title: Novel pyridine-2,4,6-tricarbohydrazide derivatives: design, synthesis, characterization and in vitro biological evaluation as α- and β-glucosidase inhibitors.
abstract: A range of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4h) were synthesized and its biological inhibition towards α- and β-glucosidases was studied. Most of the compounds demonstrate to be active against α-glucosidase, and quite inactive/completely inactive against β-glucosidase. A number of compounds were found to be more active against α-glucosidase than the reference compound acarbose (IC50 38.25±0.12μM); being compound 4d with the p-hydroxy phenyl motive the most active (IC50 20.24±0.72μM). Molecular modeling studies show the interactions of compound 4d with the active site of target α-glucosidase kinase.
authors.affiliation: Department of Chemistry, GC University, Lahore 54000, Pakistan.
authors.forename: Sadaf
authors.initials: S
authors.lastname: Riaz
authors.affiliation: Department of Chemistry, GC University, Lahore 54000, Pakistan.
authors.forename: Islam Ullah
authors.initials: IU
authors.lastname: Khan
authors.affiliation: Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan. Electronic address: drmyar@ciitlahore.edu.pk.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Yar
authors.affiliation: Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Ashraf
authors.affiliation: Department of Chemistry, GC University, Lahore 54000, Pakistan.
authors.forename: Tanzeel Ur
authors.initials: TU
authors.lastname: Rehman
authors.affiliation: Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
authors.forename: Ayesha
authors.initials: A
authors.lastname: Shaukat
authors.affiliation: Department of Bioinformatics and Biotechnology, International Islamic University, Islamabad 44000, Pakistan.
authors.forename: Syed Babar
authors.initials: SB
authors.lastname: Jamal
authors.affiliation: Department of Chemistry, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
authors.forename: Vera C M
authors.initials: VCM
authors.lastname: Duarte
authors.affiliation: Department of Chemistry, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
authors.forename: Maria J
authors.initials: MJ
authors.lastname: Alves
mesh_terms: D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D027861:Prunus / Q000201:enzymology; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000201:enzymology; D000520:alpha-Glucosidases / Q000737:chemistry / Q000378:metabolism; D001617:beta-Glucosidase / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism
chemical_list: D065089:Glycoside Hydrolase Inhibitors; D011725:Pyridines; D000520:alpha-Glucosidases; D001617:beta-Glucosidase; C023666:pyridine
keywords: Acarbose; Diabetes; MMFF94X+Solvation; Pyridine-2,4,6-tricarbohydrazide; α-Glucosidase; β-Glucosidase