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Background  Structural modifications of thiazolidinediones at 3 rd  and 5 th  position have exhibited significant biological activities. In view of the facts, and based on  in silico  studies carried out on thiazolidine-2,4-diones as HIV-1- RT inhibitors, a novel series of 2,4-thiazolidinedione analogs have been designed and synthesized.    Methods  Title compounds were prepared by the reported method. Conformations of the structures were assigned on the basis of results of different spectral data. The assay of HIV-1 RT was done as reported by Silprasit  et al.  Antimicrobial activity was determined by two fold serial dilution method. Docking study was performed for the highest active compounds by using Glide 5.0.    Results  The newly synthesized compounds were evaluated for their HIV-1 RT inhibitory activity. Among the synthesized compounds, compound  24  showed significant HIV-1 RT inhibitory activity with 73% of inhibition with an IC 50  value of 1.31 μM. Compound  10  showed highest activity against all the bacterial strains.  A molecular modeling study was carried out in order to investigate the possible interactions of the highest active compounds  24 ,  10  and  4  with the non nucleoside inhibitory binding pocket(NNIBP) of RT, active site of GlcN-6-P synthase and cytochrome P450 14-α-sterol demethylase from  Candida albicans  ( Candida  P450DM) as the target receptors respectively using the Extra Precision (XP) mode of Glide software.    Conclusion  A series of novel substituted 2-(5-benzylidene-2,4-dioxothiazolidin-3-yl)- N -(phenyl)propanamides ( 4 – 31 ) have been synthesized and evaluated for their HIV-1 RT inhibitory activity, antibacterial and antifungal activities. Some of the compounds have shown significant activity. Molecular docking studies showed very good interaction.

Synthesis, HIV-1 RT inhibitory, antibacterial, antifungal and binding mode studies of some novel N-substituted 5-benzylidine-2,4-thiazolidinediones