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Two targeted sets of novel 1,5-diaryl-1 H -imidazole-4-carboxylic acids 10 and carbohydrazides 11 were designed and synthesized from their corresponding ester intermediates 17 , which were prepared via cycloaddition of ethyl isocyanoacetate 16 and diarylimidoyl chlorides 15 . Evaluation of these new target scaffolds in the AlphaScreen TM HIV-1 IN-LEDGF/p75 inhibition assay identified seventeen compounds exceeding the pre-defined 50% inhibitory threshold at 100 µM concentration. Further evaluation of these compounds in the HIV-1 IN strand transfer assay at 100 μM showed that none of the compounds (with the exception of 10a , 10l , and 11k , with marginal inhibitory percentages) were actively bound to the active site, indicating that they are selectively binding to the LEDGF/p75-binding pocket. In a cell-based HIV-1 antiviral assay, compounds 11a , 11b , 11g , and 11h exhibited moderate antiviral percentage inhibition of 33-45% with cytotoxicity (CC 50 ) values of &gt;200 µM, 158.4 µM, &gt;200 µM, and 50.4 µM, respectively. The antiviral inhibitory activity displayed by 11h was attributed to its toxicity. Upon further validation of their ability to induce multimerization in a Western blot gel assay, compounds 11a , 11b , and 11h appeared to increase higher-order forms of IN.

molecules/molecules online/molecules annual

Studies towards the Design and Synthesis of Novel 1,5-Diaryl-1H-imidazole-4-carboxylic Acids and 1,5-Diaryl-1H-imidazole-4-carbohydrazides as Host LEDGF/p75 and HIV-1 Integrase Interaction Inhibitors