N. Jain

1,4-Benzothiazine derivatives having variable antifungal activity against four species of fungus such as Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur  were selected to develop 2D and 3DQSAR models. The best 2DQSAR model was selected, having correlation coefficient r2 (0.8747) and cross validated squared correlation coefficient q2 (0.7145) with external predictive ability of pred_r2 (0.9658). 2DQSAR parameters are Quadrople1, SssCH2count, XA Average hydrophobicity, X Amost hydrophilic area and Polar surface area excluding P and S contributed in the model. The best 3DQSAR model having the correlation coefficient r2= 0.8635 was selected for further study. The model was further validated by means of crossed squared correlation coefficient q2 =0.7614 and pred_r2 =0.6654, which show that the model has good predictive ability and was developed by Forward SW-MLR. From QSAR model it concluded that the bulky substitution is require at para and meta position of Phenyl ring and less bulky substitution at ortho position of phenyl ring for antifungal activity.

A series of [Alkyl or un/substituted phenyl]-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazin-2-yl)acetamide were designed and synthesized. In vitro antifungal activity assay indicates that the 1,4-Benzothiazine has good antifungal activity against most of the tested pathogenic fungi i. e. Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur. Some few compounds such as BTA-43 and BTA-56 have significant antifungal activity and broader spectrum, which are promising leads for the development of novel antifungal agents. The structures of the synthesized compounds were established on the basis of IR, NMR, 13CNMR and Mass spectra data.

A simple, accurate, novel, safe and precise method has been developed for estimation of poorly water soluble drug Ziprasidone Hydrochloride using 2 M Citric acid as hydrotropic agent. After solubilizing the Ziprasidone Hydrochloride in selected hydrotropic agent, it was scanned in spectrum mode and the working wavelength for the estimation, considering the reproducibility and variability was found to be 314 nm. The developed method was found to be linear in the range of 20-100 μg/ml with correlation coefficient (r2) of 0.9997. The mean percent label claims of tablets of ZIP in formulation-I and formulation-II estimated by the proposed method were found to be 97.92±0.59 and 98.46±0.39 respectively. These values are close to 100, indicating the accuracy of the proposed analytical method. Presence of hydrotropic agent do not shows any significant interference in the spectrophotometric assay thus further confirming the applicability and reproducibility of the developed method. The developed methods were validated according to ICH guidelines and values of accuracy, precision and other statistical analysis were found to be in good accordance with the prescribed values.