Semisynthesis: An Essential Tool for Antibiotics Drug Discovery

Author:

Goel Bharat12ORCID,Tripathi Nancy1,Bhardwaj Nivedita1,Pal Singh Inder3,Jain Shreyans K.1ORCID

Affiliation:

1. Department of Pharmaceutical Engineering and Technology Indian Institute of Technology (Banaras Hindu University) Varanasi Uttar Pradesh 221005 India

2. Christopher S. Bond Life Sciences Center University of Missouri Columbia MO 65211 USA

3. Department of Natural Products National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar (Mohali) 160062 Punjab India

Abstract

AbstractThe continuous emergence of antimicrobial resistance (AMR) is a serious threat to humans. The discovery and development of new antibiotics having new modes of action are the global need to save mankind. Natural products (NPs) have played a central role in antibiotics drug discovery. Although biologically active, natural products pose some critical issues in their therapeutic uses, including supply issues, pharmacokinetic properties, drug resistance, and toxicity. Semisynthesis holds promise in the discovery and development of antibiotics, offering a strategic approach to overcome challenges associated with antibiotic resistance and optimize the therapeutic properties of existing compounds. Semisynthesis strategies have been used to improve the antimicrobial activities of natural products. By modifying natural compounds, researchers can create derivatives that target specific bacterial pathways or mechanisms, potentially expanding the range of bacterial infections that can be effectively treated with an increased spectrum of resistance. The present review describes NP‐derived semisynthetic antibiotics approved between 1981 and 2022.

Publisher

Wiley

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