Affiliation:
1. Department of Pharmacy and Biotechnology, Alma Mater Studiorum − University of Bologna, I-40126, Bologna, Italy
Abstract
Molecular hybridization is a well-exploited medicinal chemistry strategy that aims to combine
two molecules (or parts of them) in a new, single chemical entity. Recently, it has been recognized
as an effective approach to design ligands able to modulate multiple targets of interest. Hybrid compounds
can be obtained by linking (presence of a linker) or framework integration (merging or fusing)
strategies. Although very promising to combat the multifactorial nature of complex diseases, the development
of molecular hybrids faces the critical issues of selecting the right target combination and the
achievement of a balanced activity towards them, while maintaining drug-like-properties. In this review,
we present recent case histories from our own research group that demonstrate why and how molecular
hybridization can be carried out to address the challenges of multitarget drug discovery in two therapeutic
areas that are Alzheimer’s and parasitic diseases. Selected examples spanning from linker- to fragment-
based hybrids will allow to discuss issues and consequences relevant to drug design.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,General Medicine
Cited by
187 articles.
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