Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens

Author:

Ma Zhenkun1ORCID,He Shijie1,Yuan Ying1,Zhuang Zhijun1,Liu Yu1,Wang Huan1,Chen Jing1,Xu Xiangyi1,Ding Charles1,Molodtsov Vadim2,Lin Wei2ORCID,Robertson Gregory T.3,Weiss William J.4,Pulse Mark4,Nguyen Phung4,Duncan Leonard5,Doyle Timothy5,Ebright Richard H.2,Lynch Anthony Simon1

Affiliation:

1. TenNor Therapeutics Ltd, 218 Xinghu Street, Suzhou Industrial Park, Suzhou 215123, China

2. Waksman Institute and Department of Chemistry and Chemical Biology, Rutgers University, Piscataway, New Jersey 08854, United States

3. Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, 80523-1682, United States

4. HSC College of Pharmacy, University of North Texas, Fort Worth, Texas 76107, United States

5. JMI Laboratories, North Liberty, Iowa 52317, United States

Funder

Ministry of Science and Technology of the People's Republic of China

National Institute of General Medical Sciences

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference51 articles.

1. World Health Organization. Global shortage of innovative antibiotics fuels emergence and spread of drug-resistance; WHO: Geneva, 2021. https://www.who.int/news/item/15-04-2021-global-shortage-of-innovative-antibiotics-fuels-emergence-and-spread-of-drug-resistance (accessed 2022-01-12).

2. U.S. Department of Health and Human Services, CDC. Antibiotic resistance threats in the United States; CDC: Atlanta, GA, 2019.

3. The Pew Charitable Trusts. Tracking the global pipeline of antibiotics in development; The Pew Charitable Trusts: Philadelphia, PA, 2021. https://www.pewtrusts.org/en/research-and-analysis/issue-briefs/2019/03/tracking-the-global-pipeline-of-antibiotics-in-development (accessed 2022-01-12).

4. Helicobacter pylori treatment in the post-antibiotics era—searching for new drug targets

5. Management of Helicobacter pylori infection: The Bhubaneswar Consensus Report of the Indian Society of Gastroenterology

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