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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Posted by admin on Aug 31, 2018 in |
The nature harbours a huge source of active principles possessing antimicrobial property. This phenomenon provokes microbiologists, ethnopharmacologist and natural product chemists to perform extensive research on phytoprinciples. The extensive use of these principles in phytotherapy is becoming an excellent alternative strategy against the occurrence of microbial resistance due to some conventional medicines. The current research article dealt with ethanolic crude extractives from the dried leaves of Ocimum sanctum Linn. and fresh Leaf stalks of Piper betle Linn. were screened for its antimicrobial activity using the agar-well diffusion method. The sample of the mentioned herbs could be easily found in large amount from the environment of north east region in India. In our present study with Ocimum sanctum L. (tulsi) leaf extract showed marked inhibitory effect on Klebsiella pneumoniae, Pseudomonas aeruginosa, E.coli, Vibrio cholerae where a highest zone of inhibition estimated was 30 mm against E. coli. Tulsi extractive possess partial inhibition against Candida albicans. Crude ethanolic extractive of Piper betle Linn. (Paan) stalk remarkably inhibited. A. niger, Escherichia coli and Candida albicans where the...
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Posted by admin on Aug 31, 2018 in |
Objective: Brucellosis in humans is the most common zoonotic infection in the world. Brucellosis can be prevented by vaccination but no effective vaccines are known for prevention of human brucellosis and minimal impact of animal brucellosis. Outer membrane proteins (OMPs) of Brucella sp. have been the focus of vaccine development and the diagnosis of brucellosis. Methods: The pathogenesis study of brucellosis used rat by intraperitoneal injection. Profile OMP detected by SDS-PAGE. The antibodies took from rabbit and the immune response did with western blotting, dot blot and immuno histochemistry. Results: B. abortus S19 cell to the rat show the presence of inflammatory cells and bleeding in the uterine rat. The 36 kDa OMP could isolated from B. abortus S19. Rabbit antibody to 36 kDa OMP can detect B. abortus of this histological of the uterus. OMP 36 kDa B. abortus S19 is antigenic characterized by its ability to stimulate antibodies in the host’s body (Oryctolagus cuniculus). Conclusion: B. abortus S19 can be detected in histopathology of rats uterus shown...
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Posted by admin on Aug 31, 2018 in |
Introduction: Antiplatelets play a crucial role in improving many metabolic disorders and complications, including dyslipidemia, atherosclerosis, diabetes mellitus and cardiovascular diseases. The most common and effective antiplatelets used widely are aspirin and clopidogrel. The aim of this study is to evaluate the dyslipidemic and protective effects of aspirin and clopidogrel in obese rats. Materials and methods: 24 rats were divided into two groups, control (n = 6) (was taken normal chow) and the other group (n = 18) were allowed to eat beef tallow (90 g) and saturated fat (10 g) for 6 weeks to induce obesity. The second group was further classified to three subgroups, subgroup I (n = 6) was kept as obese group (n = 6) (positive control), subgroup II (n = 6) obese rats were treated with aspirin and subgroup III (n = 6) obese rats were treated with clopidogrel for 7 days. At the end of experiment blood samples were taken and lipid profile, FBS measured as well as body weight and the relative...
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Posted by admin on Aug 31, 2018 in |
The purpose of the present study was to synthesize and evaluate the potential of folate-G.4.0-PAMAM dendrimer conjugates as acceptable vehicle for site specific delivery of piroxicam (PXM) to inflammatory regions and to determine its targeting efficiency in carreganan induced arthritic rats. PXM was selected as a model acidic anti inflammatory drug. Folic acid was linked to the surface amino groups of G4.0-PAMAM dendrimer through a carbodiimide reaction and loaded with PXM. The coupled conjugates were characterized by 1H-NMR, IR spectroscopy and polyacrylamide gel electrophoresis (PAGE). The drug content and % encapsulation efficiency increased with increasing folate content for the dendrimer conjugates. The in- vitro release rate was decreased for the PXM-F1, PXM-F2 and PXM-F3 conjugates when compared with PXM-D1. Drug dendrimer and conjugates were further evaluated for haemolytic toxicity and stability study. There was no change in turbidity, colour, consistency in stability study. Efficacy of plain PXM and dendrimer conjugates was tested by carrageenan induced paw edema model. Pharmacodynamic study revealed 74%, 78%, 85%, 90% inhibition at 4th hour...
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