38440-19-6Relevant academic research and scientific papers
Synthesis and SAR/3D-QSAR studies on the COX-2 inhibitory activity of 1,5-diarylpyrazoles to validate the modified pharmacophore
Singh, Sunil K.,Saibaba,Rao, K. Srinivasa,Reddy, P. Ganapati,Daga, Pankaj R.,Rajjak, S. Abdul,Misra, Parimal,Rao, Y. Koteswar
, p. 977 - 990 (2007/10/03)
Diverse analogs of 1,5-diarylpyrazoles having 3-hydroxymethyl-4-sulfamoyl (SO2NH2)/methyl sulfonyl (SO2Me)-pheny group at N1 were synthesized and evaluated for their in vitro cyclooxygenase (COX-1/COX-2) inhibitory activity. The SAR study mainly involved the variations at positions C-3, C-5 and N1 of the pyrazole ring. Several small hydrophobic groups at/around position-4 of C-5 phenyl, viz. 3,4-dimethylphenyl analog 9, 3-methyl-4-methylsulfanylphenyl analog 14 and 2,3-dihydrobenzo[b] thiophenyl analog 17, exhibited impressive COX-2 inhibitory potency. In general, the sulfonamide analogues with a CHF2 at C-3 were found to be more potent than those having a CF3 group. The three dimensional quantitative structure activity relationship comprising comparative molecular field analysis (3D-QSAR-CoMFA) afforded the models with high predictivity which further validated the acceptance of hydroxymethyl (CH2OH) group in the hydrophilic pocket of the COX-2 enzyme.
PYRAZOLO AND IMIDAZO-PYRIMIDINE DERIVATIVES
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Page/Page column 18-19, (2008/06/13)
The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula (I) wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined in the description and claims and to processes for their preparation, pharmaceutical compositions containing said derivatives and their use in the prevention and treatment of diseases.
A Modified Synthesis of Fluorinated 1,3-Diketones
Joshi, Krishna C.,Joshi, Bidya S.
, p. 229 - 232 (2007/10/02)
The reinvestigation of acylation reactions of fluorinated aryl methylketones with ethyl esters at 0 deg C afforded fluorinated 1,3-diketones in excellent yields.
