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Ramaprasad G.C.,Mangalore University | Ramaprasad G.C.,Biocon | Kalluraya B.,Mangalore University | Sunil Kumar B.,Net Pharmacy College | Mallya S.,Mangalore University
Medicinal Chemistry Research | Year: 2013

In search of pharmalogically active molecules in the class of oxadiazoles, the present article deals with the synthesis of 5-(5′-fluoro-2′- methoxybiphenyl-3-yl)-1,3,4-oxadiazol-2(3H)-one 2 from its hydrazide analog 1. The compound 2 was regioselectively N-alkylated with alkyl halides and produced the compounds 3a-f. Compound 3f was further functionalized with substituted benzenesulfonyl chlorides to give compounds 3g-j. The synthesized compounds were characterized by elemental and spectral analysis. Newly synthesized compounds were tested for their in vivo anti-inflammatory, analgesic, and in vitro antimicrobial activities. The compounds 3a-c were found to have promising anti-inflammatory and analgesic activities. Compounds 3b, 3f, and 3g showed significant antibacterial and antifungal activities. © 2013 Springer Science+Business Media New York. Source


Ramaprasad G.C.,Mangalore University | Ramaprasad G.C.,Biocon | Kalluraya B.,Mangalore University | Sunil Kumar B.,Net Pharmacy College
Medicinal Chemistry Research | Year: 2014

A series of S-alkyl derivatives of 3-(substituted-(1,1′-biphenyl)-3- yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole-6-thiol (4a-j) were synthesized by conventional and microwave irradiation methods. Microwave method proved to be a rapid and better yield compare to that of conventional method. The synthesized compounds were characterized by 1H NMR, 13C NMR, 19F NMR, IR, LCMS, and elemental spectroscopic analysis. These compounds were screened for their in vitro anticancer activity by MTT assay. Among the tested compounds, the compound 4c was the most promising anticancer agent with IC50 value 12 μM in HT29 cell line. © Springer Science+Business Media 2014. Source


Ramaprasada G.C.,Mangalore University | Ramaprasada G.C.,Biocon | Kallurayaa B.,Mangalore University | Sunil Kumarb B.,Net Pharmacy College | Sahana Mallyaa,Mangalore University
Der Pharma Chemica | Year: 2012

A series of 3-(5'-fluoro-2'-methoxybiphenyl-3-yl)-6-(substituted)[1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazole (3a-j) were synthesized by conventional and microwave irradiation methods. Microwave method proved to be a rapid and better yield compare to that of conventional method. The structures of these compounds were established on the basis of spectral and analytical data. These novel compounds were screened for their antibacterial and anticancer activity. The promising compounds 3b and 3g have been identified. Source


Puthiyapurayil P.,Mangalore University | Puthiyapurayil P.,Biocon | Poojary B.,Mangalore University | Chikkanna C.,SDM College Ujire | Buridipad S.K.,Net Pharmacy College
European Journal of Medicinal Chemistry | Year: 2012

On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl) propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These compounds were also evaluated for their in-vivo anthelmintic activity, as well as in-vitro antimicrobial studies. Amongst the tested compounds, the compound 7j was the most promising cytotoxic agent with IC50 value of 10.54 μM in MCF-7 cells. The compounds 7l and 7q exhibited excellent anthelmintic activity. The compounds 7d, 7f, 7j, 7l, 7o, 7p and 7r showed good antibacterial activity, whereas compounds 7e and 7k exhibited excellent antifungal activity. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and LCMS analysis. © 2012 Elsevier Masson SAS. All rights reserved. Source


Palusa S.K.G.,Jawaharlal Nehru Technological University | Palusa S.K.G.,Net Pharmacy College | Udupi R.H.,Net Pharmacy College | Himabindu V.,Jawaharlal Nehru Technological University | Sridhara A.M.,Kuvempu University
Organic Communications | Year: 2011

Novel pyrimidine substituted 1,3,4-oxadiazole derivatives (11a-k) were synthesized from the condensation of different substituted aromatic carboxylic acids with substituted pyrimidine carboxy hydrazide using POCl 3 as condensing agent. Their structures were characterized by physical and spectral studies. The synthesized compounds were evaluated for their in vitro antimicrobial and anti-inflammatory activity. Some of the newly synthesized compounds showed good antimicrobial and anti-inflammatory activities. © 2011 Reproduction is free for scientific studies. Source

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