Current Issue : April-June Volume : 2011 Issue Number : 2 Articles : 5 Articles
Molecular Modeling provides an array of valuable tools for drug design and analysis. Simple Visualization of molecules and easy access to structural databases has become essential component on the desktop of the medicinal chemist. Commercial software continues to expand upon the core user interface. New algorithms from industry and academia are quickly incorporated into the high end. Public domain takers are become more stable and offering functionality that rivals some of the commercial offerings. Computers continue to double in speed every year and a half while graphic displays become more sophisticated and intuitive. All of these elements make molecular modeling and integral part of the drug design....
A series of 3, 6-dihydroxy 9(H) 9-aryl xanthene derivatives were synthesized using the condensation reaction of different substituted aldehydes with resorcinol by MW irradiation technique using sulphamic acid as catalyst. The compounds were characterized by physicochemical and spectral analysis. Their antioxidant properties were evaluated using reducing power assay, hydroxyl radical scavenging activity assay, hydrogen peroxide scavenging activity assay. Ascorbic acid was used as reference standard. All synthesized xanthene derivatives exhibited pronounced antioxidant activity as a function of concentration from 50µg/ml-300µg/ml. 3, 4, 5-trimethoxy phenyl substituted xanthene had an IC50 0.89 mM/ml comparable to that of 1.32 mM/ml of standard. The antioxidant activity exhibited were a function of concentration of the derivatives. The other derivatives also showed comparable antioxidant activity at concentrations higher than that of ascorbic acid. The parameters for drug likeness were also evaluated according to the Lipinski’s rule of five which indicated that the xanthene derivatives have logP values between 4-5 and can be one of the hydrophobic classes of antioxidants to tackle the oxidative stress as compared to ascorbic acid which is hydrophilic....
In the recent year, heterocyclic compound have manifold application in medicine, agriculture and all other field due to their useful biological and pharmacological properties. The substituted benzofuran have gained attention in the resent year because substituted benzofuran and their derivatives have wide range of biological activities like antibacterial, antimicrobial, anti-inflammatory, antipshychotic, analgesic, antilipidemic and properties. The present review focous on benzofuran with potential activities that are now in development....
Many natural as well as synthetic heterocyclic compounds are known to have different biological activities. Pyridazine is an important six membered heterocyclic ring that containing two N hetero atoms. The pyridazine moiety is an important structural feature of many biologically active compounds. These pyridazine derivatives show diverse pharmacological activities. However, some compounds bearing pyridazine rings have been reported to effective in different nervous system disorders. On the basis of reported literature, we discuss here on pyridazine compounds in order to their different biological activities on nervous system. Pyridazines also hold considerable interest relative to the preparation of organic intermediates and physiologically active compounds....
Nonsteroidal anti-inflammatory drugs are widely used to treat effects of inflammation through inhibition of cyclooxygenase enzyme. The major limitation to long term therapeutic use of these drugs is their gastro toxicity. Prodrug approach is an established tool to solve this problem. Prodrug approach is now opening new doors in the challenging field of Drug Discovery and Development. The present work was targeted at the designing of carrier linked prodrug of Niflumic acid by masking the free carboxyl group with glucosamine to avoid undesirable gastro toxicity. The synthesized prodrug was characterized by analytical and spectral data. In vitro hydrolysis of prodrug indicated that they were quite stable in pH 2.5 and pH 7.4 whereas in Phosphate buffer pH 8.0 undergo hydrolysis following first order kinetics, releasing the free drug and glucosamine. The synthesized prodrug was screened for its anti-inflammatory activity and ulcerogenic potential. It exhibited comparable anti-inflammatory activity and significant less ulcerogenic than parent drug....
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