title: Hybrid Compounds as Direct Multitarget Ligands: A Review.
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.
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Department of Biological Science, State University of Paraiba, Joao Pessoa, PB,. Brazil.
authors.forename: Michelle
authors.initials: M
authors.lastname: de Oliveira Pedrosa
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Department of Biological Science, State University of Paraiba, Joao Pessoa, PB,. Brazil.
authors.forename: Rayssa Marques
authors.initials: RM
authors.lastname: Duarte da Cruz
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Department of Biological Science, State University of Paraiba, Joao Pessoa, PB,. Brazil.
authors.forename: Jessika
authors.initials: J
authors.lastname: de Oliveira Viana
authors.affiliation: Laboratory of Synthesis and Drug Delivery, Department of Biological Science, State University of Paraiba, Joao Pessoa, PB,. Brazil.
authors.forename: Ricardo Olimpio
authors.initials: RO
authors.lastname: de Moura
authors.affiliation: University of Western Sao Paulo (Unoeste), Presidente Prudente, SP,. Brazil.
authors.forename: Hamilton Mitsugu
authors.initials: HM
authors.lastname: Ishiki
authors.affiliation: Federal University of Paraiba, Campus I, Joao Pessoa-PB,. Brazil.
authors.forename: Jose Maria
authors.initials: JM
authors.lastname: Barbosa Filho
authors.affiliation: Federal University of Paraiba, Campus I, Joao Pessoa-PB,. Brazil.
authors.forename: Margareth F F M
authors.initials: MF
authors.lastname: Diniz
authors.affiliation: Federal University of Paraiba, Campus I, Joao Pessoa-PB,. Brazil.
authors.forename: Marcus Tullius
authors.initials: MT
authors.lastname: Scotti
authors.affiliation: Federal University of Paraiba, Campus I, Joao Pessoa-PB,. Brazil.
authors.forename: Luciana
authors.initials: L
authors.lastname: Scotti
authors.affiliation: Department of Chemistry, State Universtiy of Paraiba, Joao Pessoa, Paraiba -58071-160,. Brazil.
authors.forename: Francisco Jaime
authors.initials: FJ
authors.lastname: Bezerra Mendonca
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D008024:Ligands; D015394:Molecular Structure
chemical_list: D000890:Anti-Infective Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D008024:Ligands
keywords: Anti-inflammatory; Anticancer; Antimicrobial; Antiprotozoal.; Hybrid compounds; Multitarget