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

Keywords

Antitubercular activity
N-Benzylamine side chain
Pleuromutilin derivatives

UN SDGs

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

Access to Document

10.1016/j.bmcl.2015.02.023

Cite this

@article{955b14fe0ab64863b249dbaed1d4226b,

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",

publisher = "Elsevier Ltd.",

number = "8",

}

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 - http://www.scopus.com/inward/record.url?scp=84939967027&partnerID=8YFLogxK

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

Keywords

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this