Background and Aim:In an effort of drug development in the area of HIV, present work deals with development of 2D and 3D QSAR of thiazolidinone derivatives against HIV-RT activity as a powerful method for elucidation the relationships between structure and activity. Materials and Methods: 2D QSAR and 3D QSAR were performed using MLR and SA kNN method respectively. Models which had higher predictability were generated as indicated from their statistical parameters. Results and Discussion: Best models generated showed correlation coefficient r 2 = 0.9256 and q 2 =0.8623 for 2D QSAR and q 2 =0.8444 for 3D QSAR. The models indicated the requirement of electro topological, electrostatic and steric descriptors which would significantly contribute to HIV-RT inhibitory activity. Further a few compounds were designed using the outcome of QSAR studies.

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Background:: Management of Co-existence of Acquired immunodeficiency syndrome and Tuberculosis has become a global challenge due to the emergence of resistant strains and pill burden. Objective: : Hence the aim of the present work was to design and evaluate compounds for their dual activity on HIV-1 and Tuberculosis (TB). Methods: : A series of seven, novel Thiazolidin-4-one derivatives were synthesized and evaluated for their anti-HIV and anti-tubercular activity along with Molecular docking studies. All the seven compounds displayed promising activity against the replication of HIV-1 in cell-based assays. The four most active compounds were further evaluated against X4 tropic HIV-1UG070 and R5 tropic HIV-1VB59 primary isolates. The binding affinity of all the designed compounds for HIV-RT and Mycobacterium tuberculosis Enol Reductase (MTB InhA) was gauged by molecular docking studies which revealed crucial thermodynamic interactions governing their binding. Results:: The CC50 values for the test compounds were in the range of, 15.08-34.9 μg/ml, while the IC50 values were in the range of 16.1-27.13(UG070; X4) and 12.03-23.64 (VB59; R5) μg/ml. The control drug Nevirapine (NVP) exhibited CC50 value of 77.13 μg/ml and IC50 value of 0.03 μg/ml. Amongst all these compounds, compound number 3 showed significant activity with a TI value of 2.167 and 2.678 against the HIV-1 X4 and the R5 tropic virus respectively. In anti-mycobacterial screening, the compounds proved effective in inhibiting the growth of both log phase and starved MTB cultures. Conclusion: : Compound 3 has been found to be active against HIV-1 as well as MTB.

A Simple, rapid, precise and accurate stability indicating UV-Spectrophotometric method was developed for simultaneous estimation of Ilaprazole (ILA) and Domperidone (DOM) in bulk and capsule formulation and validated as per ICH guidelines. The solvent used for this method was methanol. The λmax of ILA and DOM were found to be 306 and 288 nm respectively. The linearity for ILA and DOM was in the range of 1-6 μg/ml and 3-18 μg/ml, respectively with regression coefficient(r²) of 0.999 for both drugs. The % recovery was found to be in the range of 99.29-100.87% and 99.92-100.16% for ILA and DOM respectively. Percentage RSD for precision and accuracy of the method was found to be less than 2% .LOD values for ILA and DOM were found to be 0.0866 μg/ml and 0.4026 μg/ml respectively. LOQ values for ILA and DOM were found to be 0.2625 μg/ml and 1.241 μg/ml respectively. The Forced degradation study is validated as per ICH guidelines. The developed method is suitable for the analysis of tablet formulation for quality control purposes.