IRIS

We investigated some pyrrolobenzoxazepinone (PBOs, 3e-i) analogues of early described effective non-nucleoside inhibitors of HIV-1 reverse transcriptase (RT). Enzymological studies of 3e-i enantiomers, with wild type (wt) RT and some drug-resistant mutants, revealed a stereoselective mode of action and selectivity for RT ternary complex. Unexpectedly (+)-3g was found more potent towards the L100I mutant than towards the wt RT, whereas (+)-3h inhibited the K103N mutant and RT wt with comparable potency. (C) 2011 Elsevier Ltd. All rights reserved.

Butini, S., Gemma, S., Brindisi, M., Borrelli, G., Fiorini, I., Samuele, A., et al. (2011). Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21(13), 3935-3938 [10.1016/j.bmcl.2011.05.020].

Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants

Butini, S.;Gemma, S.;Borrelli, G.;Fiorini, I.;Campiani, G.;
2011-01-01

Abstract

We investigated some pyrrolobenzoxazepinone (PBOs, 3e-i) analogues of early described effective non-nucleoside inhibitors of HIV-1 reverse transcriptase (RT). Enzymological studies of 3e-i enantiomers, with wild type (wt) RT and some drug-resistant mutants, revealed a stereoselective mode of action and selectivity for RT ternary complex. Unexpectedly (+)-3g was found more potent towards the L100I mutant than towards the wt RT, whereas (+)-3h inhibited the K103N mutant and RT wt with comparable potency. (C) 2011 Elsevier Ltd. All rights reserved.
2011
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Butini, S., Gemma, S., Brindisi, M., Borrelli, G., Fiorini, I., Samuele, A., et al. (2011). Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21(13), 3935-3938 [10.1016/j.bmcl.2011.05.020].
1.1 Articolo in rivista
File in questo prodotto:
File Dimensione Formato  
43_2011_BMCL_RT.pdf

non disponibili

Tipologia: Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 319.28 kB
Formato Adobe PDF
  Visualizza/Apri   Richiedi una copia
319.28 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.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/3207
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo