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Papers by Farzana Ansari
1,4-Disubstituted-1,2,3-triazoles were synthesized by Cu(I) catalyzed click reaction, where the a... more 1,4-Disubstituted-1,2,3-triazoles were synthesized by Cu(I) catalyzed click reaction, where the
azides, with electron donating and electron withdrawing groups acted as 1,3-dipoles and 1-
ethynyl-1-cyclohexanol served as the terminal alkyne. These synthesized triazoles were
subjected to enzymatic assay which showed promising activity against α–glucosidase; 1-(2-
Cyano-4-nitrophenyl)-4-(1-hydroxycyclohexyl)-1H-1,2,3-triazole 3m being the most active
members of the library. Molecular docking studies of these triazoles with the homologymodeled
α–glucosidase protein were also performed to delineate ligand-protein interactions at
molecular level which suggested that Phe157, Arg312 and His279 are the major interacting
residues in the biding site of the protein and may have a significant role in the inhibition of
enzyme’s function.
European Journal of Organic Chemistry, 2011
ABSTRACT Several C-terminal peptidyl-substituted bis- and tris(electrophiles) were prepared by st... more ABSTRACT Several C-terminal peptidyl-substituted bis- and tris(electrophiles) were prepared by starting from polymeric phosphoranylidenacetates as acyl anion equivalents. After C-acylations with amino acids and peptide elongation, the obtained peptidyl-phosphoranylideneacetate resins were either cleaved oxidatively, delivering peptidyl-diketo esters, or saponified, leading to immediate decarboxylation. The generated peptidyl-phosphorane could be treated with aldehydes to yield peptidyl vinyl ketones or could be cleaved oxidatively to yield peptidyl keto aldehydes. Ligation with various bis(nucleophiles) including hydrazines, hydroxylamine, diamines, amino-thiols, amidines, and guanidines were investigated in the formation of peptide-heterocycle chimera containing pyrazoline, pyrazole, isoxazole, isoxazoline, thiazepine, quinoxaline, and imidazolone heterocycles.
1,4-Disubstituted-1,2,3-triazoles were synthesized by Cu(I) catalyzed click reaction, where the a... more 1,4-Disubstituted-1,2,3-triazoles were synthesized by Cu(I) catalyzed click reaction, where the
azides, with electron donating and electron withdrawing groups acted as 1,3-dipoles and 1-
ethynyl-1-cyclohexanol served as the terminal alkyne. These synthesized triazoles were
subjected to enzymatic assay which showed promising activity against α–glucosidase; 1-(2-
Cyano-4-nitrophenyl)-4-(1-hydroxycyclohexyl)-1H-1,2,3-triazole 3m being the most active
members of the library. Molecular docking studies of these triazoles with the homologymodeled
α–glucosidase protein were also performed to delineate ligand-protein interactions at
molecular level which suggested that Phe157, Arg312 and His279 are the major interacting
residues in the biding site of the protein and may have a significant role in the inhibition of
enzyme’s function.
European Journal of Organic Chemistry, 2011
ABSTRACT Several C-terminal peptidyl-substituted bis- and tris(electrophiles) were prepared by st... more ABSTRACT Several C-terminal peptidyl-substituted bis- and tris(electrophiles) were prepared by starting from polymeric phosphoranylidenacetates as acyl anion equivalents. After C-acylations with amino acids and peptide elongation, the obtained peptidyl-phosphoranylideneacetate resins were either cleaved oxidatively, delivering peptidyl-diketo esters, or saponified, leading to immediate decarboxylation. The generated peptidyl-phosphorane could be treated with aldehydes to yield peptidyl vinyl ketones or could be cleaved oxidatively to yield peptidyl keto aldehydes. Ligation with various bis(nucleophiles) including hydrazines, hydroxylamine, diamines, amino-thiols, amidines, and guanidines were investigated in the formation of peptide-heterocycle chimera containing pyrazoline, pyrazole, isoxazole, isoxazoline, thiazepine, quinoxaline, and imidazolone heterocycles.