Design synthesis and biological evaluation of thiophene 2- pentafluoro benzamide derivatives as antitubercular agent

Tuberculosis, a major contagious air-borne disease, killing millions in a year. Many of the existing anti-tubercular drugs have acquired bacterial resistance. Though they are highly bactericidal but, later on due to several factors like poor patient compliance, incomplete therapy, etc. leading to treatment relapse. This enables researcher to focus on identifying new leads utilizing structure-based drug design which plays a crucial role in drug development. The mycolic acid synthesized by Pks 13 is identified as a perfect target and hence a series of molecules were designed and the best fit ligands with a least energy were picked and analysed for Insilco bioactivity and drug likeness. Five best docked Molecules satisfied the Lipinski rule of five, namely the number of hydrogen bond donors, acceptors, log P, total polar surface area and the number of rotatable bonds. The bioactivity was found to be moderate to excellent against the receptor. The target molecules were synthesised via amino esters to yield pentafluorinated thiophene derivatives. Among the series, molecule 12 was found to be more potent when tested for antitubercular activity by Microplate Alomar blue assay technique.</jats:p

Evaluation of Physicochemical Properties and Chemical Constituents of Rasam, a Traditional South Indian Soup

Aims: To evaluate the physical and chemical properties of rasam, a traditional south Indian soup. Each ingredient present in rasam are known for their medicinal value individually. Moreover, rasam has being suggested as a general control measure in the treatment of SARS-CoV-2 by Ministry of AYUSH. For formulation designing the properties of material under study is generally determined. Hence, this study was carried out to evaluate the physiochemical properties of rasam so that it would be convenient to chose a suitable dosage form.&#x0D; Study Design: The physical and chemical studies was carried simultaneously in order to achieve the confirmatory results.&#x0D; Place and Duration of Study: Study was performed at Parul Institute of Pharmacy &amp; Research, Parul University, Vadodara, Gujarat, India. The study took about 45 days.&#x0D; Methodology: The physical parameters evaluated were pH, viscosity, density, boiling range, surface tension, miscibility, refractive index and loss on drying. The chemical evaluation included preliminary qualitative phytochemical screening.&#x0D; Results: The pH of rasam was 3.916 ±0.0133, viscosity was 0.956 cp, density was 0.993 g/mL, relative density was 0.995, boiling point was 110.3333 ± 0.333, surface tension was 107.093 N/m, refractive index was 1.37, and loss on drying was 80%. It contains several chemical constituents like alkaloids, glycosides, saponins, etc. &#x0D; Conclusion: The evaluated physical and chemical properties of rasam would provide a gateway for the formulation researchers to follow-up with various dosage forms designing.</jats:p

Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: in vitro, cytotoxicity assessment and in silico

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