Pharmaceutical Chemistry

Efficient synthesis of some new N-Benzyl substituted benzimidazole chalcone derivatives were performed by multistep reaction sequences. The synthesized compounds were characterized using IR, 1 H NMR, mass spectrometry and elemental analysis. The synthesized compounds were screened for their antibacterial activity against selective gram positive and gram negative bacteria. Compound 10 was found to be most active among the series.

A novel series of 2-Benzyl substituted benzimidazole acetohydrazone derivatives was synthesized by multistep reaction sequences. The synthesized compounds were characterized using IR, 1 H NMR, mass and elemental analysis. Antibacterial activities of the compounds were evaluated against selective gram positive and gram negative bacteria. Compound 7 was found to be most active among the series.

Background: Emergence of resistance to accessible anticancer drugs became a threat to human lives in the recent time. To address this issue, discovery of novel anticancer agents becomes very essential. Benzimidazoles and pyrimidines have been reported to possess potent anticancer activity. Material and Methods: A hybrid approach has been used, in which core structure of potentially active N-benzyl benzimidazole and pyrimidine derivatives are brought together in to a single molecule. The desired compounds were prepared by the condensation of N-benzyl benzimidazole chalcones with guanidine hydrochloride. The synthesized compounds were characterized using spectral studies (IR, 1H, 13C-NMR techniques and mass spectrometry). All the compounds were screened for their anticancer activity against human breast cancer cell line MDA-MB-231. Results: The spectral data’s are in well agreement with the synthesized compounds 5a-e. Compounds 5b (GI50 = 39.6 μM) and 5a (GI50=84.0 μM) exhibited significant anticancer activity. Conclusion: Owing to the anticancer activity, compound 5b can be used as lead structure in the development of yet more potent anticancer agents.

Objective: The objective of the present work is to develop and validate a new UV derivative spectrophotometric method for simultaneous estimation of metoprolol succinate and ramipril in methanol: water (50:50v/v). Methods: "Zero crossing technique" was chosen for quantitative determination. The zero-crossing points (ZCP's) were found to be 209 nm where metoprolol succinate was quantified and 211 nm where ramipril was quantified. This method was then subjected to accuracy, linearity, sensitivity and reproducibility according to ICH guidelines to ensure and confirm its validity. Results: The method was found to be obeying Beer's law in the range of 10-50 µg/ml and 5-25 µg/ml for metoprolol succinate and ramipril, respectively. The % recoveries were observed between the range of 99.2-100.2 for metoprolol succinate and 99.57-99.86 for ramipril. The intra-day and inter-day results showed reproducibility. Conclusion: It can be concluded that the developed third-order UV derivative spectroscopic method for the simultaneous determination of metoprolol succinate and ramiprilcan be recommended for routine quantitative analysis.

A simple, selective, linear, precise and accurate RP-HPLC method was developed and validated for rapid assay of Ritonavir in pharmaceutical dosage form. Isocratic elution at a flow rate of 1ml/min was employed on a symmetry C18 column at ambient temperature. The mo bile phase consisted of acetonitrile: methanol: buffer 50:35:15 (V/V). The UV detection wavelength was at 252 nm. Linearity was observed in concentra tion range of 5-150 ppm. The retention time for Ritonavir was 5.32 min. The method was validated as per the ICH guidelines. The proposed method can be successfully applied for the estimation of Ritonavir in pharmaceutical dosage forms.

The present study was undertaken to evaluate the Anthelmintic activity of ethanol extracts of Zingiber officinalis (Zingiberacae), Zingiber zerumbet (Zingiberacae) and Curcuma longa on Indian earthworm, Pheretima posthuma.Various concentrations (10ug/ml, 25ug/ml, 50ug/ml) of all extracts were tested and results were expressed in terms of time of paralysis and time of death of the earthworm. Piperazine citrate (10ug/ml) was used as reference standard and sterile water as control group

The medicinal plants are widely used by the traditional medical practitioners for curing various diseases. Helminthiasis is the most common infection in human affecting a large proportion of world population. Parasitic diseases may cause severe morbidities including lymphatic filariasis and onchocerciasis. Development of resistance to most of the commercially available anti helminthiasis becomes a severe problem worldwide. The present study was under taken to evaluate antihelmenthic activity of ethanol extract of seeds of Cucurbita maxima, Moringa olifera and fruits of Solanum surattense on Indian earthworm pheritima phosthuma. Various concentrations (10, 25, 50 mg/ml) of extracts
were tested and results were expressed in terms of time of paralysis and time of death of the worm. Piperazine citrate (10mg/ml) is used as reference standard and saline water as control.

A reverse phase HPLC method was successfully developed and validated for concurrent assessment of omeprazole and aspirin for bulk and pharmaceutical formulation. The method was developed employing a reversed phase C 18 column. A optimized mobile phase having a composition of acetonitrile-methanol (20:80 v/v) was used. The experiment was carried out at flow rate of 0.6 ml/min and wavelength of 233 nm. Retention times for omeprazole and aspirin were found at 2.667 and 1.720 min respectively. Across a concentration span of 10-50 µg/ml and 5-25 µg/ml the method was linear for aspirin and omeprazole, respectively. The proposed method have potential for the regular quality scrutiny of this combination in bulk and pharmaceutical dosage form.

The present study was undertaken to evaluate Anthelmintic activity of petroleum ether and alcoholic extracts of whole plant of Tephrosia purpurea against Pheretima posthuma and Ascardi galli. Various concentrations (10, 25 and 50 mg/ml) of extracts were evaluated and results were expressed in terms of time of paralysis (P) and time of death (D) for both types of worms. Piperazine citrate was used as a s tandard Anthelmintic drug and distilled water was used as control. The results of present study indicated that the alcoholic and petroleum ether extract exhibited paralysis and death of worms. Further studies are in process to isolate the active principles responsible for the activity.

Benzimidazole is an important moiety from a medicinal chemistry perspective due to its various biological activities such as antimicrobial, anti-cancer, anti-diabetic, anti-Alzheimers, and anti-inflammatory, etc. 2-acetylbenzimidazole is exploited to obtain various heterocyclic compounds of pharmacological interest. This review's main motive is to present the literature on 2-acetylbenzimidazole chemistry and provide valuable and up-to-date information for its applications. The present review is carried out by compiling literature from 1964 to 2020 concerning the synthesis and biological aspects of various heterocyclic compounds derived from 2-acetylbenzimidazole. Literature was collected from various online search engines viz. Google Scholar, PubMed, Science Direct, Core, and Semantic scholar. 2-acetylbenzimidazole has been successfully employed as a synthon to obtain heterocyclic system viz. oxirane, pyrazoline, thiazole, pyrazole, isoxazoline, isoxazole, pyridine, pyrimidine, thiazine, diazepine, and other miscellaneous rings. 2-acetylbenzimidazole has shown promise for the convenient synthesis of various heterocyclic compounds. The reactions can be carried out on various reactive sites of 2-acetylbenzimidazole, which are the carbonyl group and the amino group. This review will help to explore various heterocyclic compounds and particularly in the synthesis of biologically useful compounds.

ã2020 Published by HOPE on behalf of RJPLS This is an open access article under the CC-BY-NC-ND License. ______________________ * Corresponding author: Gopal Krishna Padhy, Department of Pharmaceutical Chemistry, School of Pharmacy, Centurion University of Technology and Management, Pitamahal, Rayagada, Odisha-765002, India. E mail ID: gopalmedchem@gmail.com Introduction Aspirin (ASP), a non-steroidal antiinflammatory (NSAID) medication indicated to cure pain, inflammation and fever ( Figure 1). Due to it’s antithrombotic action, aspirin is also given to decreases the incidence of heart failure and used in long term basis to prevent strokes and heart attacks. Omeprazole (OME, Figure 2), a selective and irreversible proton pump inhibitor indicated in the treatment of peptic ulcer and Zollinger–Ellison syndrome.

Spathodea campanulata P. Beauv., belonging to the family Bignoniaceae, is a big erect tree with an ancient history of medicinal use in Africa. In the traditional system, it is mentioned for the treatment of malaria, diabetes, stomach ulcers, wounds, skin infections and viral diseases. The aim of the review is to make available the current information that exists on the traditional uses, phytochemistry, pharmacology, and toxicology of S. campanulata. Additionally, the potential uses of this plant to treat various diseases and to bring in a foundation for further research are emphasized. The present review is carried out by compiling literature from 1972 to 2021, concerning the morphology, traditional uses, phytochemistry, pharmacological activities, and toxicological aspects of S. campanulata. Literatures were collected from various online search engines, viz. Google Scholar, PubMed, Science Direct, Core, and Semantic Scholar. Diverse chemical compounds including iridoids, terpenoids, steroids, cinnamic acid derivatives, cerebrosides, flavonoids, and carotenoids have been isolated from this plant. Mostly in-vivo models have indicated several evidences of the use of this plant particularly to cure malaria. Few in-vivo studies have also proved the usefulness of this plant in inflammation, wound healing, diabetes, and convulsion. In some in-vitro studies, the anticancer, antibacterial, antiviral insecticidal, larvicidal, and anti-oxidant potential has been proved. Preclinical studies have demonstrated remarkable activity which supports the conventional use of the plant as an antimalarial, wound healing, antidiabetic, antimicrobial, and anti-inflammatory agent for years without any adverse effects. Based on the results obtained from a combination of in vivo and in vitro potency and toxicity studies reported, S. campanulata is a promising agent in the development of nutraceuticals against malaria and diabetes. Although few phytochemicals isolated (ursolic acid, tomentosolic acid, 20β-hydroxyursolic acid, verminoside, specioside, spathoside, kaempferol, and β-sitosterol-3-acetate) from the plant exhibited remarkable biological activity, it was only confined to preclinical study. The only clinical study documented is for curing malaria, but with crude extract only. With its current extensive traditional use, there is a need for additional studies of the isolated compounds, clinical trials, and product development to take full advantage of this widely distributed medicinal plant.

Benzimidazole is an important moiety from a medicinal chemistry perspective due to its various biological activities such as antimicrobial, anti-cancer, anti-diabetic, anti-Alzheimers, and anti-inflammatory, etc. 2-acetylbenzimidazole is exploited to obtain various heterocyclic compounds of pharmacological interest. This review's main motive is to present the literature on 2-acetylbenzimidazole chemistry and provide valuable and up-to-date information for its applications. The present review is carried out by compiling literature from 1964 to 2020 concerning the synthesis and biological aspects of various heterocyclic compounds derived from 2-acetylbenzimidazole. Literature was collected from various online search engines viz. Google Scholar, PubMed, Science Direct, Core, and Semantic scholar. 2-acetylbenzimidazole has been successfully employed as a synthon to obtain heterocyclic system viz. oxirane, pyrazoline, thiazole, pyrazole, isoxazoline, isoxazole, pyridine, pyrimidine, ...

Objective: The objective of the present work is to develop and validate a new UV derivative spectrophotometric method for simultaneous estimation of metoprolol succinate and ramipril in methanol: water (50:50v/v). Methods: “Zero crossing technique” was chosen for quantitative determination. The zero-crossing points (ZCP’s) were found to be 209 nm where metoprolol succinate was quantified and 211 nm where ramipril was quantified. This method was then subjected to accuracy, linearity, sensitivity and reproducibility according to ICH guidelines to ensure and confirm its validity. Results: The method was found to be obeying Beer’s law in the range of 10-50 µg/ml and 5-25 µg/ml for metoprolol succinate and ramipril, respectively. The % recoveries were observed between the range of 99.2-100.2 for metoprolol succinate and 99.57-99.86 for ramipril. The intra-day and inter-day results showed reproducibility. Conclusion: It can be concluded that the developed third-order UV derivative spectro...

A novel series of 2-Benzyl substituted benzimidazole acetohydrazone derivatives was synthesized by multistep reaction sequences. The synthesized compounds were characterized using IR, 1H NMR, mass and elemental analysis. Antibacterial activities of the compounds were evaluated against selective gram positive and gram negative bacteria. Compound 7 was found to be most active among the series.