Unknown

Dataset Information

0

Synthesis, biological activity and molecular docking of new tricyclic series as ?-glucosidase inhibitors.

ABSTRACT: Diabetes is an emerging metabolic disorder. ?-Glucosidase inhibitors, such as acarbose, delay the hydrolysis of carbohydrates by interfering with the digestive enzymes. This action decreases the glucose absorption and the postprandial glucose level. We have synthesized 25 tricyclic 2-phenoxypyrido[3,2-e][1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones hybrids and evaluated their ?-glucosidase inhibitory activity. Compounds 6h and 6d have shown stronger activity than that of acarbose. Compound 6h exhibited the highest inhibition with an IC50 of 104.07 µM. Molecular modelling studies revealed that compound 6h inhibits ?-glucosidase due to the formation of a stable ligand-?-glucosidase complex and extra hydrogen bond interactions, and directed in the binding site by Trp329.25 tricyclic 2-phenoxypyrido[3,2-e][1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones hybrids have been synthesized and evaluated their ?-glucosidase inhibitory activity. Compounds 6h have shown stronger activity than that of acarbose.

SUBMITTER: Abuelizz HA 

PROVIDER: S-EPMC6661812 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis, biological activity and molecular docking of new tricyclic series as α-glucosidase inhibitors.

Abuelizz Hatem A HA   Iwana Nor Azman N I NANI   Ahmad Rohaya R   Anouar El-Hassane EH   Marzouk Mohamed M   Al-Salahi Rashad R  

BMC chemistry 20190405 1

Diabetes is an emerging metabolic disorder. α-Glucosidase inhibitors, such as acarbose, delay the hydrolysis of carbohydrates by interfering with the digestive enzymes. This action decreases the glucose absorption and the postprandial glucose level. We have synthesized 25 tricyclic 2-phenoxypyrido[3,2-<i>e</i>][1,2,4]triazolo[1,5-<i>a</i>]pyrimidin-5(4H)-ones hybrids and evaluated their α-glucosidase inhibitory activity. Compounds <b>6h</b> and <b>6d</b> have shown stronger activity than that of  ...[more]

Similar Datasets

Unknown Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.
| S-EPMC6154535 | biostudies-literature
Unknown Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.
| S-EPMC6150375 | biostudies-literature
Unknown Synthesis, molecular modeling and biological evaluation of aza-flavanones as α-glucosidase inhibitors.
| S-EPMC6072087 | biostudies-literature
Unknown Synthesis of novel coumarin-hydrazone hybrids as α-glucosidase inhibitors and their molecular docking studies.
| S-EPMC10475976 | biostudies-literature
Unknown Synthesis and Molecular Docking Studies of Alkoxy- and Imidazole-Substituted Xanthones as α-Amylase and α-Glucosidase Inhibitors.
| S-EPMC10222686 | biostudies-literature
Unknown Synthesis, <i>in vitro</i> biological assessment, and molecular docking study of benzimidazole-based thiadiazole derivatives as dual inhibitors of α-amylase and α-glucosidase.
| S-EPMC10196468 | biostudies-literature
Unknown Design, synthesis, and molecular docking studies of diphenylquinoxaline-6-carbohydrazide hybrids as potent α-glucosidase inhibitors.
| S-EPMC9341091 | biostudies-literature
Unknown Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors.
| S-EPMC8757611 | biostudies-literature
Unknown Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking.
| S-EPMC6864627 | biostudies-literature
Unknown Benzimidazole Bearing Thiosemicarbazone Derivatives Act as Potent α-Amylase and α-Glucosidase Inhibitors; Synthesis, Bioactivity Screening and Molecular Docking Study.
| S-EPMC9609971 | biostudies-literature