Diaryl ethers with carboxymethoxyphenacyl motif as potent HIV-1 reverse transcriptase inhibitors with improved solubility.
J Enzyme Inhib Med Chem
; 33(1): 9-16, 2018 Dec.
Article
em En
| MEDLINE
| ID: mdl-29098886
ABSTRACT
In search of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) with improved solubility, two series of novel diaryl ethers with phenacyl moiety were designed and evaluated for their HIV-1 reverse transcriptase inhibition potentials. All compounds exhibited good to excellent results with IC50 at low micromolar to submicromolar concentrations. Two most active compounds (7e and 7 g) exhibit inhibitory potency comparable or even better than that of nevirapine and rilpivirine. Furthermore, SupT1 and CD4+ cell infectivity assays for the most promising (7e) have confirmed its strong antiviral potential while docking studies indicate a novel binding interactions responsible for high activity.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Resorcinóis
/
Catecóis
/
HIV-1
/
Inibidores da Transcriptase Reversa
/
Fármacos Anti-HIV
/
Éteres
/
Transcriptase Reversa do HIV
Limite:
Humans
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article