Discovery of mercaptopropanamide-substituted aryl tetrazoles as new broad-spectrum metallo-β-lactamase inhibitors-Reference-Cited by-同舟云学术

Discovery of mercaptopropanamide-substituted aryl tetrazoles as new broad-spectrum metallo-β-lactamase inhibitors

Published:2020 Issue:52 Volume:10 Page:31377-31384
ISSN:2046-2069
Container-title:RSC Advances
language:en
Short-container-title:RSC Adv.

Author:

Yan Yu-Hang¹²³⁴⁵,Chen Jian¹²³⁴⁵,Zhan Zhen¹²³⁴⁵,Yu Zhu-Jun¹²³⁴⁵,Li Gen¹²³⁴⁵,Guo Li¹²³⁴⁵,Li Guo-Bo¹²³⁴⁵^ORCID,Wu Yong¹²³⁴⁵^ORCID,Zheng Yongxiang¹²³⁴⁵^ORCID

Affiliation:

1. Key Laboratory of Drug Targeting and Drug Delivery System of Ministry of Education

2. Sichuan Engineering Laboratory for Plant-Sourced Drug

3. Sichuan Research Center for Drug Precision Industrial Technology

4. West China School of Pharmacy

5. Sichuan University

Abstract

Compound 13a showed IC₅₀ values of 0.044 μM, 0.396 μM and 0.71 μM against VIM-2, NDM-1 and IMP-1 MBL, respectively. It binds to chelates via active site zinc ions and forms interactions with residues on the L1 and L3 loops of VIM-2.

Funder

National Natural Science Foundation of China

West China Hospital, Sichuan University

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2020/RA/D0RA06405J

Reference25 articles.

1. Global antibiotic consumption 2000 to 2010: an analysis of national pharmaceutical sales data

2. A β-lactamase inhibitor revival provides new hope for old antibiotics