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Synthesis of the pyrimidine analog of 4,5,6,7-tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)one (TIBO) potential for HIV-1 inhibition by Chih Y. Ho; Michael J. Kukla is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Efficent synthesis of the pyrimidine TIEtO analog 3, starting from 9-benzyl-6chloropurine and testing of its ability to inhibit the replication of the HIV-1 virus in MT-4 cells ate described. We have reported that members of a novel series of teaahydro-imidazo[4,5,1-\_ik][l,4]-benzodiazepin-2(lH)one and -thione(TIBO), such as 1 and 2, inhibit the replication of HIV-l 1.2, the main etiological agent of AIDS, but not of HIV-2, or of any other DNA or RNA viruses tested to dates-5. The unprecedented specificity of these compounds is believed to result from an interaction with reverse tmnscriptase. the tmique viral enzyme responsible for translation of HIV-1 viral RNA into DNA which is incorporated into host cells genomic DNA. Previous studies have established that 2 inhibits the isolated reverse transcriptase6. In laboratory tests, TIBO derivatives inhibited reproduction of the HIV-l virus at concentrations far below those toxic to uninfected cells. Compound 2 is currently being evaluated in clinical trials as another drug to add to anti-AIDS therapy. In the course of SAR studies to find even more potent analogs, phenyl substituents were varied and those studies will be published in th

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Author

Chih Y. Ho; Michael J. Kukla

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

1991

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)