Synthesis of new 2,2-dimethyl-2H-chromen derivatives as potential anticancer agents

874-880The synthesis of some new heterocyclic derivatives comprising imidazothaidiazole, diaryl ketone and chromen as starting compound has been reported. The new series of chromen analogues have been synthesized. The reaction has been monitored by Thin Layer Chromatography (TLC) using suitable mobile phase. The Rf values have been compared and the melting points of derivatives determined. Further, these derivatives have been characterized and confirmed by IR, 1H NMR and mass spectral (MS) studies. All the selected compounds submitted to National Cancer Institute (NCI) for in vitro anticancer assay have been evaluated for their anticancer activity

Development and Validation of Stability Indicating Reverse Phase High Performance Liquid Chromatographic Method for estimation of Donepezil HCl from bulk drug

Stability of Donepezil Hydrochloride(DONE) was investigated using stability indicating Reverse phase high performance liquid chromatography (RP-HPLC) utilizing C-18 column and mobile phase containing Acetonitrile:Water (pH 3.5)  in ratio of 40:60 at flow rate of 1 ml min-1. Peaks of donepezil and degradation products were well resolved at retention times < 7 min. Stability was performed in 0.1N hydrochloric acid, 0.1N sodium hydroxide, 3 % hydrogen peroxide, neutral, photolytic and dry heat conditions. Fast hydrolysis was seen in alkaline condition as compared to oxidative and neutral conditions. Methods was validated with respect to linearity, precision, accuracy, specificity and robustness LOQ and LOD. It was also found to be stability indicating, and therefore suitable for the routine analysis of Donepezil hydrochloride in the pharmaceutical formulation

2D QSAR STUDIES ON THE DIFFERENTIAL INHIBITION OF ALDOSE REDUCTASE BY FLAVONIODS COMPOUNDS:A COMPARATIVE STUDY

A quantitative structure activity relationship study of  66 molecules was performed using MLR(Multiple Linear Regression) and PCR (Principal component Analysis) of aldose reductase by flavonoids compounds.Various descriptors, topological indices were used to characterize flavonoids molecules.In the developed model MLR is giving vary significant results wheras PCR  has revealed some important information. Keywords: Flavonoids, aldose reuctase, QSAR, Multiple Linear Regression, Principle Component Regressio

Synthesis of new 2,2-dimethyl-2H-chromen derivatives as potential anticancer agents

The synthesis of some new heterocyclic derivatives comprising imidazothaidiazole, diaryl ketone and chromen as starting compound has been reported. The new series of chromen analogues have been synthesized. The reaction has been monitored by Thin Layer Chromatography (TLC) using suitable mobile phase. The Rf values have been compared and the melting points of derivatives determined. Further, these derivatives have been characterized and confirmed by IR, 1H NMR and mass spectral (MS) studies. All the selected compounds submitted to National Cancer Institute (NCI) for in vitro anticancer assay have been evaluated for their anticancer activity.

Synthesis, and antimicrobial evaluation of new pyridine imidazo [2,1b]-1,3,4-thiadiazole derivatives

With the aim of producing new biologically active compounds, a series of New Pyridine Imidazo [2,1b]-1,3,4-thiadiazole derivatives 4(a–k) were synthesized. All the compounds were characterized via IR, 1H-NMR and Mass spectral studies. The antimicrobial activity of newly synthesized compounds against various bacteria; Bacillus pumillus, Staphylococcus aureus, Vibrio cholera, Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, and fungi; Candida albicans were evaluated. Among the compounds tested, 4(a), 4(b), 4(f), 4(h) and 4(k) exhibited good antimicrobial activity while others responded moderately with reference to standard drugs ampicillin and amphotericin B

Synthesis and antimicrobial evaluation of novel 1,3,4-thiadiazole derivatives of 2-(4-formyl-2-methoxyphenoxy) acetic acid

A series of 1,3,4-thiadiazole derivatives of 2-(4-formyl-2-methoxyphenoxy) acetic acid (6a–s) were synthesized by cyclization of carboxylic acid group of 2-(2-methoxy-4-(3-oxo-3-substituted phenylprop-1-enyl)phenoxy) acetic acid (4a–s) with thiosemicarbazide in the presence of POCl3 or PPA. The structures of the compounds were confirmed by IR, 1H NMR and mass analysis. All the compounds have been evaluated in vitro for their antimicrobial activities against several strains of microbes and show significant activity

Synthesis and antitubercular evaluation of imidazo[2,1-b][1,3,4]thiadiazole derivatives

In the present study, a series of imidazo[2,1-b][1,3,4]thiadiazole derivatives 5(a–j) were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral technique. The compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain by using Alamar Blue susceptibility test as part of the TAACF TB screening program under direction of the US National Institutes of Health, the NIAID division. Among the tested compounds, 2-(1-methyl-1H-imidazol-2-yl)-6-(4-nitrophenyl)imidazo[2,1-b][1,3,4]thiadiazole (5f) has shown the highest (98%) inhibitory activity with MIC of 3.14 μg/ml as compared to other tested compounds. Further, some potent compounds were also assessed for their cytotoxic activity against a mammalian Vero cell line using MTT assay. The results reveal that these compounds exhibit anti-tubercular activity at non-cytotoxic concentrations