Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different biological activities and a benzothiophene containing inhibitor has shown high potency against wild type HIV-1 protease with IC50 = 60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety
Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: the benzothiophene ring as an effective moiety
CHIUMMIENTO, Lucia;FUNICELLO, Maria;LUPATTELLI, Paolo;
2012-01-01
Abstract
Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different biological activities and a benzothiophene containing inhibitor has shown high potency against wild type HIV-1 protease with IC50 = 60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moietyFile in questo prodotto:
| File | Dimensione | Formato | |
|---|---|---|---|
|
BMCLbenzothiopene-inhibitor 2012.pdf
non disponibili
Tipologia:
Abstract
Licenza:
DRM non definito
Dimensione
584.33 kB
Formato
Adobe PDF
|
584.33 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
