2. Academic Validation
  3. Design, Synthesis, and Activity Evaluation of C-23-Modified 5- O-Mycaminosyltylonolide Derivatives

Design, Synthesis, and Activity Evaluation of C-23-Modified 5- O-Mycaminosyltylonolide Derivatives

  • ACS Med Chem Lett. 2024 Nov 25;15(12):2171-2180. doi: 10.1021/acsmedchemlett.4c00458.
Zhengmin Fan 1 2 3,  Ziwei Lin 1 2 3,  Hongjin Zhai 1 2 3 4,  Yaquan Cao 1 2 3 5,  Huanhuan Wang 1 2 3,  Aichata Maiga 1 2 3,  Firas Obald Arhema Frejat 1 2 3,  Changzhong Ren 6,  Chun-Li Wu 1 2 3 6
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
  • 2 Key Laboratory of Technology of Drug Preparation, Zhengzhou University, Ministry of Education of China, Zhengzhou 450001, PR China.
  • 3 Key Laboratory of Henan Province for Drug Quality and Evaluation, Zhengzhou 450001, PR China.
  • 4 Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China.
  • 5 Henan University of Science and Technology, Luoyang 471000, PR China.
  • 6 Henan Qunbo Pharmaceutical Research Institute Co. LTD, Zhengzhou 450001, PR China.
PMID: 39691534 DOI: 10.1021/acsmedchemlett.4c00458
Abstract

The widespread use of tylosin family drugs in clinical practice has led to Bacterial resistance and reduced therapeutic efficacy. We designed and synthesized a series of new semisynthetic derivatives of tylosin with 5-O-mycaminosyltylonolide as the mother nucleus, mainly by introducing a variety of amino groups at its C-23 position. Some of the compounds showed high Antibacterial activity against Gram-negative and Gram-positive bacteria. These findings indicate that the best compound, c9, possessed significant Antibacterial activity (MIC = 0.5 ug/mL), excellent bactericidal efficacy, and a low induction rate of drug resistance against Staphylococcus aureus and Escherichia coli; it also showed good Antibacterial activity against drug-resistant bacteria. In addition, compound c9 has a low toxicity in vitro and in vivo. In conclusion, compound c9 could be a potential antimicrobial lead compound that could also contribute to the development of Macrolide Antibiotics.

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