280570-98-1Relevant academic research and scientific papers
Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain
Cuzzucoli Crucitti, Giuliana,Métifiot, Mathieu,Pescatori, Luca,Messore, Antonella,Madia, Valentina Noemi,Pupo, Giovanni,Saccoliti, Francesco,Scipione, Luigi,Tortorella, Silvano,Esposito, Francesca,Corona, Angela,Cadeddu, Marta,Marchand, Christophe,Pommier, Yves,Tramontano, Enzo,Costi, Roberta,Di Santo, Roberto
, p. 1915 - 1928 (2015/04/27)
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
Aromatic heterocycle compounds having HIV integrase inhibiting activities
-
, (2008/06/13)
A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORAwherein RAis hydrogen or ester residue, —CONRBRCwherein RBand RCeach is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.
