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Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads.

Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads.
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Bi Y, Liu XX, Zhang HY, Yang X, Liu ZY, Lu J, Lewis PJ, Wang CZ, Xu JY, Meng QG, Ma C, Yuan CS,


Bi Y, Liu XX, Zhang HY, Yang X, Liu ZY, Lu J, Lewis PJ, Wang CZ, Xu JY, Meng QG, Ma C, Yuan CS, (click to view)

Bi Y, Liu XX, Zhang HY, Yang X, Liu ZY, Lu J, Lewis PJ, Wang CZ, Xu JY, Meng QG, Ma C, Yuan CS,

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Molecules (Basel, Switzerland) 2017 04 0722(4) pii E590
Abstract

Due to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2-16 µg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI < 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity.

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