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Current Bioactive Compounds

Editor-in-Chief

ISSN (Print): 1573-4072
ISSN (Online): 1875-6646

Review Article

Bioactive Extracts: Strategies to Generate Diversified Natural Product- Like Libraries

Author(s): Meenu Aggarwal, Raman Singh, Priyanka Ahlawat and Kuldeep Singh*

Volume 18, Issue 9, 2022

Published on: 14 March, 2022

Article ID: e110122200131 Pages: 20

DOI: 10.2174/1573407218666220111105443

Price: $65

Abstract

Natural products have stimulated the interest of chemists owing to their abundant structural diversity and complexity. Indeed, natural products have performed an essential role, particularly in the cure of cancerous and infectious diseases, thereby providing medicinal researchers with several unexplored chemotypes for the innovation of new drugs. Fusion of chemical derivatization and combinatorial synthesis forms the basis of the concept of chemo diversification of plants. Diverse libraries of natural product analogs are constructed through existing biological and chemical approaches using unique schemes to expand natural product frameworks. This review aims to present several approaches employed to offer innovative opportunities to synthesize NP-inspired compound libraries. Reactive molecular fragments present in most natural products are chemically converted to chemically engineered extracts (CEEs) or semisynthetic compounds constituting distinct libraries. Bio-guided isolation for natural products required vital tools like reverse phase chromatography and bioautographic assays. Different established strategies from DTS, BIOS, CtD, FOS, FBDD to late-stage diversification facilitate the expansion of molecules with physicochemical properties. In particular, fragment-like natural products with novel skeletons may be used as preliminary points for chemical biology and medicinal chemistry programs with great capacity. In this review, we sum up how NPs have proven fruitful for the novel methodologies responsible for the diversification of complex natural products; therefore, it is worth going over the upcoming integration of natural products with combinatorial chemistry.

Keywords: Bioactive extracts, chemo diversification, natural product-like libraries, bioautographic assays, diversity-oriented synthesis, biology-oriented synthesis, fragment-based drug discovery.

Graphical Abstract


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