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A large variety of carboxanilide derivates in which the original oxathiin moiety present in the prototype compound UC84 was replaced by a non-cyclic lipophilic entity has been evaluated for their inhibitory effect against wild-type human immunodeficiency virus type 1 (HIV-1/IIIB) and several mutant viruses derived thereof (i.e. HIV-1/138-Lys, HIV-1/181-Cys, HIV-1/106-Ala and HIV-1/100-IIe). Isopropoxy was the most favorable substituent resulting in molecules that were markedly inhibitory to the wild-type (EC50 0.004-0.04 microgram/ml) as well as the mutant HIV-1 strains (EC50 0.06-0.75 microgram/ml). In this respect, they proved superior to several other HIV-1-specific non-nucleoside reverse transcriptase inhibitors (NNRTIs) that are currently the subject of clinical trials. One of the most potent HIV-1 inhibitors among the thiocarboxanilide derivatives, namely UC38, selected for a mutant virus strain in which Lys at position 101 and Gly at position 190 of the reverse transcriptase was replaced by Glu.
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
April 1995,
Antimicrobial agents and chemotherapy,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
December 1990,
Journal of virology,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
June 1993,
Journal of virology,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
December 1994,
Journal of virology,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
February 1999,
Antimicrobial agents and chemotherapy,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
January 1989,
Journal of acquired immune deficiency syndromes,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
October 1998,
Virology,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
November 2004,
Biochemistry,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
March 1996,
Antiviral research,
J Balzarini, and
W G Brouwer, and
E E Felauer, and
E De Clercq, and
A Karlsson
December 1995,
Antiviral research,
