This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Reprints and Permissions Copyright Information Books from ASM Press MicrobeWorld Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Kleim, J P Articles by Paessens, A Search for Related Content PubMed PubMed Citation Articles by Kleim, J P Articles by Paessens, A

 Previous Article  |  Next Article 

Antimicrob Agents Chemother. 1993 August; 37(8): 1659-1664

Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication.

J P Kleim, R Bender, U M Billhardt, C Meichsner, G Riess, M Rösner, I Winkler and A Paessens

SBU Antiinfectives Research, Hoechst AG, Frankfurt, Germany.

ABSTRACT

S-2720 [6-chloro-3,3-dimethyl-4-(isopropenyloxycarbonyl)-3,4- dihydroquinoxalin-2(1H)-thione], a quinoxaline derivative, was found to be a very potent inhibitor of both human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) activity and HIV-1 replication in tissue culture. Like other nonnucleoside RT inhibitors, S-2720 does not affect the HIV-2 RT. A S-2720-resistant virus was selected and shown to possess a mutation within the RT-coding region that has not previously been described. Notably, this mutation gives rise to a dramatic decrease in enzyme activity. S-2720, therefore, belongs to a new class of RT inhibitors that bind differently to the RT than other known nonnucleoside RT inhibitors. As no toxic effects were observed with S-2720 in mice, these quinoxaline derivatives deserve further evaluation to prove their potency as possible therapeutic agents for HIV-1 infection.

---

Antimicrob Agents Chemother. 1993 August; 37(8): 1659-1664

This article has been cited by other articles:

• Huang, W., Gamarnik, A., Limoli, K., Petropoulos, C. J., Whitcomb, J. M. (2002). Amino Acid Substitutions at Position 190 of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Increase Susceptibility to Delavirdine and Impair Virus Replication. J. Virol. 77: 1512-1523 [Abstract] [Full Text]  
• Ren, J., Nichols, C., Bird, L. E., Fujiwara, T., Sugimoto, H., Stuart, D. I., Stammers, D. K. (2000). Binding of the Second Generation Non-nucleoside Inhibitor S-1153 to HIV-1 Reverse Transcriptase Involves Extensive Main Chain Hydrogen Bonding. J. Biol. Chem. 275: 14316-14320 [Abstract] [Full Text]  
• Witvrouw, M., Arranz, M. E., Pannecouque, C., Declercq, R., Jonckheere, H., Schmit, J.-C., Vandamme, A.-M., Diaz, J. A., Ingate, S. T., Desmyter, J., Esnouf, R., Van Meervelt, L., Vega, S., Balzarini, J., De Clercq, E. (1998). 1,1,3-Trioxo-2H,4H-Thieno[3,4-e][1,2,4]Thiadiazine (TTD) Derivatives: a New Class of Nonnucleoside Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase Inhibitors with Anti-HIV-1 Activity. Antimicrob. Agents Chemother. 42: 618-623 [Abstract] [Full Text]  
• Boyer, P. L., Gao, H.-Q., Hughes, S. H. (1998). A Mutation at Position 190 of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Interacts with Mutations at Positions 74 and 75 via the Template Primer. Antimicrob. Agents Chemother. 42: 447-452 [Abstract] [Full Text]  
• Balzarini, J., Pelemans, H., Karlsson, A., De Clercq, E., Kleim, J.-P. (1996). Concomitant combination therapy for HIV infection preferable over sequential therapy with 3TC and non-nucleoside reverse transcriptase inhibitors. Proc. Natl. Acad. Sci. USA 93: 13152-13157 [Abstract] [Full Text]