Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity

Ying Jie Dong; Zi Hui Meng; Yan Qing Mi; Chun Zhang; Zhi Hao Cui; Peng Wang; Zhi Bin Xu

doi:10.1016/j.bmcl.2015.02.023

Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity

Ying Jie Dong
, Zi Hui Meng
, Yan Qing Mi
, Chun Zhang
, Zhi Hao Cui
, Peng Wang
, Zhi Bin Xu^*

^*Corresponding author for this work

School of Chemistry and Chemical Engineering

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

Abstract

The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 μM, with a MIC of one of the analogues as low as 7.2 μM.

Original language	English
Pages (from-to)	1799-1803
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2015.02.023
Publication status	Published - 15 Apr 2015

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antitubercular activity
N-Benzylamine side chain
Pleuromutilin derivatives

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10.1016/j.bmcl.2015.02.023

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title = "Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity",

abstract = "The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 μM, with a MIC of one of the analogues as low as 7.2 μM.",

keywords = "Antitubercular activity, N-Benzylamine side chain, Pleuromutilin derivatives",

author = "Dong, \{Ying Jie\} and Meng, \{Zi Hui\} and Mi, \{Yan Qing\} and Chun Zhang and Cui, \{Zhi Hao\} and Peng Wang and Xu, \{Zhi Bin\}",

year = "2015",

month = apr,

day = "15",

doi = "10.1016/j.bmcl.2015.02.023",

language = "English",

volume = "25",

pages = "1799--1803",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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}

TY - JOUR

T1 - Synthesis of novel pleuromutilin derivatives. Part 1

T2 - Preliminary studies of antituberculosis activity

AU - Dong, Ying Jie

AU - Meng, Zi Hui

AU - Mi, Yan Qing

AU - Zhang, Chun

AU - Cui, Zhi Hao

AU - Wang, Peng

AU - Xu, Zhi Bin

PY - 2015/4/15

Y1 - 2015/4/15

N2 - The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 μM, with a MIC of one of the analogues as low as 7.2 μM.

AB - The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 μM, with a MIC of one of the analogues as low as 7.2 μM.

KW - Antitubercular activity

KW - N-Benzylamine side chain

KW - Pleuromutilin derivatives

UR - https://www.scopus.com/pages/publications/84939967027

U2 - 10.1016/j.bmcl.2015.02.023

DO - 10.1016/j.bmcl.2015.02.023

M3 - Article

C2 - 25736994

AN - SCOPUS:84939967027

SN - 0960-894X

VL - 25

SP - 1799

EP - 1803

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity

Abstract

UN SDGs

Keywords

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