The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors
Cuzzucoli Crucitti, G., Métifiot, M., Pescatori, L., Messore, A., Madia, V.N., Pupo, G., et al. (2015). Structure−activity relationship of pyrrolyl diketo acid derivatives as dual Inhibitors of HIV‑1 integrase and reverse transcriptase ribonuclease H domain. JOURNAL OF MEDICINAL CHEMISTRY, 58(4), 1915-1928 [10.1021/jm501799k].
Structure−activity relationship of pyrrolyl diketo acid derivatives as dual Inhibitors of HIV‑1 integrase and reverse transcriptase ribonuclease H domain
MADIA, VALENTINA NOEMI;
2015-01-01
Abstract
The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitorsI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
