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- W2084727729 abstract "Syn dimeric N-benzyl 4-aryl-1,4-dihydropyridine H19 is a nonpeptidic HIV-1 protease inhibitor of the dihydroxyethylene type representing novel C2-symmetric inhibitors. Great interest was focussed on the extent of metabolism of these novel inhibitory structures as their functional groups are similar to certain peptidic and non-peptidic HIV-1 protease inhibitors with poor bioavailability due to extensive metabolism. Thus, early characterization of metabolic and toxic properties decisively determines the future prospects of those novel HIV-1 protease inhibitors. Both metabolism and toxicity were evaluated in Hep G2 monolayers. While no phase-I metabolites were found the extent of conjugation in phase-II of biotransformation was poor. Moreover, cytotoxic evaluation of protein and DNA decrease and, furthermore, of membrane toxicity characterized the novel inhibitors as non-toxic. Consequently, the favourable poor metabolism and non-toxic properties encourage further development of these novel HIV-1 protease inhibitors." @default.
- W2084727729 created "2016-06-24" @default.
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- W2084727729 date "2000-06-01" @default.
- W2084727729 modified "2023-09-27" @default.
- W2084727729 title "Bioanalysis ofSyn Dimeric HIV-1 Protease InhibitorN-Benzyl 4-Aryl-1,4-dihydropyridine H19: Metabolic and Cytotoxic Properties in Hep G2 Cells" @default.
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- W2084727729 doi "https://doi.org/10.1002/1521-4184(20006)333:6<195::aid-ardp195>3.0.co;2-4" @default.
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