Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase

M. Font; A. Monge; A. Cuartero; A. Elorriaga; J. J. Martínez-Irujo; E. Alberdi; E. Santiago; I. Prieto; J. J. Lasarte; P. Sarobe; F. Borrás

doi:10.1016/0223-5234(96)88316-4

Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase

M. Font
, A. Monge^*
, A. Cuartero
, A. Elorriaga
, J. J. Martínez-Irujo
, E. Alberdi
, E. Santiago
, I. Prieto
, J. J. Lasarte
, P. Sarobe
, F. Borrás

^*Autor corresponent d’aquest treball

Producció científica: Article en revista indexada › Article › Avaluat per experts

31 Cites (Scopus)

Resum

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-1_IIIB-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.

Idioma original	Anglès
Pàgines (de-a)	963-971
Nombre de pàgines	9
Revista	European Journal of Medicinal Chemistry
Volum	30
Número	12
DOIs	https://doi.org/10.1016/0223-5234(96)88316-4
Estat de la publicació	Publicada - 1995
Publicat externament	Sí

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10.1016/0223-5234(96)88316-4

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@article{1aadb81aacf6480bac8b42bff3050dfa,

title = "Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase",

abstract = "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.",

keywords = "indole, nonnucleoside RT inhibitor, syncytia assay/HIV-1 HT4lacZ-1 cells",

author = "M. Font and A. Monge and A. Cuartero and A. Elorriaga and Mart{\'i}nez-Irujo, \{J. J.\} and E. Alberdi and E. Santiago and I. Prieto and Lasarte, \{J. J.\} and P. Sarobe and F. Borr{\'a}s",

year = "1995",

doi = "10.1016/0223-5234(96)88316-4",

language = "English",

volume = "30",

pages = "963--971",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

number = "12",

}

Font, M, Monge, A, Cuartero, A, Elorriaga, A, Martínez-Irujo, JJ, Alberdi, E, Santiago, E, Prieto, I, Lasarte, JJ, Sarobe, P & Borrás, F 1995, 'Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase', European Journal of Medicinal Chemistry, vol. 30, núm. 12, pàg. 963-971. https://doi.org/10.1016/0223-5234(96)88316-4

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 - https://www.scopus.com/pages/publications/0029593290

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 -

Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase

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