Compounds bearing thiazole and chalcone pharmacophores have been reported to possess excellent antitubercular and anticancer activities. In view of this, we designed, synthesized and characterized a novel series of thiazole−chalcone hybrids (1–20) and further evaluated them for antitubercular and antiproliferative activities by employing standard protocols. Among the twenty compounds, chalcones 12 and 7, containing 2,4-difluorophenyl and 2,4-dichlorophenyl groups, showed potential antitubercular activity higher than the standard pyrazinamide (MIC = 25.34 µM) with MICs of 2.43 and 4.41 µM, respectively. Chalcone 20 containing heteroaryl 2-thiazolyl moiety exhibited promising antiproliferative activity against the prostate cancer cell line (DU-145), higher than the standard methotrexate (IC50 = 11 ± 1 µM) with an IC50 value of 6.86 ± 1 µM. Furthermore, cytotoxicity studies of these compounds against normal human liver cell lines (L02) revealed that the target molecules were comparatively less selective against L02. Additional computational studies using AutoDock predicted the key binding interactions responsible for the activity and the SwissADME tool computed the in silico drug likeliness properties. The lead compounds generated through this study, create a way for the optimization and development of novel drugs against tuberculosis infections and prostate cancer.
Two simple, accurate, economical and reproducible UV spectrophotometric and one HPLC method for simultaneous estimation of two-component drug mixture of pseudoephedrine hydrochloride and loratadine in combined tablet dosage form have been developed. The first developed method employs multiwavelength spectroscopy using seven mixed standards and 257.0 nm and 283.0 nm as two wavelengths for estimation. The second method involves first derivative spectroscopy using 308.6 nm and 263.0 nm as zero crossing points for pseudoephedrine hydrochloride and loratadine respectively. For both spectrophotometric methods, 0.2 M hydrochloric acid was used as solvent. Linearity was observed in concentration range of 0-40 µ
Two simple and sensitive visible spectrophotometric methods have been developed for the quantitative estimation of ketotifen fumarate from its tablet formulation. The developed methods are based on formation of chloroform extractable colored complex of with 2-nitroso- napthol-4- sulphonic acid and rhodizonic acid. The extracted complex of drug with 2-nitroso- napthol-4- sulphonic acid (method-I), showed absorbance maxima at 436.5 nm and with rhodizonic acid (method-II), showed absorbance maxima at 489.5 nm. The linearity range for both the developed methods was observed in the concentration range of 50-250 µg/ml of drug. Results of analysis for both the developed methods were validated statistically and by recovery studies.
Objective: Commonly used organic solvents for spectrophotometric analysis of water-insoluble drugs are methanol, ethanol, chloroform, benzene, toluene etc. The main drawbacks of organic solvents include high cost, toxicity, and pollution. Organic solvents have numerous adverse effects caused by single exposure like dermatitis, headache, drowsiness, nausea, eye irritation and long-term exposure causes serious effects such as neurological disorder, chronic renal failure, and liver damage. They should be replaced by other eco-friendly alternative sources.
Methods:The present study is an attempt to show that solid can also be used to act as solvent precluding the use of organic solvents. A simple, safe and sensitive method of spectrophotometric determination of diazepam obeyed beers law in the concentration range of 5-25 mcg/ml at 306 nm.
Results:The results of analyses have been validated statistically for Linearity, accuracy, precision, LOD and LOQ. The results of validation parameters also indicated that proposed method was found to be accurate, precise, reproducible, sensitive, and suitable for routine quality control analysis for estimation of diazepam in bulk drug and solid dosage formulation.
Conclusion:A rapid, simple, and non-toxic UV spectrophotometric method has been developed for the determination and quantification of diazepam. The present method also validated as per ICH guidelines for linearity, precision, accuracy.
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