Strategies towards expansion of chemical space of natural product-based compounds to enable drug discovery
Braz. J. Pharm. Sci. (Online)
; 54(spe): e01004, 2018. tab, graf
Article
in English
| LILACS
| ID: biblio-974430
Responsible library:
BR1.1
Localization: BR40.1
ABSTRACT
Natural products (NPs) are an excellent source of biologically active molecules that provide many biologically biased features that enable innovative designing of synthetic compounds. NPs are characterized by high content of sp3-hybridized carbon atoms; oxygen; spiro, bridged, and linked systems; and stereogenic centers, with high structural diversity. To date, several approaches have been implemented for mapping and navigating into the chemical space of NPs to explore the different aspects of chemical space. The approaches providing novel opportunities to synthesize NP-inspired compound libraries involve NP-based fragments and ring distortion strategies. These methodologies allow access to areas of chemical space that are less explored, and consequently help to overcome the limitations in the use of NPs in drug discovery, such as lack of accessibility and synthetic intractability. In this review, we describe how NPs have recently been used as a platform for the development of diverse compounds with high structural and stereochemical complexity. In addition, we show developed strategies aiming to reengineer NPs toward the expansion of NP-based chemical space by fragment-based approaches and chemical degradation to yield novel compounds to enable drug discovery
Full text:
Available
Collection:
International databases
Health context:
Sustainable Health Agenda for the Americas
Health problem:
Goal 5: Medicines, vaccines and health technologies
Database:
LILACS
Main subject:
Biological Products
/
Health Strategies
Language:
English
Journal:
Braz. J. Pharm. Sci. (Online)
Journal subject:
Farmacologia
/
Teraputica
/
Toxicologia
Year:
2018
Document type:
Article
Affiliation country:
Brazil
Institution/Affiliation country:
University of Sao Paulo/BR