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Your search keyword '"Coco N. Kapanda"' showing total 2 results
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2 results on '"Coco N. Kapanda"'

1. Insight into the Willgerodt-Kindler Reaction of ω-Haloacetophenone Derivatives: Mechanistic Implication

Author

Jacques H. Poupaert, Christopher R. McCurdy, Fernand Gbaguidi, Urbain C. Kasséhin, and Coco N. Kapanda

Subjects
chemistry.chemical_compound, chemistry, Article Subject, Stereochemistry, Morpholine, Yield (chemistry), Condensation, Octasulfur, Combinatorial chemistry
Abstract

This paper reports efforts aimed at tuning up the synthesis of a compound library centered on the general template 2-amino-1-phenyl-2-thioxoethanone taking the condensation of ω-haloacetophenone, octasulfur, and morpholine as pilot reaction. Considerations about atomic economy were found extremely precious in selecting the best starting halo-reagent. A one-pot practical method based on use of 2-bromo-1-phenylethanone as substrate and N,N-dimethylformamide as solvent can be easily scaled up to gram amounts (72% yield). Based on this synthetic approach, some more specific examples are reported.

Published
2014
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2. Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors.

Author

Coco N. Kapanda, Giulio G. Muccioli, Geoffray Labar, Jacques H. Poupaert, and Didier M. Lambert

Subjects
*MONOGLYCERIDES, *LIPASE inhibitors, *FATTY acids, *AMIDES, *HYDROLASES, *CLINICAL drug trials, *CANNABINOIDS
Abstract

Monoglyceride lipase (MGL) inhibition may offer an approach in treating diseases in which higher 2-arachidonoyglycerol activity would be beneficial. We report here the synthesis and pharmacological evaluation of bis(dialkylaminethiocarbonyl)disulfide derivatives as irreversible MGL inhibitors. Inhibition occurs through interactions with MGL C208 and C242 residues, and these derivatives exhibit high inhibition selectivity over fatty acid amide hydrolase, another endocannabinoid-hydrolyzing enzyme. [ABSTRACT FROM AUTHOR]

Published
2009
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