FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2790071180> ?p ?o ?g. }

• W2790071180 endingPage "229" @default.
• W2790071180 startingPage "221" @default.
• W2790071180 abstract "Glucokinase (GK) is the main enzyme which controls the blood glucose levels in a safe and narrow physiological range in humans. GK activators are the novel type of therapeutic agents which act on GK enzyme and show their anti-diabetic potential. The present work was planned to synthesize and evaluate the antidiabetic potential of a new series of thiazole-2-yl benzamide derivatives as potential GK activators. A series of thiazole-2-yl benzamide derivatives were synthesized from benzoic acid and evaluated by in vitro enzymatic assay for GK activation. In silico docking studies were carried out to determine the binding interactions for the best fit conformations in the allosteric site of GK enzyme. Based on the results of in vitro enzyme assay and in silico studies, the selected molecules were tested for their antidiabetic activity in the oral glucose tolerance test (OGTT). The results of the in vitro enzymatic assay were found to be in accordance to that of in silico studies. Amongst the synthesized molecules, compounds 1, 2, 5 and 8 displayed good in vitro GK activation (activation fold between 1.48 and 1.83). Compounds 2 and 8 exhibited highest antidiabetic activity in OGTT studies. The results of the in vivo antidiabetic studies were found to be in parallel to that of docking and in vitro studies. These newly synthesized thiazol-2-yl benzamide derivatives thus can be treated as the initial hits for the development of new, safe, effective and orally bioavailable GK activators as therapeutic agents for the treatment of type 2 diabetes." @default.
• W2790071180 created "2018-03-29" @default.
• W2790071180 creator A5033469809 @default.
• W2790071180 creator A5041962364 @default.
• W2790071180 creator A5043957222 @default.
• W2790071180 creator A5060524726 @default.
• W2790071180 date "2018-04-01" @default.
• W2790071180 modified "2023-09-29" @default.
• W2790071180 title "Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators" @default.
• W2790071180 cites W1966753603 @default.
• W2790071180 cites W1968195928 @default.
• W2790071180 cites W1972695067 @default.
• W2790071180 cites W1989585701 @default.
• W2790071180 cites W2005110124 @default.
• W2790071180 cites W2025758722 @default.
• W2790071180 cites W2028078645 @default.
• W2790071180 cites W2032689953 @default.
• W2790071180 cites W2037809940 @default.
• W2790071180 cites W2043203394 @default.
• W2790071180 cites W2043985474 @default.
• W2790071180 cites W2048598152 @default.
• W2790071180 cites W2052993305 @default.
• W2790071180 cites W2055911662 @default.
• W2790071180 cites W2056967386 @default.
• W2790071180 cites W2058591039 @default.
• W2790071180 cites W2070793266 @default.
• W2790071180 cites W2075194050 @default.
• W2790071180 cites W2086802315 @default.
• W2790071180 cites W2087927715 @default.
• W2790071180 cites W2091992338 @default.
• W2790071180 cites W2094732496 @default.
• W2790071180 cites W2100125011 @default.
• W2790071180 cites W2105668062 @default.
• W2790071180 cites W2125812684 @default.
• W2790071180 cites W2126946832 @default.
• W2790071180 cites W2132041174 @default.
• W2790071180 cites W2134293572 @default.
• W2790071180 cites W2138404388 @default.
• W2790071180 cites W2140415161 @default.
• W2790071180 cites W2155905771 @default.
• W2790071180 cites W2509277076 @default.
• W2790071180 cites W2920057851 @default.
• W2790071180 doi "https://doi.org/10.1016/j.compbiolchem.2018.02.018" @default.
• W2790071180 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29518630" @default.
• W2790071180 hasPublicationYear "2018" @default.
• W2790071180 type Work @default.
• W2790071180 sameAs 2790071180 @default.
• W2790071180 citedByCount "30" @default.
• W2790071180 countsByYear W27900711802018 @default.
• W2790071180 countsByYear W27900711802019 @default.
• W2790071180 countsByYear W27900711802020 @default.
• W2790071180 countsByYear W27900711802021 @default.
• W2790071180 countsByYear W27900711802022 @default.
• W2790071180 countsByYear W27900711802023 @default.
• W2790071180 crossrefType "journal-article" @default.
• W2790071180 hasAuthorship W2790071180A5033469809 @default.
• W2790071180 hasAuthorship W2790071180A5041962364 @default.
• W2790071180 hasAuthorship W2790071180A5043957222 @default.
• W2790071180 hasAuthorship W2790071180A5060524726 @default.
• W2790071180 hasConcept C104317684 @default.
• W2790071180 hasConcept C150903083 @default.
• W2790071180 hasConcept C159110408 @default.
• W2790071180 hasConcept C166342909 @default.
• W2790071180 hasConcept C181199279 @default.
• W2790071180 hasConcept C185592680 @default.
• W2790071180 hasConcept C202751555 @default.
• W2790071180 hasConcept C207001950 @default.
• W2790071180 hasConcept C2775905019 @default.
• W2790071180 hasConcept C2778464347 @default.
• W2790071180 hasConcept C2780231548 @default.
• W2790071180 hasConcept C33618052 @default.
• W2790071180 hasConcept C41685203 @default.
• W2790071180 hasConcept C55493867 @default.
• W2790071180 hasConcept C71240020 @default.
• W2790071180 hasConcept C71924100 @default.
• W2790071180 hasConcept C86803240 @default.
• W2790071180 hasConcept C98274493 @default.
• W2790071180 hasConcept C98335778 @default.
• W2790071180 hasConceptScore W2790071180C104317684 @default.
• W2790071180 hasConceptScore W2790071180C150903083 @default.
• W2790071180 hasConceptScore W2790071180C159110408 @default.
• W2790071180 hasConceptScore W2790071180C166342909 @default.
• W2790071180 hasConceptScore W2790071180C181199279 @default.
• W2790071180 hasConceptScore W2790071180C185592680 @default.
• W2790071180 hasConceptScore W2790071180C202751555 @default.
• W2790071180 hasConceptScore W2790071180C207001950 @default.
• W2790071180 hasConceptScore W2790071180C2775905019 @default.
• W2790071180 hasConceptScore W2790071180C2778464347 @default.
• W2790071180 hasConceptScore W2790071180C2780231548 @default.
• W2790071180 hasConceptScore W2790071180C33618052 @default.
• W2790071180 hasConceptScore W2790071180C41685203 @default.
• W2790071180 hasConceptScore W2790071180C55493867 @default.
• W2790071180 hasConceptScore W2790071180C71240020 @default.
• W2790071180 hasConceptScore W2790071180C71924100 @default.
• W2790071180 hasConceptScore W2790071180C86803240 @default.
• W2790071180 hasConceptScore W2790071180C98274493 @default.
• W2790071180 hasConceptScore W2790071180C98335778 @default.
• W2790071180 hasLocation W27900711801 @default.

• next