstract: Mycobacterium tuberculosis FabH, an essential enzyme in the mycolic acid biosynthetic pathway, is an attractive target for novel anti-tubercolosis agents. Structure-based design and synthesis of 1-(4-carboxybutyl)-4-(4-(substituted benzyloxy) phenyl)-1H-pyrrole-2-carboxylic acid derivatives 7a–h, a subset of eight potential FabH inhibitors, is described in this paper. The Vilsmeier-Haack reaction was employed as a key step. The structures of all the newly synthesized compounds were identified by IR, 1H-NMR, 13C-NMR, ESI-MS and HRMS. The alamarBlue™ microassay was employed to evaluate the compounds 7a–h against Mycobacterium tuberculosis H37Rv. The result