Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1

C. Bartolucci; L. Cellai; P. Di Filippo; A. Segre; M. Brufani; L. Filocamo; A. D. Bianco; M. Guiso; V. Brizzi; A. Benedetto; A. Di Caro; G. Elia

Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1

C. Bartolucci, L. Cellai, P. Di Filippo, A. Segre, M. Brufani, L. Filocamo, A. D. Bianco, M. Guiso, V. Brizzi, A. Benedetto, A. Di Caro, G. Elia

Istituto Nazionale per le Malattie Infettive Lazzaro Spallanzani

Research output: Contribution to journal › Article › peer-review

Abstract

29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.

Original language	English
Pages (from-to)	1367-1383
Number of pages	17
Journal	Farmaco
Volume	47
Issue number	11
Publication status	Published - 1992

ASJC Scopus subject areas

Drug Discovery
Pharmaceutical Science

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title = "Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1",

abstract = "29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.",

author = "C. Bartolucci and L. Cellai and {Di Filippo}, P. and A. Segre and M. Brufani and L. Filocamo and Bianco, {A. D.} and M. Guiso and V. Brizzi and A. Benedetto and {Di Caro}, A. and G. Elia",

year = "1992",

language = "English",

volume = "47",

pages = "1367--1383",

journal = "Farmaco",

issn = "0014-827X",

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TY - JOUR

T1 - Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1

AU - Bartolucci, C.

AU - Cellai, L.

AU - Di Filippo, P.

AU - Segre, A.

AU - Brufani, M.

AU - Filocamo, L.

AU - Bianco, A. D.

AU - Guiso, M.

AU - Brizzi, V.

AU - Benedetto, A.

AU - Di Caro, A.

AU - Elia, G.

PY - 1992

Y1 - 1992

N2 - 29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.

AB - 29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.

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