Title:Design of Multifunctional Compounds for Cardiovascular Disease: From Natural Scaffolds to “Classical” Multitarget Approach
VOLUME: 20 ISSUE: 13
Author(s):A. Bisi, S. Gobbi, F. Belluti and A. Rampa
Affiliation:Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Keywords:ACE, AT receptors, flavonoids, hybrid drugs, hypertension, multitarget drugs, natural scaffolds, nitric oxide releasing
drugs, renin-angiotensin system, vasodilators
Abstract:Cardiovascular disease represents the main cause of death worldwide. Novel therapies to reduce elevated blood
pressure and treat resistant hypertension, to consequently reduce the associated cardiovascular risk factors, are still required.
Among the different strategies commonly used in medicinal chemistry to develop new molecules, the synthesis of
multitarget/hybrid compounds combining two or more pharmacophore groups targeting simultaneously selected factors
involved in cardiovascular diseases, has gained increasing interest. This review will focus on the most recent literature on
multifunctional cardiovascular drugs, paying particular attention on hybrid compounds bearing natural scaffolds, considering
that compounds derived from medicinal extracts are generally appealing for the medicinal chemist as they often bear
the so-called “privileged structures”. Moreover, taking into account many excellent reviews dealing with multitarget cardiovascular
drugs published in the last few years, mainly devoted to RAAS inhibition and/or NO donors hybrid drugs,
herein the most significant results obtained and the benefits and limitations of these approaches will be highlighted.