Current Issue : January - March Volume : 2015 Issue Number : 1 Articles : 4 Articles
In the present investigation a series of pyrollo[2,3-d]pyrimidines analogues (4a-4q) were designed and subjected to molecular properties prediction and drug-likeness by Molinspiration (Molinspiraion 2008), Molsoft (Molsoft 2007) and Osiris. Out of 17 analogues, only 7 were chosen on conformity with Lipinski’s “Rule of Five” and other parameters for the synthesis and their onward screening for antimicrobial activity as orally active leads/molecules. Maximum drug-likeness model score for compound 4b was found to be (0.84). Selected compounds viz., 4b, 4f, 4h, 4j, 4k, 4m and 4n were synthesized and characterized by spectral analysis and then subjected to antimicrobial screening. All these compounds were found possess good antibacterial and antifungal activity. Compounds 4b, 4h showed pronounced activity against all strains of bacteria and compounds 4b and 4f possessed good antifungal activity....
N-phenylacridin-9-amine derivative having anticancer activity on the different human cancer cell like; human nasopharyngeal carcinoma [HONE-1] cell line, human adenocarcinoma [colon and rectal] tumor [HT-29] cell line, human brain tumor [DBTRG] cell line, gastric carcinoma TSGH, hepatoma liver hepa-G2, mouth carcinoma KB, lung adenocarcinoma H460, breast adenocarcinoma MX-1 and MCF-7 cell line and it’s significant cytotoxic activity against human leukemic HL-60 cell growth. N-phenylacridin-9-amine derivative exhibit both in-vivo as well as in-vitro potent antitumor activity. The alkylcarbamates of the N-phenylacridin-9-amine is more effective than their corresponding parent N-phenylacridin-9-amine derivatives. The cytotoxic activity of the N-phenylacridin-9-amine ethylcarbamates is decreased with increasing length and size of the alkyl function. It’s having also drug-DNA binding affinity which affected the antitumor activity of 9-anilinoacridines. These compound having higher cytotoxic activity due to high lipophilicity. We were used 24 compounds and those pIC50 activities on the HONE-1, HT-29 and DBTRG cell line for the QSAR study. Here the QSAR studies of N-phenylacridin-9-amine analogues were performed by using software CHEM-DRAW ULTRA-8.0, OPENBABLE-2.2.1, DRAGON, VALSTAT. We are considering here four model equations for QSAR study. All models question were validated by the VALSTAT software....
The thiazolidinedione ring is an important structural moiety found in numerous pharmaceutically active compounds for diabetes treatment. This is mainly due to the ease preparation and the important versatile pharmacological activity of thiazolidinedione. When thiazolidinedione were discovered, they were mostly useful as an anti-diabetic but in recent times, they are known to exhibit anticancer activity in combination with hypoglycaemic agents. The activation of PPAR- γ receptor is the basic mechanism of these categories of drugs. The present study involves synthesis of substituted Thiazolidinedione derivatives as an anti-diabetic activity. The structure activity Relationship of 2-(4-((3-aryl-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy) -N-arylacetamide and pharmacophore pattern of target molecule suggest that it gives antidiabetic and anti-cancer activity. Substituted thiazolidinedione synthesized by knoevenagel condensation reaction between 4-hydroxy benzaldehyde and Thiazolidinedione. The synthesis of compounds was confirmed by TLC, IR, NMR and Mass spectroscopy. The synthesized compounds were screened for anti-diabetic activity. The compounds with thiazolidinedione were found active and show optimal activity. The Compound 2-(4-((3-aryl-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)-N-arylacetamide(1) was found to be most active among the series....
Tuberculosis (TB) is a common and often deadly chronic bacterial infectious disease caused by a bacterium called mycobacterium, kills four people every minute some-where in the world and accounts about two million deaths per year. Isatin is a versatile lead molecule for designing of potential anti-microbial and anti-TB agents. Using this pharmacophore, it was envisaged that its combined effect with an active moiety may result in increased anti-microbial and anti-TB activity. Quinolones were found to be active against wide range of bacteria and also for some fungi. Synthesis of amide linkage containing some novel compounds using these two versatile moieties (isatin and quinolones) have been done and checked for their anti-microbial and anti-TB activity. With the base of dual concept, amide bond going to metabolize first and two moieties get separated where both having individual activity like anti-TB and other activities. 5-subsituted-1H-indole-2,3-dione-3-thiosemicarbazides were prepared by using 5-subsituted-1H-indole-2,3-dione and thiosemicarbazide and formed Schiff base with quinolones as ofloxacin and levofloxacin synthesized five novel derivatives containing amide linkage and one novel derivative synthesized using 1Hindole- 2,3-dione-3-thiosemicarbazide was treated with ester of ciprofloxacin. All the synthesized derivatives were confirmed by spectral analysis. With the study it was found that in compare to levofloxacin and ciprofloxacin as standard, novel compounds shows good to moderate activity against E. coli, S. aureus and C. albicans and also shows moderate anti-TB activity against H37Rv strain of M. tuberculosis....
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