Antidepressant, analgesic activity and SAR studies of substituted benzimidazoles

Purpose. Benzimidazole class of compound is found to have diverse biological properties. From the literature study, it is observed that depression is a severe mental disease affecting a huge population and pain is affecting about 20% of world population. In continuation of our previous research work, we selected benzimidazole pharmacophore to further explore its pharmacological activities. Methods. Forced swim test and Thermal stimulus test were used to assess the antidepressant and analgesic activity of synthesized benzimidazole analogs. Results. The antidepressant activity results showed that compound 3j was found most potent having Mean ± SEM value 21.6 ± 0.8 for treated group. Furthermore, in the analgesic test, 3b, 3j, and 3o showed Mean ± SEM values; 1.8 ± 0.10, 2.3 ± 0.10 and 2.2 ± 0.10, respectively. The study results suggested that these compounds could be explored further for the development of better antidepressant and analgesic agents. Conclusion. From the present study, it may be concluded that these active benzimidazole derivatives have been found to possess potential antidepressant and analgesic activit

Synthesis and antimycobacterial activity of novel heterocycles

In the present investigation 4-hydroxy-3-methylacetophenone on condensation with various aromatic aldehydes in methanolic KOH solution yielded the corresponding chalcones (CI–CXI). These chalcones were further reacted with hydrazine hydrate in ethanol which led to the formation of pyrazoline derivatives (HI–HXI). The newly synthesized heterocyles were characterized on the basis of their chemical properties and spectroscopic data. All newly synthesized compounds were evaluated for their antimycobacterial activities against Mycobacterium tuberculosis H37Rv

Design of targeted dosage form of ofloxacin

The targeted pro-drug is a classical pro-drug design often representing a non-specific chemical approach to mask undesirable drug properties, such as limited bioavailability, lack of site specificity, and chemical instability. On the other hand, targeted pro-drug design represents a new strategy for directed and efficient drug delivery. Quinolone antibiotics exert their pharmacological effect by inhibiting the cell wall synthesis of the pathogen. However, development of resistance exists, which instigates for a new higher congener to remain in clinical practice. To overcome this phenomenon and also to produce site-specific activity of the cell walls of the pathogen, ofloxacin is conjugated with a hydroxypropyl methacrylamide polymer backbone moiety. The results of in vitro release studies indicate the possibilities for the development of a new drug for site-specific therapy with an improved t1/2 of the drug. This novel pro-drugmay have opened a new vista in antibiotic chemotherapy

SHORT COMMUNICATION Design of targeted dosage form of ofloxacin +

Abstract: The targeted pro-drug is a classical pro-drug design often representing a non-specific chemical approach to mask undesirable drug properties, such as limited bioavailability, lack of site specificity, and chemical instability. On the other hand, targeted pro-drug design represents a new strategy for directed and efficient drug delivery. Quinolone antibiotics exert their pharmacological effect by inhibiting the cell wall synthesis of the pathogen. However, development of resistance exists, which instigates for a new higher congener to remain in clinical practice. To overcome this phenomenon and also to produce site-specific activity of the cell walls of the pathogen, ofloxacin is conjugated with a hydroxypropyl methacrylamide polymer backbone moiety. The results of in vitro release studies indicate the possibilities for the development of a new drug for site-specific therapy with an improved t1/2 of the drug. This novel pro-drug may have opened a new vista in antibiotic chemotherapy