ChemInform Abstract: Two Isosteric Fluorinated Derivatives of the Powerful Glucosidase Inhibitors, 1-Deoxynojirimycin and 2,5-Dideoxy-2,5-imino-D-mannitol: Syntheses and Glycosidase-Inhibitory Activities of 1,2,5-Trideoxy-2- fluoro-1,5-imino-D-glucitol an

ChemInform ◽  
2010 ◽  
Vol 28 (40) ◽  
pp. no-no
Author(s):  
S. M. ANDERSEN ◽  
M. EBNER ◽  
C. W. EKHART ◽  
G. GRADNIG ◽  
G. LEGLER ◽  
...  
Keyword(s):  
Glucosidase Inhibitors ◽  
Inhibitory Activities ◽  
Fluorinated Derivatives ◽  
Derivatives Of

Synthesis and Biological Activity of Novel Deoxynojirimycin Derivatives as Potent α-Glucosidase Inhibitors

2013 ◽  
Vol 68 (4) ◽  
pp. 383-390 ◽  
Keyword(s):  
Biological Activity ◽  
Kinetic Parameters ◽  
Competitive Inhibitor ◽  
Skeletal Structures ◽  
Glucosidase Inhibitors ◽  
Ic50 Value ◽  
Inhibitory Activities ◽  
Derivatives Of

Thirteen 1-deoxynojirimycin (DNJ) derivatives of five different skeletal structures were designed and synthesized. The newly synthesized compounds were evaluated using an in vitro a- glucosidase assay, and kinetic parameters (Ki, IC50) were measured. Some DNJ derivatives showed weak a-glucosidase inhibitory activities, and the compounds 1-(3-benzyloxy-2-hydroxypropyl)- 2-hydroxymethyl-piperidine-3,4,5-triol (2a) and 1-{3-[1-(4-fluorophenyl)-1H-[1,2,3]triazol-4-ylmethoxy]- 2-hydroxypropyl}-2-hydroxymethyl-piperidine-3,4,5-triol (13d) showed activities comparable to that of DNJ. While 2a was found to be a reversible, non-competitive inhibitor of a-glucosidase with a Ki value of 1.56X10-4 M and an IC50 value of 3.07X10x4 M, 13d was a reversible, competitive inhibitor of a-glucosidase with a Ki value of 2.08X10-4 M and an IC50 value of 3.31X10-4 M.

scholarly journals Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Fariba Peytam ◽  
Ghazaleh Takalloobanafshi ◽  
Toktam Saadattalab ◽  
Maryam Norouzbahari ◽  
Zahra Emamgholipour ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Study ◽  
Rat Small Intestine ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Mild Conditions ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities

AbstractIn an attempt to find novel, potent α-glucosidase inhibitors, a library of poly-substituted 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines 3a–ag have been synthesized through heating a mixture of 2-aminobenzimidazoles 1 and α-azidochalcone 2 under the mild conditions. This efficient, facile protocol has been resulted into the desirable compounds with a wide substrate scope in good to excellent yields. Afterwards, their inhibitory activities against yeast α-glucosidase enzyme were investigated. Showing IC50 values ranging from 16.4 ± 0.36 µM to 297.0 ± 1.2 µM confirmed their excellent potency to inhibit α-glucosidase which encouraged us to perform further studies on α-glucosidase enzymes obtained from rat as a mammal source. Among various synthesized 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines, compound 3k exhibited the highest potency against both Saccharomyces cerevisiae α-glucosidase (IC50 = 16.4 ± 0.36 μM) and rat small intestine α-glucosidase (IC50 = 45.0 ± 8.2 μM). Moreover, the role of amine moiety on the observed activity was studied through substituting with chlorine and hydrogen resulted into a considerable deterioration on the inhibitory activity. Kinetic study and molecular docking study have confirmed the in-vitro results.

Concise synthesis of a new triterpenoid saponin from the roots of Gypsophila oldhamiana and its derivatives as α-glucosidase inhibitors

2016 ◽  
Vol 40 (11) ◽  
pp. 9537-9549 ◽  
Author(s):  
Qingchao Liu ◽  
Tiantian Guo ◽  
Fahui Li ◽  
Dong Li
Keyword(s):  
Triterpenoid Saponin ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities

The natural triterpenoid saponin 1 and its derivatives 2–3 were synthesized and exhibited potent inhibitory activities against α-glucosidase in vitro.

scholarly journals Synthesis and tyrosinase inhibitory activities of 4-oxobutanoate derivatives of carvacrol and thymol

2019 ◽  
Vol 29 (1) ◽  
pp. 56-58 ◽  
Author(s):  
Nicholas Brotzman ◽  
Yiming Xu ◽  
Allison Graybill ◽  
Alexander Cocolas ◽  
Andrew Ressler ◽  
...  
Keyword(s):  
Inhibitory Activities ◽  
Derivatives Of

scholarly journals Cinnamic Acid Derivatives as α-Glucosidase Inhibitor Agents

2017 ◽  
Vol 17 (1) ◽  
pp. 151 ◽  
Author(s):  
Teni Ernawati ◽  
Maksum Radji ◽  
Muhammad Hanafi ◽  
Abdul Mun’im ◽  
Arry Yanuar
Keyword(s):  
Functional Groups ◽  
Cinnamic Acid ◽  
Phenyl Group ◽  
Chemical Compounds ◽  
Cinnamic Acid Derivative ◽  
Cinnamic Acid Derivatives ◽  
Glucosidase Inhibitor ◽  
Glucosidase Inhibitors ◽  
Derivatives Of ◽  
Additive Reaction

This paper reviews biological activity of some cinnamic acid derivative compounds which are isolated from natural materials and synthesized from the chemical compounds as an agent of α-glucosidase inhibitors for the antidiabetic drug. Aegeline, anhydroaegeline and aeglinoside B are natural products isolated compounds that have potential as an α-glucosidase inhibitor. Meanwhile, α-glucosidase inhibitor class of derivatives of cinnamic acid synthesized compounds are p-methoxy cinnamic acid and p-methoxyethyl cinnamate. Chemically, cinnamic acid has three main functional groups: first is the substitution of the phenyl group, second is the additive reaction into the α-β unsaturated, and third is the chemical reaction with carboxylic acid functional groups. The synthesis and modification of the structure of cinnamic acid are very influential in inhibitory activity against α-glucosidase.

Ultrafast photoinduced charge transfer in fluorinated derivatives of DMABN

2004 ◽  
pp. 323-326
Author(s):  
S. Murali ◽  
P. Changenet-Barret ◽  
C. Ley ◽  
P. Plaza ◽  
W. Rettig ◽  
...  
Keyword(s):  
Charge Transfer ◽  
Photoinduced Charge Transfer ◽  
Fluorinated Derivatives ◽  
Photoinduced Charge ◽  
Derivatives Of

ChemInform Abstract: N-Alkylated Derivatives of 1,5-Dideoxy-1,5-iminoxylitol as β-Xylosidase and β-Glucosidase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 33 (31) ◽  
pp. no-no
Author(s):  
Herwig Haeusler ◽  
Karen Rupitz ◽  
Arnold E. Stuetz ◽  
Stephen G. Withers
Keyword(s):  
Glucosidase Inhibitors ◽  
Derivatives Of
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