Amériques

Chiasson, Herménégilde

doi:10.2307/j.ctt1ww3wkk.13

Cited by 1 publication

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It converts poly-and oligosaccharides into monomers by hydrolysis, and as a result the concentration of glucose in the blood increases. 2 Alpha-glucosidase inhibitors slow down the digestion process and carbohydrate absorption. As a result, a rapid increase in blood glucose level after a meal can be controlled independent of insulin.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, molecular docking, and pharmacological evaluation of halobenzodithiophene derivatives against alpha-glucosidase, urease, and free radical production

Abbas¹,

Hassan²,

Al‐Harrasi³

et al. 2018

Turk J Chem

View full text Add to dashboard Cite

Benzodithiophenes are heterocyclic compounds that have various medicinal and industrial applications. In the present study, halobenzodithiophene, the simplest benzofused thiophene, and its derivatives were synthesized and evaluated against alpha-glucosidase, urease, and free radical production. In the alpha-glucosidase inhibition assay, compound 2,2-bisbenzothiophne (1) exhibited potent activity with IC 50 = 135 ± 0.51 µ M, while its derivative 2,7-bis(butoxycarbonyl)-3,6-dichlorobenzo[1,2b ;6,5b ']dithiophene (2) exhibited promising inhibition with IC 50 = 263 ± 0.32 µ M. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging assay, compound 2 exhibited promising activity with IC 50 = 33 ± 0.42 µ M, while compound 1 showed moderate inhibition in the urease inhibition assay. Molecular docking studies determined the possible interaction of benzodithiophene and alpha-glucosidase on the basis of binding energy and scoring function. Structure-activity relationship analysis revealed that compound 2,7-bis (butoxycarbonyl)-3,6-dichlorobenzo[1,2b ;6,5b '] dithiophene (2) containing two chlorine substitutions exhibited more alpha-glucosidase inhibition (IC 50 = 263 ± .0.32 µ M) than other derivatives. Moreover, compound 2,7-bis (butoxycarbonyl)-3,6-dichlorobenzo[1,2b ;6,5b '] dithiophene (2) with two chlorine substitutions exhibited potent DPPH radical scavenging activity compared to other derivatives.

show abstract

Section: Introductionmentioning

confidence: 99%