PMID: 7541619Mar 1, 1995Paper

The inhibition of human immunodeficiency virus type 1 in vitro by a non-nucleoside reverse transcriptase inhibitor MKC-442, alone and in combination with other anti-HIV compounds

Antiviral Research
T M BrennanA S Tyms

Abstract

MKC-442, a derivative of the non-nucleoside reverse transcriptase (RT) inhibitor 1-[(2-hydroxyethoxy)methyl)-6-(phenylthio)thymidine (HEPT), showed potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) replication in vitro, using a range of host-cell/virus systems including human peripheral blood mononuclear cells infected with primary clinical isolates. MKC-442 was evaluated in combination with the nucleoside analogues AZT, ddI and ddC, the non-nucleoside RT inhibitor nevirapine, the HIV-1 proteinase inhibitor Ro-31-8959, and the alpha-glucosidase 1 inhibitor, MDL-28,574, using a cell viability assay. Drug interactions were evaluated by the isobologram technique and by calculating combination indices. Notable synergistic inhibition of HIV-1 replication was observed when MKC-442 was combined with AZT and MDL-28,574 and moderate synergy with ddI. In combination with ddC, nevirapine or Ro-31-8959, only a slightly better than additive effect was observed. Impressive synergy was seen using the three-drug combinations of MKC-442, AZT and MDL-28,574 or MKC-442, AZT and Ro-31-8959. No additional cytotoxicity was observed as measured by [3H]thymidine incorporation by concanavalin A-stimulated peripheral blood m...Continue Reading

References

Aug 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·M E GoldmanJ M Hoffman
Oct 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·D L RomeroL Resnick
Dec 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·D RichmanJ Griffin
Apr 20, 1990·Science·N A RobertsA Kröhn
Nov 23, 1990·Science·J P MooreQ J Sattentau
Aug 1, 1988·Journal of Virological Methods·R PauwelsE De Clercq
Dec 1, 1989·Journal of Medicinal Chemistry·T MiyasakaE De Clercq
Dec 29, 1989·Biochemical and Biophysical Research Communications·M BabaT Miyasaka
Jun 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·M TisdaleB A Larder
Aug 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·M J OttoY S Cheng

❮ Previous
Next ❯

Citations

May 25, 1999·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·P BonfantiG Rizzardini
Jun 10, 2003·Acta Microbiologica Et Immunologica Hungarica·A Aszalos
Jun 8, 2013·Antiviral Chemistry & Chemotherapy·Pinar Iyidogan, Karen S Anderson
Jun 26, 2013·Antimicrobial Agents and Chemotherapy·Atsuko HachiyaStefan G Sarafianos
Jun 27, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Monique Araújo de BritoMagaly Girão Albuquerque

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antivirals

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Antivirals (ASM)

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.