Current Issue : July - September Volume : 2014 Issue Number : 3 Articles : 7 Articles
Flavanones are important naturally occurring organic compounds possessing a wide range of biological activities, used in the treatment of various diseases. Flavanones are an important member of the flavonoid family that have been receiving increasing attention due to their medicinal properties. The biological activity of flavanones mainly depends on its physical and chemical property. Various analogues of flavanones were synthesized from oxidative cyclization of chalcones. In the present study flavanones were synthesized by claisen–schmidt condensation between benzaldehyde and O-hydroxyacetophenone. Semicarbazide is a derivative of urea and has been known for various reasons with in foods. It occurs as one of the break-down products of nitrofurans, a group of widely used veterinary drugs and as a break-down product of azodicarbonamide, used as a flour treatment agent to improve baking properties. Semicarbazide are the raw material of semicarbazone, have been known to have biological activity against the most common species of bacteria, it is also used as a detection reagent in thin layer chromatography (TLC). Semicarbazide products having antiviral, anti-infective and antineoplastic activities. We synthesized some novel flavanones incorporated Semicarbazide derivatives. The derivatives were characterized by physico-chemical (TLC and melting point) and spectral analysis (I.R., N.M.R and Mass Spectroscopy) and finally the biological activities were performed by using different animal models like pentylenetetrazole-induced convulsions in rats for anti-convulsant and tail immersion method for analgesic activities respectively....
Recently, a large number of anthelmintics are being used, each claiming to have desired therapeutic efficacy and low toxicity. We have observed promising activity of synthesized azetidin-2-one derivatives. In this paper, we are presenting anthelmintic activity of titled compounds in comparison with albendazole, a reference standard. An attempt is also made to correlate the anthelmintic activity of the compounds with their structures and thus come to a concrete conclusion regarding their structure activity relationship (SAR)....
N-phenylacridin-9-amine derivative having anticancer activity on the human adenocarcinoma (colon and rectal)\r\ntumor (HT-29) cell line, human nasopharyngeal carcinoma (HONE-1) cell line, human brain tumor (DBTRG) cell line, gastric\r\ncarcinoma TSGH, hepatoma liver hepa-G2, mouth carcinoma KB, lung adenocarcinoma H460, breast adenocarcinoma MX-1 and\r\nMCF-7 cell line and it�s significant cytotoxic activity against human leukemic HL-60 cell growth. N-phenylacridin-9-amine\r\nderivative exhibit both in-vivo as well as in-vitro potent antitumor activity. The alkylcarbamates of the N-phenylacridin-9-amine\r\nis more effective than their corresponding parent N-phenylacridin-9-amine derivatives. The cytotoxic activity of the Nphenylacridin-\r\n9-amine ethylcarbamates is decreased with increasing length and size of the alkyl function. It is also having drug-\r\nDNA binding affinity which affects the antitumor activity of 9-anilinoacridines. These compound having higher cytotoxic activity\r\ndue to high lipophilicity. We used 25 compounds and their pIC50 activities on the HT-29 cell line for the 2-D QSAR study. Here the\r\n2D-QSAR studies of N-phenylacridin-9-amine analogues were performed by using software chem-draw ultra-8.0, openbable-\r\n2.2.1, dragon, valstat. We are considering here two model equations for QSAR study. The value of linearity r2 for model-1 of HT-\r\n29 cell line (model-1) is; r2 = 0.922608, Q2 = 0.888065, Spress = 0.232872 and SDEP = 0.21343 while this value for model-2 of\r\nHT-29 cell line is; r2 = 0.879102, Q2 = 0.835641, Spress = 0.282183 and SDEP = 0.258625. Both models were validated by the\r\nvalstat software....
Novel 2-(5-((4,5-dihydro-3-methyl-5-oxo-1-aryl-1H-pyrazol-4-yl)methylene)-1,3,4-oxadiazol-2-ylthio)-1-(4-arylphenyl)\r\nethanone derivatives with anti-inflammatory activity were subjected for the two and three dimensional quantitative structure\r\nactivity relationships (2D-QSAR and 3D-QSAR) studies. The 2D-QSAR models multiple linear regression, partial least square and\r\nprinciple component regression approach and 3D-QSAR model using the k nearest neighbour (kNN) approach were developed.\r\nThe MLR, PLS and PCR model predicted the training data with r2 of 0.9928, 0.9923 and 0.9703 together with q2 estimating to\r\n0.9733, 0.9021 and 0.9209 respectively. For 3D QSAR negative values in steric field descriptors indicated the requirement of\r\nnegative steric potential, for enhancing the anti-inflammatory activity and more numbers of positive value in electrostatic\r\ndescriptors suggested that electropositive groups were important for anti-inflammatory activity. Thus these validated models\r\nbring important structural insight to aid the design of effective anti-inflammatory agent....
The benzofuran nucleus and derivatives occupy a position of considerable significance for widespread occurrence in\r\nplants and their potential as important pharmaceuticals. It has also been reported that benzofuran derivative possess\r\nbacteriostatic, bactericidal, fungistatic, fungicidal activities. The natural products possessing benzofuran nucleus are frequently\r\nassociated with useful pharmacological properties. This fact created interest in synthetic products containing benzofuran\r\nnucleus. Kreamer and Spilker discovered benzofuran in coal tar. It was synthesized by Perkin in 1870. Thus the chemistry of\r\nbenzofuran has developed in a spectacular fashion during the last several years. Natural benzofuran compounds have varied\r\nchemical structures. They exist in simple form such as a substituted benzofuran to highly complicated molecule like morphine.\r\nDue to wide scope for synthetic investigations leading to more potent synthetic leads, voluminous synthetic work has been\r\nproduced so far....
A new series of 2,5-diphenyl-1,3,4-oxadiazole (3a-j) and 3,6-diphenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (6a-j) derivatives were synthesized and evaluated for their antimicrobial and antioxidant activity to study the effect of substitution on the phenyl ring of benzoicacid on these activities. 2,5-diphenyl-1,3,4-oxadiazole (3a-j) were obtained from acid hydrazide on treatment with different benzoicacid in the presence of phosphorous oxychloride. Cyclo-condensation of the SH and NH2 groups of aminothiol 5 with appropriate benzoic acid derivatives in presence of phosphoryl chloride gave 3,6-diphenyl [1,2,4] triazolo [3,4-b][1,3,4]thiadiazole derivatives (6a-j). The toxicity risk assessment; cLogP, solubility, drug likeness and drug score for these compounds was predicted, compounds 3a-c and 3f-i were assessed as non-toxic, while 3d indicated irritating effects and 3e medium risk mutagenicity. 3,6-diphenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives (6a-j) have shown high risk of reproductive effects. The compounds 3b, 3d, 3f, 3g, 6b, 6c and 6i; and 3d-g, 6b, 6f showed pronounced antibacterial and antifungal activity respectively, while 6b and 6c exhibited promising antioxidant activity....
In the present work we have synthesized benzothiazole with dithiocabamate side chain substituting different alkyl/aralkyl halides and calculated molecular properties by mol inspiration, Osiris, molsoft software’s and ALOPGPS 2.1 program. Structures of the new compounds were established by 1HNMR, IR, Mass spectral data and elemental analysis. All of the synthesized compounds (4a-4g) obey lipinski’s “rule of five” and other parameters. The newly synthesized compounds were evaluated for antibacterial and antifungal activities. The final synthesized compounds have exhibited promising antibacterial antifungal activity....
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