- SYNTHESES OF RACEMIC AND ENANTIOMERIC (S)-(+)-4,5,6,7-TETRAHYDRO-5-METHYL-IMIDAZOBENZODIAZEPIN-2(1H)-ONE DERIVATIVES
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Racemic and enantiomeric (S)-(+)-4,5,6,7-tetrahydro-5-methylimidazobenzodiazepin-2(1H)-one derivatives were prepared using free amino acids and 3-nitroisatoic anhydride.Simultaneous reduction of two amide functions was efficiently achieved
- Pfaendler, Hans Rudolf,Weisner, Frank
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p. 717 - 728
(2007/10/02)
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- Anti-HIV-1 tetrahydroimidazo[1,4]benzodiazepin-2-(thi) ones
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Novel tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing anti-HIV-1 activity, compositions containing these compounds as active ingredients, and methods of treating subjects suffering from HIV-1 infection by administering these compounds. The comp
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- Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazobenzodiazepin-2(1H)-one (TIBO) Derivatives
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A series of 6-substituted 4,5,6,7-tetrahydro-5-methylimidazobenzodiazepin-2(1H)-ones (9) have been synthesized and tested for their ability to inhibit the replication of the HIV-1 virus in MT-4 cells.Two synthetic methods are described, one of which allows the synthesis of single enantiomers of the final products.A structure-activity study was done within the series of compounds to determine the optimum group for the 6-position substitution and to determine whether the activity was enantiospecific at the 5-position, which was substituted with a methyl group.The best analogue, 9jj, inhibited HIV-1 with an IC50 of 4 μM, which is comparable to the activity level of DDI, a 2',3'-dideoxynucleoside-type structure undergoing clinical trials as an anti-AIDS therapy.
- Kukla, Michael J.,Breslin, Henry J.,Pauwels, Rudi,Fedde, Cynthia L.,Miranda, Milton,et al.
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p. 746 - 751
(2007/10/02)
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