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Molecules 2016, 21(11), 1488;

Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties

Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development, Ministry of Agriculture, Lanzhou Institute of Husbandry and Pharmaceutical Sciences of CAAS, 335 Jiangouyan, Lanzhou 730050, China
College of Life Science and Engineering, Lanzhou University of Technology, 287 Langongping Road, Lanzhou 730050, China
Yancheng Shunbao Chemical Co., Ltd., Yancheng 224555, China
Author to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 13 October 2016 / Revised: 2 November 2016 / Accepted: 2 November 2016 / Published: 8 November 2016
(This article belongs to the Section Medicinal Chemistry)
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A series of novel pleuromutilin derivatives with substituted benzimidazole moieties were designed and synthesized from pleuromutilin and 5-amino-2-mercaptobenzimidazole through sequential reactions. All the newly synthesized compounds were characterized by IR, NMR, and HRMS. Each of the derivatives was evaluated in vitro for their antibacterial activity against Escherichia coli (E. coli) and five Gram (+) inoculums. 14-O-((5-amino-benzimidazole-2-yl) thioacetyl) mutilin (3) was the most active compound and showed highest antibacterial activities. Furthermore, we evaluated the inhibition activities of compound 3 on short-term S. aureus and MRSA growth and cytochrome P450 (CYP). The bioassay results indicate that compound 3 could be considered potential antibacterial agents but with intermediate inhibition of CYP3A4. View Full-Text
Keywords: pleuromutilin derivatives; synthesis; antibacterial activity; inhibition; CYP3A4 pleuromutilin derivatives; synthesis; antibacterial activity; inhibition; CYP3A4

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Ai, X.; Pu, X.; Yi, Y.; Liu, Y.; Xu, S.; Liang, J.; Shang, R. Synthesis and Pharmacological Evaluation of Novel Pleuromutilin Derivatives with Substituted Benzimidazole Moieties. Molecules 2016, 21, 1488.

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