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Titolo:
Structure-activity relationship studies on potential non-nucleoside DABO-like inhibitors of HIV-1 reverse transcriptase
Autore:
Costi, R; Di Santo, R; Artico, M; Massa, S; Lavecchia, A; Marceddu, T; Sanna, L; La Colla, P; Marongiu, ME;
Indirizzi:
Univ Rome La Sapienza, Dipartimento Studi Farmaceut, Ist Pasteur Fdn CenciBolognetti, Rome, Italy Univ Rome La Sapienza Rome Italy steur Fdn CenciBolognetti, Rome, Italy Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy Univ Siena Siena Italy I-53100 Farmaco Chim Tecnol, I-53100 Siena, Italy Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, Naples, Italy Univ Naples Federico II Naples Italy armaceut & Tossicol, Naples, Italy Univ Cagliari, Sez Microbiol, Dipartimento Med Sperimentale, I-09042 Cagliari, Italy Univ Cagliari Cagliari Italy I-09042 erimentale, I-09042 Cagliari, Italy
Titolo Testata:
ANTIVIRAL CHEMISTRY & CHEMOTHERAPY
fascicolo: 2, volume: 11, anno: 2000,
pagine: 117 - 133
SICI:
0956-3202(200003)11:2<117:SRSOPN>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
IMMUNODEFICIENCY-VIRUS TYPE-1; 6-SUBSTITUTED ACYCLOURIDINE DERIVATIVES; ANTI-HIV-1 ACTIVITY; HIGHLY POTENT; 1-<(2-HYDROXYETHOXY)METHYL>-6-(PHENYLTHIO)THYMINE HEPT; 3,4-DIHYDRO-2-ALKOXY-6-BENZYL-4-OXOPYRIMIDINES DABOS; SELECTIVE-INHIBITION; ANTIVIRAL ACTIVITY; DEOXY ANALOGS; SERIES;
Keywords:
DABO derivatives; NNRTIs; HEPT-like derivatives; pyrimidine derivatives;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Artico, M Univ Rome La Sapienza, Dipartimento Studi Farmaceut, Ist PasteurFdn CenciBolognetti, Rome, Italy Univ Rome La Sapienza Rome Italy CenciBolognetti, Rome, Italy
Citazione:
R. Costi et al., "Structure-activity relationship studies on potential non-nucleoside DABO-like inhibitors of HIV-1 reverse transcriptase", ANTIVIR CHE, 11(2), 2000, pp. 117-133

Abstract

Using 2,6-dichloro-4-aminopyrimidine, a number of uracil and cytosine derivatives with both arylthio and alkoxy moieties were prepared. These novel pyrimidines share chemical similarities with DABOs and HEPTs, two classes ofnonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors (NNRTIs), which have been widely studied of late. All new derivatives were tested in MT-4 cells to explore their potential in vivo anti-HIV activity. Like other NNRTIs, they selectively inhibit HIV-1 but not HIV-2. The majority of test derivatives were found to have low potency and were sometimes more cytotoxic than zidovudine and emivirine (formerly MKC-442), used here as reference drugs. Uracil and cytosine derivatives bearing a sec-butoxy chain and a methyl-substituted benzenesulphonyl moiety were the most potent. Enzyme assays proven that these derivatives target RT. Structure-activity relationship studies established a correlation between the anti-HIV-l activity and the meta substitution on the phenyl ring; furthermore, oxidation of sulphide to sulphone significantly increased the potency of certain derivatives.

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Documento generato il 30/09/20 alle ore 09:22:22