Posted by admin on Aug 31, 2018 in |
A series of (Z)-3-((1H-benzo[d]imidazol-2-yl)methyl)-substituted thiazolidine-2,4-dione (9a-n) have been synthesized and evaluated for their mycobacterium inhibitory activity against Mycobacterium tuberculosis H37Rv strain. The structures of the newly synthesized compounds were characterized by FTIR and NMR spectral analysis. Most of the synthesized compounds showed moderate to good anti-tubercular activity. Among these compounds 9a, 9d, 9f and 9g have displayed good anti-tubercular activity (MIC 6.25 μg/ml). Further, the molecular docking studies were carried out in order to rationalze the biological...
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Posted by admin on Aug 31, 2018 in |
A simple, economical, accurate and precise high performance liquid chromatographic method was developed and validated for the determination of rifabutin. A Shimadzu LC-2010C HT version 3.01 system using a C-18 column with dimensions of 250 × 4.6 mm and silica particle size of 5 μm. Isocratic elution was employed with methanol, acetonitrile and water (75:25 v/v) were used. The flow rate was 1 ml/min, and effluents were monitored at 242 nm. The HPLC method was extensively validated for linearity, accuracy, precision (Interday precision, Intraday precision), repeatability and robustness. The exalted results receive of a drug were procured all significance values were established to be under the acceptable range in International Conference of Harmonization (ICH) guidelines requirements. The results demonstrate that the developed HPLC modus could be successfully used up for identification and quantification of Rifabutin in any form of the drug, with high resolution, accuracy, and...
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Posted by admin on Aug 31, 2018 in |
The percutaneous delivery of salicylates to muscle and joints via the application of trolamine salicylate including transfersomes is the goal of this study and is beneficial for the treatment of inflammatory muscle, tendon and joint diseases. In this study, Trolamine salicylate permeability parameters through rat skin were evaluated with different trasfersome formulations in comparison with controls with Franz diffusion cells. Transfersomes were prepared with Solvent evaporation technique. Full factorial design was applied for the experimental design and data analysis. Ethanol / lipid ratio, percentage of sodium cholate, and homogenizer rate were considered as independent variables. On the other hand, transfersome size, drug loading, stability, drug release and skin permeability parameters were regarded as responses. The results showed that the main barrier for Trolamine salicylate permeability was the horny layer and partitioning from aqueous donor phase into the skin was rate limiting step for drug flux. Maximum flux and diffusion coefficient enhancement obtained by transfersomes no. 8 and 7 were 5.5 and 2.2 – folds, respectively. Regression analysis suggested significantly...
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Posted by admin on Aug 31, 2018 in |
Excessive antimicrobial use leads to adverse drug effects, thus increased healthcare costs and promoting the emergence of antimicrobial resistance worldwide. The aim of the study was to evaluate the prescription pattern of antibiotics in pediatric outpatients at private hospitals in Rajshahi city of Bangladesh. WHO / INRUD prescribing indicators were used for the analysis of prescription pattern. A total of 329 pediatric prescriptions were analyzed of which 54% male and 46% female. Most of the patients (48%) belongs to the age group of 1 year – 6 years. Body weight was not mentioned in 17% of prescr-iptions, diagnosis was confirmed only in 11% patients and also 11% of children did not take or completed immunization. Among the children born 83% were of caesarian and 17% of normal delivery. The results also indicated that 964 drugs were used by the patients with an average 2.93 per prescription. However, none of the drugs was prescribed in generic name. Interestingly, only 37.24% drugs were prescribed from the national essential drug list. Children...
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Posted by admin on Aug 31, 2018 in |
Chalcones (3a-m) was prepared by condensing 4-aminoacetophenone (1) with various aromatic aldehydes (2a-m) according to Claisen-Schmidt condensation. These 4-aminochalcones on cyclization with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines 4a-m with quantitative yields. Novel 4-amino-5,7-disubstituted pyrido[2,3-d]pyrimidines 6a-g were synthesized via a facile regioselective cyclization followed by aromatization of 2-amino-3-cyano-4,6-disubstitutedpyridines 5a-k which were in turn prepared from 4-aminochalcones 3a-m. All the synthesized compounds were characterized by spectroscopic means (FT-IR, 1H and 13C NMR, LC-MS) and elemental analysis and screened for anticancer activity by in-vitro MTT assay against Hos, HT 29, G 361, A 549 and DU 145 cell lines. Pyridopyrimidine nucleus was found to be the best pharmacophore than chalcone and pyrimidine nucleus in cancer therapy. And also it was found that compounds which possess 2,4-dichlorophenyl (3b,4b and 6b), 4-fluorophenyl (4c and 6c) and 4-dimethylamino (3i,4i and 6g) moieties as substituent at respective position in chalcones, pyrimidines and pyrido[2,3-d]pyrimidines identified as lead molecules. All the molecules were found to possess better activity against Hos (bone cancer) and G...
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