- Evolution of anti-HIV drug candidates. Part 1: From α-Anilinophenylacetamide (α-APA) to imidoyl thiourea (ITU)
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Stemming from work on a previous clinical candidate, loviride, and other α-APA derivatives, a new series of potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been synthesized. The ITU analogues, which contain a unique diarylated imidoyl thiourea, are very active in inhibiting both wild-type and clinically important mutant strains of HIV-1.
- Ludovici, Donald W.,Kukla, Michael J.,Grous, Philip G.,Krishnan, Suma,Andries, Koen,De Bethune, Marie-Pierre,Azijn, Hilde,Pauwels, Rudi,De Clercq, Erik,Arnold, Edward,Janssen, Paul A.J.
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p. 2225 - 2228
(2007/10/03)
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- Serotonin antagonists
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A compound of the formula EQU1 or an acid addition salt thereof wherein R1 and R2 are the same or different and each is a phenyl or thien-2-yl group optionally substituted in one or more positions by a substituent selected from the class consisting of halogen, lower alkyl, lower alkoxy, hydroxy, lower alkylthio, phenyl, phenoxy, phenyl-(lower-alkyl) and phenyl-(lower-alkoxy), each of the said phenyl, phenoxy, phenyl-(lower-alkyl) and phenyl-(lower-alkoxy) substituent groups being optionally substituted in one or more positions by a member selected from the class consisting of halogen, lower alkyl, lower alkoxy, hydroxy, and lower alkylthio; A1 is a divalent straight or branched alkylene group containing from two to six carbon atoms and one or two divalent atoms which are each an oxygen or sulphur atom, provided that there are at least two carbon atoms between the divalent atom and the --NH-- group and between the two divalent atoms; and A2 is the methylene group --CH2 --.
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