Abstract
Molecular Hybridization is an approach in rational drug design where new chemical entities are obtained by combining two or more pharmacophoric units from different bioactive compounds into a single molecule. Through this approach, medicinal chemists hope that the new hybrid derivative presents: better affinity and efficacy when compared to the parent drugs; a modified selectivity profile with improvement over pharmacokinetic and pharmacodynamic restrictions; dual or multiple modes of action; reduction of undesirable side effects; decreases in drug-drug interactions; reduced emergence or spread of drug resistance in microorganisms and protozoans; and lower cost. The approach has been successfully used by many research groups around the world and has had very promising results with diseases having multifactorial profiles, like Alzheimer´s, Parkinson´s disease, cancer, inflammation, and hypertension among others. The purpose of this paper is to conduct an updated review of molecular hybridization and multitarget profiling (a rational drug design approach), and its applications to the design and discovery of novel hybrid compounds with anti-inflammatory, antimicrobial, anticancer and antiprotozoal (leishmaniasis, malaria, and schistosomiasis) activities over the last six years.
Keywords: Hybrid compounds, Multitarget, Anti-inflammatory, Antimicrobial, Anticancer, Antiprotozoal.
Current Topics in Medicinal Chemistry
Title:Hybrid Compounds as Direct Multitarget Ligands: A Review
Volume: 17 Issue: 9
Author(s): Michelle de Oliveira Pedrosa, Rayssa Marques Duarte da Cruz, Jessika de Oliveira Viana, Ricardo Olimpio de Moura, Hamilton Mitsugu Ishiki, Jose Maria Barbosa Filho, Margareth F. F. M. Diniz, Marcus Tullius Scotti, Luciana Scotti and Francisco Jaime Bezerra Mendonca
Affiliation:
Keywords: Hybrid compounds, Multitarget, Anti-inflammatory, Antimicrobial, Anticancer, Antiprotozoal.
Abstract: Molecular Hybridization is an approach in rational drug design where new chemical entities are obtained by combining two or more pharmacophoric units from different bioactive compounds into a single molecule. Through this approach, medicinal chemists hope that the new hybrid derivative presents: better affinity and efficacy when compared to the parent drugs; a modified selectivity profile with improvement over pharmacokinetic and pharmacodynamic restrictions; dual or multiple modes of action; reduction of undesirable side effects; decreases in drug-drug interactions; reduced emergence or spread of drug resistance in microorganisms and protozoans; and lower cost. The approach has been successfully used by many research groups around the world and has had very promising results with diseases having multifactorial profiles, like Alzheimer´s, Parkinson´s disease, cancer, inflammation, and hypertension among others. The purpose of this paper is to conduct an updated review of molecular hybridization and multitarget profiling (a rational drug design approach), and its applications to the design and discovery of novel hybrid compounds with anti-inflammatory, antimicrobial, anticancer and antiprotozoal (leishmaniasis, malaria, and schistosomiasis) activities over the last six years.
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Oliveira Pedrosa de Michelle, Duarte da Cruz Marques Rayssa, Oliveira Viana de Jessika, de Moura Olimpio Ricardo, Ishiki Mitsugu Hamilton, Barbosa Filho Maria Jose, Diniz F. F. M. Margareth, Scotti Tullius Marcus, Scotti Luciana and Bezerra Mendonca Jaime Francisco, Hybrid Compounds as Direct Multitarget Ligands: A Review, Current Topics in Medicinal Chemistry 2017; 17 (9) . https://dx.doi.org/10.2174/1568026616666160927160620
DOI https://dx.doi.org/10.2174/1568026616666160927160620 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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