Synthesis and biological evaluation of some novel 2-phenyl benzimidazole-1-acetamide derivatives as potential anthelmintic agentsThe present study describes synthesis of a series of 2-phenyl benzimidazole-1-acetamide derivatives and their evaluation for anthelmintic activity using Indian adult earthworms,Pheretima posthuma.The structure of the title compounds was elucidated by elemental analysis and spectral data. The compounds 4-({[2-(4-nitrophenyl)-1H-benzimidazol-1-yl]acetyl}amino) benzoic acid (3a),N-ethyl-2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl] acetamide (3c),N-benzyl-2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl] acetamide (3d),N-(4-hydroxyphenyl)-2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl] acetamide (3f), 2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl]-N-phenyl acetamide (3h), 2-[2-(4-chlorophenyl)-1H-benzimidazol-1-yl]-N'-phenylacetohydrazide (3k), 2-[2-(4-chlorophenyl)-1H-benzimidazol-1-yl]-N-(4-nitrophenyl) acetamide (3n) and 2-[2-(4-chlorophenyl)-1H-benzimidazol-1-yl]-N-phenyl acetamide (3q) were found better to paralyze worms whereasN-ethyl-2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl] acetamide (3c), N-(4-nitrophenyl)-2-[2-(4-nitrophenyl)-1H-benzimidazol-1-yl] acetamide (3e), 4-({[2-(4-chlorophenyl)-1H-benzimidazol-1-yl] acetyl}amino) benzoic acid (3j), 2-[2-(4-chlorophenyl)-1H-benzimidazol-1-yl]-N-ethyl acetamide (31) and 2-[2-(4-chlorophenyl)-1H-benzimidazol-1-yl]-N-phenyl acetamide (3q) were better to cause death of worms compared to the anthelmintic drug albendazole.

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Introduction:The present work aimed to develop and validate spectrophotometric methods for simultaneous estimation of rabeprazole sodium and aceclofenac in a pure and capsule dosage form.Materials and Methods:Method 1 is based on solving a simultaneous equation. Absorbances of rabeprazole sodium and aceclofenac were measured at their respective absorbance maximas (λmax) of 283 and 276 nm. Method 2 is the Q-analysis or absorption ratio method. Absorbances were measured at 256 nm (isosbestic point) and 276 nm (λmax of aceclofenac). Methods are validated according to ICH guidelines.Results:A linearity range for rabeprazole sodium and aceclofenac is 10–60 μg/ml at respective selected wavelengths. The coefficient of correlation for rabeprazole at 283 nm and for aceclofenac at 276 nm is 0.9981 and 0.9997, respectively. A percentage estimation of rabeprazole sodium and aceclofenac from the capsule dosage form by method 1 is 100.22 and 99.96 and by method 2 is 99.99 and 100.05, respectively, with a standard deviation less than 2.Conclusion:The proposed methods are simple, rapid, and validated and can be used successfully for routine simultaneous estimation of rabeprazole sodium and aceclofenac in a pure and capsule dosage form.

A series of 2-methylthio-1,4-dihydropyrimidine derivatives (IIa-IIl) were synthesized in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (Ia-Il) with methyl iodide in the presence of pyridine. Their structures were confirmed by elemental analysis, IR, and 1H NMR spectra. Molecular docking of title compounds was done using VLife MDS 3.5 on voltage-dependent calcium channel b subunit functional core and its complex with the a1 interaction domain i.e. AID-b complex (PDB code 1T3L) to identify potential candidates with minimum dock score for cardioprotective activity. Biological screening of the potential candidates (IIf and IIi) was done for cardioprotective activity. Adult Sprague-dawley rats were pretreated with test compounds IIf and IIi. After the treatment period, adrenaline was subcutaneously injected to rats at an interval of 24 h for 2 days to induce myocardial injury. After 48 h, rats were anaesthetized and electrocardiographic (ECG) observations were performed. Potential compounds IIf and IIi showed significant cardioprotective activity against adrenaline-induced myocardial infarction in rats. Adrenaline-induced ECG alterations such as reduced R-R interval, increased heart rate, reduced P duration, and ST-segment elevation were brought to the near normal values by pretreatment of compounds IIf and IIi.

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