This paper describes the design, development, synthesis, in silico, and in vitro evaluation of fourteen novel heterocycle hybrids as inhibitors of the α-glucosidase enzyme. The primary aim of this study was to explore the potential of novel pyrazole-phthalazine hybrids as selective inhibitors of α-glucosidase, an enzyme involved in carbohydrate metabolism, which plays a key role in the management of type 2 diabetes. The rationale for this study stems from the need for new, more effective inhibitors of α-glucosidase with improved efficacy and safety profiles compared to currently available therapies like Acarbose.
View Article and Find Full Text PDFChem Biodivers
July 2022
Tyrosinase plays a pivotal role in the hyperpigmentation and enzymatic browning of fruit and vegetable. Therefore, tyrosinase inhibitors can be of interest in industries as depigmentation compounds as well as anti-browning agents. In the present study, a series of chlorophenylquinazolin-4(3H)-one derivative were rationally designed and synthesized.
View Article and Find Full Text PDFA novel series of phenoxymethybenzoimidazole derivatives (9a-n) were rationally designed, synthesized, and evaluated for their α-glycosidase inhibitory activity. All tested compounds displayed promising α-glycosidase inhibitory potential with IC values in the range of 6.31 to 49.
View Article and Find Full Text PDFA new series of arylmethylene hydrazine derivatives bearing 1,3-dimethylbarbituric moiety 7a-o were designed, synthesized, and evaluated for their in vitro urease inhibitory activity. All the title compounds displayed high anti-urease activity, with IC values in the range of 0.61 ± 0.
View Article and Find Full Text PDFMelanin pigment and melanogenesis are a two-edged sword. Melanin has a radioprotection role while melanogenesis has undesirable effects. Targeting the melanogenesis pathway, a series of kojyl thioether conjugated to different quinazolinone derivatives were designed, synthesized, and evaluated for their inhibitory activity against mushroom tyrosinase.
View Article and Find Full Text PDFBioorg Chem
April 2021
A series of new quinazolinone-dihydropyrano[3,2-b]pyran derivatives 10A-L were synthesized by simple chemical reactions and were investigated for inhibitory activities against α-glucosidase and α-amylase. New synthesized compounds showed high α-glucosidase inhibition effects in comparison to the standard drug acarbose and were inactive against α-amylase. Among them, the most potent compound was compound 10L (IC value = 40.
View Article and Find Full Text PDFIn this study, novel quinazolinone derivatives 7a-n were synthesized and evaluated against metabolic enzymes including α-glycosidase, acetylcholinesterase, butyrylcholinesterase, human carbonic anhydrase I, and II. These compounds exhibited high inhibitory activities in comparison to used standard inhibitors with K values in the range of 19.28-135.
View Article and Find Full Text PDFIn this paper, we introduce various definitions of R-duals, to be called R-duals of type I, II, which leads to a generalization of the duality principle in Banach spaces. A basic problem of interest in connection with the study of R-duals in Banach spaces is that of characterizing those R-duals which can essentially be regarded as M-basis. We give some conditions under which an R-dual sequence to be an M-basis for .
View Article and Find Full Text PDFFourteen novel 4,5-diphenyl-imidazol-1,2,3-triazole hybrids 8a-n were synthesized with good yields by performing click reaction between the 4,5-diphenyl-2-(prop-2-yn-1-ylthio)-1H-imidazole and various benzyl azides. The synthesized compounds 8a-n were evaluated against yeast α-glucosidase, and all these compounds exhibited excellent inhibitory activity (IC values in the range of 85.6 ± 0.
View Article and Find Full Text PDFIn this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC = 90.4-246.
View Article and Find Full Text PDFA novel series of biscoumarin-1,2,3-triazole hybrids 6a-n was prepared and evaluated for α-glucosidase inhibitory potential. All fourteen derivatives exhibited excellent α-glucosidase inhibitory activity with IC values ranging between 13.0 ± 1.
View Article and Find Full Text PDF