TY - JOUR
T1 - Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase
AU - Font, M.
AU - Monge, A.
AU - Cuartero, A.
AU - Elorriaga, A.
AU - Martínez-Irujo, J. J.
AU - Alberdi, E.
AU - Santiago, E.
AU - Prieto, I.
AU - Lasarte, J. J.
AU - Sarobe, P.
AU - Borrás, F.
PY - 1995
Y1 - 1995
N2 - The synthesis and the study of the activity of new indol-2-carboxamides and pyridazino[4,5-b]indoles as inhibitors of HIV-1 reverse transcriptase (RT) are presented. The activity of the compounds synthesized as inhibitors of different types of HIV-1 RT (wild type enzyme and mutant forms P236L, Y 181C and P236L/Y181C) was evaluated. The activity of the most active compounds was investigated in the syncytia reduction in vitro assay, in HIV-1IIIB-infected HT4lacZ-1 cells. Their potential cytotoxicity was determined in parallel. Two lead compounds, N-[1-[2-(3-isopropylamino)pyridyl]piperazin]-5,6-methylenedioxy indol-2-carboxamide 7q and N-[1-[2-(3-ethylamino)pyridyl]piperazin]-5,6-methylenedioxyindol-2-carboxamide 7s have been identified.
AB - The synthesis and the study of the activity of new indol-2-carboxamides and pyridazino[4,5-b]indoles as inhibitors of HIV-1 reverse transcriptase (RT) are presented. The activity of the compounds synthesized as inhibitors of different types of HIV-1 RT (wild type enzyme and mutant forms P236L, Y 181C and P236L/Y181C) was evaluated. The activity of the most active compounds was investigated in the syncytia reduction in vitro assay, in HIV-1IIIB-infected HT4lacZ-1 cells. Their potential cytotoxicity was determined in parallel. Two lead compounds, N-[1-[2-(3-isopropylamino)pyridyl]piperazin]-5,6-methylenedioxy indol-2-carboxamide 7q and N-[1-[2-(3-ethylamino)pyridyl]piperazin]-5,6-methylenedioxyindol-2-carboxamide 7s have been identified.
KW - indole
KW - nonnucleoside RT inhibitor
KW - syncytia assay/HIV-1 HT4lacZ-1 cells
UR - http://www.scopus.com/inward/record.url?scp=0029593290&partnerID=8YFLogxK
U2 - 10.1016/0223-5234(96)88316-4
DO - 10.1016/0223-5234(96)88316-4
M3 - Article
AN - SCOPUS:0029593290
SN - 0223-5234
VL - 30
SP - 963
EP - 971
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 12
ER -
