Inhibitory Activity of Pyrroloisoxazolidine Derivatives against Chlamydia trachomatis

Author:

Ni Min1ORCID,Xu Shunxin1ORCID,Liu Ziyi1ORCID,Xue Yin1ORCID,Xie Wenxia1ORCID,Yang Shengju2ORCID,Liu Lingyan3ORCID,Bao Xiaofeng14ORCID

Affiliation:

1. School of Pharmacy, Nantong University, Nantong 226001, China

2. Department of Dermatology and Venereology, Affiliated Hospital of Nantong University, Nantong 226001, China

3. State Key Laboratory of Elemento-Organic Chemsitry, Nankai University, Tianjin 300071, China

4. Key Laboratory of Inflammation and Molecular Drug Target of Jiangsu Province, Nantong University, Nantong 226001, China

Abstract

The obligate intracellular bacterium Chlamydia trachomatis is a group of worldwide human pathogens that can lead to serious reproductive problems. The frequent clinical treatment failure promoted the development of novel antichlamydial agents. Here, we firstly reported a group of pyrroloisoxazolidine-inhibited C. trachomatis in a dose-dependent manner in vitro. Among them, compounds 1 and 2 exhibited the strongest inhibitory activity with IC50 values from 7.25 to 9.73 μM. The compounds disturbed the whole intracellular life cycle of C. trachomatis, mainly targeting the middle reticulate body proliferation stages. Besides, the compounds partially inhibited the chlamydial infection by reducing elementary body infectivity at high concentration. Our findings suggest the potential of pyrroloisoxazolidine derivatives as promising lead molecules for the development of antichlamydial agents.

Funder

National Natural Science Foundation of China

Publisher

Hindawi Limited

Subject

General Immunology and Microbiology,General Biochemistry, Genetics and Molecular Biology,General Medicine

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