Drug/Lead Compound Hydroxymethylation as a Simple Approach to Enhance Pharmacodynamic and Pharmacokinetic Properties

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dc.contributor.authorSantos, Soraya S.
dc.contributor.authorGonzaga, Rodrigo V.
dc.contributor.authorScarim, Cauê B. [UNESP]
dc.contributor.authorGiarolla, Jeanine
dc.contributor.authorPrimi, Marina C.
dc.contributor.authorChin, Chung M. [UNESP]
dc.contributor.authorFerreira, Elizabeth I.
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)
dc.contributor.institutionThe Scripps Research Institute
dc.contributor.institutionUnião Das Faculdades Dos Grande Lagos (UNILAGO)
dc.date.accessioned2022-04-29T08:40:05Z
dc.date.available2022-04-29T08:40:05Z
dc.date.issued2022-02-14
dc.description.abstractHydroxymethylation is a simple chemical reaction, in which the introduction of the hydroxymethyl group can lead to physical–chemical property changes and offer several therapeutic advantages, contributing to the improved biological activity of drugs. There are many examples in the literature of the pharmaceutical, pharmacokinetic, and pharmacodynamic benefits, which the hydroxymethyl group can confer to drugs, prodrugs, drug metabolites, and other therapeutic compounds. It is worth noting that this group can enhance the drug’s interaction with the active site, and it can be employed as an intermediary in synthesizing other therapeutic agents. In addition, the hydroxymethyl derivative can result in more active compounds than the parent drug as well as increase the water solubility of poorly soluble drugs. Taking this into consideration, this review aims to discuss different applications of hydroxymethyl derived from biological agents and its influence on the pharmacological effects of drugs, prodrugs, active metabolites, and compounds of natural origin. Finally, we report a successful compound synthesized by our research group and used for the treatment of neglected diseases, which is created from the hydroxymethylation of its parent drug.en
dc.description.affiliationLaboratório de Planejamento e Síntese de Quimioterápicos Potencialmente Ativos Em Doenças Negligenciadas (LAPEN) Departamento de Farmácia Faculdade de Ciências Farmacêuticas Universidade de São Paulo – USP
dc.description.affiliationLaboratório de Pesquisa e Desenvolvimento de Fármacos (LAPDESF) Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual de São Paulo “Júlio de Mesquita Filho” (UNESP)
dc.description.affiliationThe Scripps Research Institute
dc.description.affiliationCentro de Pesquisa Avançada Em Medicina (CEPAM) Faculdade de Medicina União Das Faculdades Dos Grande Lagos (UNILAGO)
dc.description.affiliationUnespLaboratório de Pesquisa e Desenvolvimento de Fármacos (LAPDESF) Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual de São Paulo “Júlio de Mesquita Filho” (UNESP)
dc.identifierhttp://dx.doi.org/10.3389/fchem.2021.734983
dc.identifier.citationFrontiers in Chemistry, v. 9.
dc.identifier.doi10.3389/fchem.2021.734983
dc.identifier.issn2296-2646
dc.identifier.scopus2-s2.0-85125329513
dc.identifier.urihttp://hdl.handle.net/11449/230463
dc.language.isoeng
dc.relation.ispartofFrontiers in Chemistry
dc.sourceScopus
dc.subjecthydroxymethyl compounds
dc.subjecthydroxymethyl drug
dc.subjecthydroxymethylation
dc.subjecthydroxymethylnitrofurazone
dc.subjectprodrug design
dc.titleDrug/Lead Compound Hydroxymethylation as a Simple Approach to Enhance Pharmacodynamic and Pharmacokinetic Propertiesen
dc.typeResenha

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Artigos - Fármacos e Medicamentos - FCFAR