Posted by admin on Nov 30, 2018 in |
Background: It has been developed a new combination of Palladium catalyzed Buchwald-Hartwig type reaction for the synthesis of N–tert– Butyl- 3- {[5- methyl- 2- (arylamino)pyrimidin- 4- yl]amino}benzene-sulfonamides 5 by the treatment of N–tert-butyl-3-[(2-chloro-5-methyl pyrimidin-4-yl)-amino]benzene sulfonamide 4 with various aromatic amines in the presence of Cs2CO3 and in DMF under microwave conditions. Method: All the eight compounds 5a-h were screened in-vitro for their antibacterial Gram-positive bacteria namely, Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus and three Gram-negative bacteria Pseudomonas aeruginosa, Klebsiella aerogenes, Chromobacterium violaceum. All the synthesized compounds were tested for their antifungal activity against five test organisms, Aspergillus niger, Chrysosporium tropicum, Rhizopus oryzae, Fusarium moniliforme and Curvularia lunata. Results: Among the title compounds 5d and 5e exhibited potent activity towards both gram positive and gram negative bacteria. Compounds 5e and 5f showed good antifungal activity. Conclusion: A new efficient catalyst/ligand combination was developed for the synthesis of title compounds 5a-5h under microwave conditions. The microwave procedure is slightly superior to the conventional method in terms of reduced time period...
Read More
Posted by admin on Nov 30, 2018 in |
Efavirenz (EFA) solid binary systems were prepared with β-CD by co-grinding and microwave irradiation methods. Detection of inclusion complexation was done in solution state by means of phase solubility analysis and in solid state by FTIR, DSC and in-vitro Dissolution studies. Apparent stability constant revealed EFA with β-CD at 1:1 M produces stiochometric complex with AL type phase solubility profile. A true inclusion of EFA with β-CD at 1:2 M in solid state was confirmed by FTIR and DSC. Dissolution properties of EFA- β-CD binary systems were superior when compared to physical mixture and pure drug. Overall the rank order of improvement in dissolution properties of Efavirenz with ratios is 1:2M > 1:1M and methods MW > CG > PM > pure drug. One way ANOVA suggest the DP60 and DE60 values were significantly higher (P<0.01) in solid binary systems prepared by microwave irradiation method when compared to co-grinding and its corresponding physical mixtures and pure...
Read More
Posted by admin on Nov 30, 2018 in |
As in the cases of non-communicable but chronic and autoimmune disorders like diabetes, cancer, anemia and rheumatoid arthritis are growing threat to humans. They depend on the genetic information and the genome sequence of the patients and other factors like environmental factors. In most of the cases, the pattern of the disease, i.e. pathogenesis is different for every individual, though phenotypic expression is same. Hence, there is a greater risk for the patient having the genes which are likely to cause above mentioned diseases and side effects or adverse drug reactions due to the therapy available. This occurs due to only one reason that every individual will not react to a drug in a same way. For minimizing these unwanted side effects or adverse reactions which are disease related and for giving patients a better and a bit healthy life, personalizing the medication is essential. This personalization involves the study of phenotypic and genotypic information of the patient and then planning the 3D’s i.e. choice of drug, dose and...
Read More
Posted by admin on Nov 30, 2018 in |
Salicylic acid is a phenolic plant growth regulator found in plants with various important physiological roles. This investigation was aimed to study the effect of exogenous application of salicylic acid on the growth, metabolism and health status of Mentha spicata, an aromatic medicinal plant having several monoterpenes and antioxidants which show various kinds of medicinal properties. In the present work, some growth and biochemical parameters were recorded at 30 and 60 days after treatment with different concentrations of salicylic acid (0, 100, 200 and 300 µg ml-1). Results clearly revealed that salicylic acid particularly at 200 µg ml-1 concentration significantly enhanced most of the growth and some of the biochemical attributes as well as the antioxidant property when compared with that of control plants. It can be concluded that exogenously applied salicylic acid at particular doses can enhance the biomass production as well as the medicinal potential of M. spicata as evidenced from some reliable physiobiochemical...
Read More
Posted by admin on Nov 30, 2018 in |
The objective of this study was to formulate and characterize Tacrine loaded poly (lactide-co-glycolide) (PLGA) nanoparticles used for the treatment of alzheimer’s disease and were prepared by modified nano precipitation method. Pharmacodynamics studies of the nanoparticles were evaluated for brain targeting and memory improvement in scopolamine-induced amnesic mice using Morris water maze test and inhibitory step down avoidance. The nanoparticles were characterized for drug content, particle size and particle morphology using TEM. In-vitro studies were determined by diffusion cells. The particle size of the prepared nanoparticles ranged from 247 nm to 293 nm. Nanoparticles of Tacrine were obtained with entrapment efficiency of 72.34-81.32%. The drug release from the Tacrine nanoparticles was sustained in batch TPGN-3for 24 h with 85.67% drug release. The in-vitro cytotoxicity studies indicate that the IC50 of the Tacrine loaded nanoformulations shown improved in the reduction of the IC50 but plain nanoparticles did not show severe cytotoxicity. In cellular uptake study of the optimized formulation TPGN-3, shows significant intracellular accumulation when compared with pure drug and...
Read More
