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Abstract The present thesis dealt with design and synthesis of certain derivatized anthranilamide dimers 2-(2-acylamino)benzamido)benzoic acid 5a-n and their cyclic congeners N-(2-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl)acylamide6a-n and evaluation of their HIV-1 RT inhibitory activity using reverse transcriptase enzyme as a target and nevirapine as a reference drug. The thesis included four main parts; introduction, scope of investigation, results and discussion and the experimental part.The introduction gave an overview on HIV infections, AIDS, including recent statistics of AIDS patients worldwide in general and in Egypt in particular. Introduction also presented an overview on HIV life cycle including drugs used for treatment of HIV classified according to mechanism of action (inhibition of different steps of HIV life cycle) focusing on NNRTIs like (HEPT, TIBO, DABOs, BHAP, dipyridodiazepinones and benzoxazinones).A brief on resistance mutation of HIV-1 RT was presented. This resistance mutation of HIV-1 RT was the engine for continuous development of next generation NNRTIs.The scope of investigation displayed the scheme of synthesis of anthranilic acid amide dimers and their cyclized congeners (4H-benzo[d][1,3]oxazin-4-one derivatives). |