Background:
Benzimidazole is the fused heterocyclic aromatic compound. It is an essential
pharmacophore and privileged structure for the development of new drug molecules. These are
bioactive molecules present in various anthelmintic drugs such as albendazole, mebendazole, parbendazole,
triclabendazole etc.
Methods:
Benzimidazole derivatives are synthesized by reaction between orthophenylene diamine
and anthranillic acid followed by acetylation in the presence of acetic anhydride. Finally, the acetylated
products undergo Claisen-Schimdt condensation with various substituted benzaldehydes to produce
corresponding benzimidazole derivatives or chalcones. Both conventional and microwave irradiation
technology are followed to get the titled compounds. The titled compounds are screened for
their anticonvulsant and neurotoxicity activity.
Results:
By the help of microwave synthesis, the yield of product was increased in less reaction time.
So, it follows Green chemistry approach by making above reactions eco-friendly. Some of the compounds
exhibited significant anticonvulsant activity as compared to standard drug.
Conclusion:
In the present investigation, we have synthesized novel benzimdazole derivatives with
chalone moiety to improve the biological activity. The compounds were obtained under microwave
reaction with high yield in a short reaction time.
A simple, Accurate, precise method was developed for the simultaneous estimation of the Sofosbuvir and Ledipasvir in Tablet dosage form. Chromatogram was run through Std Discovery C8 150 x 4.6 mm, 5m. Mobile phase containing Buffer 0.1% OPA: Acetonitrile taken in the ratio 60:40 was pumped through column at a flow rate of 1 ml/min. Buffer used in this method was 0.1% OPA buffer. Temperature was maintained at 30°C. Optimized wavelength selected was 260 nm. Retention time of Sofosbuvir and Ledipasvir were found to be 2.367 min and 3.436 min. %RSD of the Sofosbuvir and Ledipasvir were and found to be 0.6 and 0.5 respectively. %Recovery was obtained as 99.61% and 99.80% for Sofosbuvir and Ledipasvir respectively. LOD, LOQ values obtained from regression equations of Sofosbuvir and Ledipasvir were 0.67, 2.02 and 0.70, 2.12 respectively. Regression equation of Sofosbuvir is y = 4266.x + 7700, and y = 4861.x + 2656.of Ledipasvir. Retention times were decreased and run time was decreased, so the method developed was simple and economical that can be adopted in regular Quality control test in Industries.
A simple, rapid, precise, sensitive and reproducible reverse phase high performance liquid chromatography (RP-HPLC) method has been developed for the quantitative analysis of Dolutegravir and Rilpivirine in pharmaceutical dosage form. Chromatographic separation of Dolutegravir and Rilpivirine was achieved on Waters Alliance -2695, by using Luna C18 (250mm x 4.6mm, 5µm) column and the mobile phase containing 0.1% OPA & ACN in the ratio of 50:50 v/v. The flow rate was 1.0 ml/min, detection was carried out by absorption at 245 nm using a photodiode array detector at ambient temperature. The number of theoretical plates and tailing factor for Dolutegravir and Rilpivirine were NLT 2000 and should not more than 2 respectively. The linearity of the method was excellent over the concentration range 10-150 µg/ml and 5-75 µg/ml for Dolutegravir and Rilpivirine respectively. The correlation coefficient was 0.999. % Relative standard deviation of peak areas of all measurements always less than 2.0. The proposed method was validated according to ICH guidelines. The method was found to be simple, economical, suitable, precise, accurate & robust method for quantitative analysis of Dolutegravir and Rilpivirine study of its stability.
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