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Synthesis of N-phenylphthalimide Derivatives as ${\alpha}-Glucosidase$ Inhibitors
Pluempanupat, Wanchai,Adisakwattana, Sirichai,Yibchok-Anun, Sirintorn,Chavasiri, Warinthorn 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
Sixteen N-phenylphthalimide derivatives were synthesized and their ability to inhibit ${\alpha}-glucosidase$ was investigated. N-(2,4-dinitrophenyl)phthalimide was a potent inhibitor of yeast ${\alpha}-glucosidase\;(IC_{50};\;0.158{\pm}0.005mM)\;and\;maltase\;(IC_{50};\;0.051{\pm}0.008mM)$, whereas it did not inhibit sucrase. From a Lineweaver-Burk plot of ${\alpha}-glucosidase$ kinetics, N-(2,4-dichlorophenyl)phthalimide was found to be a competitive inhibitor of yeast ${\alpha}-glucosidase$. These results indicate that N-(2,4-dinitrophenyl)phthalimide could be a representative of a new group of ${\alpha}-glucosidase$ inhibitors.
Synthesis of N-phenylphthalimide Derivatives as α-Glucosidase Inhibitors
Wanchai Pluempanupat,Sirichai Adisakwattana,Sirintorn Yibchok-Anun,Warinthorn Chavasiri 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
Sixteen N-phenylphthalimide derivatives were synthesized and their ability to inhibit α-glucosidase was investigated. N-(2,4-dinitrophenyl)phthalimide was a potent inhibitor of yeast α-glucosidase (IC50; 0.158 ± 0.005 mM) and maltase (IC50; 0.051 ± 0.008 mM), whereas it did not inhibit sucrase. From a Lineweaver-Burk plot of α-glucosidase kinetics, N-(2,4-dichlorophenyl) phthalimide was found to be a competitive inhibitor of yeast α-glucosidase. These results indicate that N-(2,4-dinitrophenyl)phthalimide could be a representative of a new group of α- glucosidase inhibitors.
Application of Cl3CCONH2/PPh3 towards the Synthesis of Bioactive Amides
Skydow Chaysripongkul,Wanchai Pluempanupat,장두옥,Warinthorn Chavasiri 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.9
Cl3CCONH2 coupled with PPh3 was determined to be an effective reagent for the conversion of carboxylic acids to their corresponding acid chlorides. Subsequently, these acid chlorides were successfully trapped with amines in the presence of 4-picoline, yielding amides. This practical and efficient protocol can be utilized for the synthesis of biological amides in excellent yields.
Chaysripongkul, Skydow,Pluempanupat, Wanchai,Jang, Doo-Ok,Chavasiri, Warinthorn Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.9
$Cl_3CCONH_2$ coupled with $PPh_3$ was determined to be an effective reagent for the conversion of carboxylic acids to their corresponding acid chlorides. Subsequently, these acid chlorides were successfully trapped with amines in the presence of 4-picoline, yielding amides. This practical and efficient protocol can be utilized for the synthesis of biological amides in excellent yields.