Current Issue : October - December Volume : 2015 Issue Number : 4 Articles : 6 Articles
Thiazolidinedione (TZD) is considered as a biologically important active scaffold that possesses almost all types of biological activities includes antibacterial and antifungal activity, antitubercular activity, anticancer activity, anti-inflammatory and analgesic activity, anticonvulsant and antidepressant activity, antiviral/anti-HIV activity, antidiabetic activity, muscarinic receptor 1 agonist, follicle-stimulating hormone (FSH) receptor agonist, trypanocidal (anti-epimastigote) activity and antiarrhythmic activity. This review is complementary to earlier research work of on various biological activities of thiazolidinedione derivatives....
Docking of small molecules in the receptor binding site is a vital part of structure based drug design. The current study deals with the synthesis and evaluation of Nitromethane substituted Chalcone derivatives with various targets of Mycobacterium Tuberculosis and Antimicrobial activity using in-silico docking studies. In this perspective Nitromethane substituted Chalcone derivatives are docked with various targets like 1A69 (Purine nucleoside phosphorylase), 3IFZ (Mycobacterium tuberculosis gyrase), 1TED (Polyketide synthase), 2A7S (Acetyl CoA Carboxylase), 3ORI (Protein Kinase B), Aspartate aminotransferase (PDB ID: 1AHG), Amidophosphoribosyl transferase (PDB ID: 1AO0) and Dihydropterote synthase (PDB ID: 1AD4). In-silico docking studies were carried out using mcule online docking. OSIRIS property explorer used to explore the molecular properties. Metabolic sites are predicted using metaprint 2D. Substituted acetophenones on treatment with substituted aldehydes affords the corresponding chalcones (1a-1k). Treatment of chalcones with nitromethane under Michael addition condition furnished the corresponding Michael adducts (2a-2k). The structure was proposed based on their 1H NMR and IR spectral data. All the synthesized compounds (2a-2k) were screened for their Anti-tubercular, Anthelmentic and Anti-microbial activities. Among synthesized compounds 2g, 2j and 2k showed highest Anti-tubercular activity at 50µg/ml concentration. Compounds 2g, 2j and 2k showed highest activity suggesting that electron donating groups aid in anthelmentic activity. Compounds 2d, 2g and 2j were found to be more effective anti-microbial activity. All the compounds showed significant Anti-tubercular, Anthelmentic and Anti-microbial activities....
A series of new N-substituted 5-arylidenerhodanine derivatives (D1-D10) were synthesized starting from 5- arylidenerhodanines. The 5-arylidinerhodanines were reacted with 2-bromo-1-phenylethanone in presence of potassium hydroxide and dimethyl formamide under microwave conditions to give N-substituted 5-arylidenerhodanine derivatives. The synthesized compounds were confirmed on the basis of spectral data and elemental analyses. The synthesized compounds evaluated for their cytotoxic activity against two different human cancer cell lines using MTT assay. The cytotoxic activity results revealed that the synthesized compounds demonstrated the ability to inhibit HT-29 (colon cancer), MCF-7 (breast cancer) cancer cell lines against reference drug methotrexate. Among the compounds tested, the most active compounds (4-trifluoro, 2- thienyl and 4-fluoro-substituted) possess significant cytotoxic activity against both the cancer cell lines and all other compounds showed moderate to weak activity....
In pursuit of compounds which show antimicrobial activity, synthesis of novel morpholine linked substituted chalcones done by condensing different aldehydes with diazotized 4-amino acetophenone coupled to morpholine and evaluated them for in-vitro anticancer, anti-inflammatory and antibacterial activities. The synthesized compounds were screened for anticancer activity against human breast cancer cell lines MCF-7 and MDA-MB-468. In-vitro methods for anti-inflammatory activity like inhibition of bovine albumin denaturation and heat induced hemolysis methods were used. Antibacterial and antitubercular activities were also performed. The structures of synthesized compounds were confirmed based on the IR, 1H NMR and mass spectral data. Among the synthesized compounds, 3HM shown IC50 value of 25 µg against the MCF-7 cell line, whereas 3JM shown IC50 value of 10 µg against MDA-MB-468 cell lines. Compound 3GM has moderate anti inflammatory activity in bovine denaturation and heat induced hemolytic method. Compounds 3DM, 3EM and 3DGM shown MIC of 0.025 µg/ml against Staphylococcus aureus, while compounds 3IM shown MIC of 0.025 µg/ml against E. faecalis. 3AM, 3BM and 3EM is sensitive to Mycobacterium tuberculosis with a MIC of 3.12 µg/ml....
In the recent past years, the 1,4-benzothiazine derivatives have been covering a large area of studying because of their synthetic possibility, different chemical behavior, there biological activities and different applications in the pharmaceutical drug. The 1, 4-benzothiazine forms an important class of heterocyclic system, it include the N and S molecules in the ring. The novel 1, 4-benzothiazine derivatives occupancy several biological activities such as anti-inflammatory, anti-rheumatic, antimicrobial, antioxidant, anti-hypertensive, anti-HIV, cardiovascular, ATP-sensitive potassium channel opener, anti-malarial, cytotoxic, immunomodulator, neuroprotective and aldose reductase inhibitor etc....
A novel series of quinazoline is described; quinazolines (IVa-e) were prepared from the lead molecule anthranilic acid. On bromination of anthranilic acid 5-Bromo anthranillic acid was formed. It was treated with benzoyl chloride in the presence of dry pyridine to get 6-Bromo-2-ethyl-3, 1-benzoxazin-4-one, which was further treated with substituted aromatic amines to get 6-Bromo-phenyl-3-substituted quinazolines 4(3H) one, by substituting the aromatic ring at 3rd position. The structures of the synthesized compounds were assigned on the basis of UV analysis, IR, mass and PMR spectral data. All the products were screened against different strains of bacteria and fungi. Most of these compounds showed better inhibitory activity in comparison to the standard drugs....
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