BIOMAT Database Logo BIOMAT Database Logo

Synthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity. 2018

Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.

A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14-3.92 nM against AChE, 0.24-1.64 nM against BChE, 6.73-51.10 nM against α-glycosidase, 1.80-5.10 nM against hCA I, and 1.14-5.45 nM against hCA II.

UI MeSH Term Description Entries
D010696 Phloroglucinol A trinitrobenzene derivative with antispasmodic properties that is used primarily as a laboratory reagent. 1,3,5-Benzenetriol,Benzene-1,3,5-triol,Spasfon-Lyoc,Spassirex
D002091 Butyrylcholinesterase An aspect of cholinesterase (EC 3.1.1.8). Pseudocholinesterase,Benzoylcholinesterase,Butyrylthiocholinesterase
D002256 Carbonic Anhydrases A family of zinc-containing enzymes that catalyze the reversible hydration of carbon dioxide. They play an important role in the transport of CARBON DIOXIDE from the tissues to the LUNG. EC 4.2.1.1. Carbonate Dehydratase,Carbonic Anhydrase,Anhydrases, Carbonic,Dehydratase, Carbonate
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004593 Electrophorus A genus of fish, in the family GYMNOTIFORMES, capable of producing an electric shock that immobilizes fish and other prey. The species Electrophorus electricus is also known as the electric eel, though it is not a true eel. Eel, Electric,Electric Eel,Electrophorus electricus
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006026 Glycoside Hydrolases Any member of the class of enzymes that catalyze the cleavage of the glycosidic linkage of glycosides and the addition of water to the resulting molecules. Endoglycosidase,Exoglycosidase,Glycohydrolase,Glycosidase,Glycosidases,Glycoside Hydrolase,Endoglycosidases,Exoglycosidases,Glycohydrolases,Hydrolase, Glycoside,Hydrolases, Glycoside
D006736 Horses Large, hoofed mammals of the family EQUIDAE. Horses are active day and night with most of the day spent seeking and consuming food. Feeding peaks occur in the early morning and late afternoon, and there are several daily periods of rest. Equus caballus,Equus przewalskii,Horse, Domestic,Domestic Horse,Domestic Horses,Horse,Horses, Domestic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000110 Acetylcholinesterase An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7. Acetylcholine Hydrolase,Acetylthiocholinesterase,Hydrolase, Acetylcholine

Related Publications

Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Evaluation of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Inhibition Effects and Antioxidant Activity of Baicalin Hydrate.
October 2023, Life (Basel, Switzerland),
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
meta-Cyanobenzyl substituted benzimidazolium salts: Synthesis, characterization, crystal structure and carbonic anhydrase, α-glycosidase, butyrylcholinesterase, and acetylcholinesterase inhibitory properties.
July 2018, Archiv der Pharmazie,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors.
December 2017, Journal of enzyme inhibition and medicinal chemistry,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Screening of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Enzyme Inhibition Effects and Antioxidant Activity of Coumestrol.
May 2022, Molecules (Basel, Switzerland),
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Synephrine and phenylephrine act as α-amylase, α-glycosidase, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase enzymes inhibitors.
November 2017, Journal of biochemical and molecular toxicology,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Synthesis and discovery of potent carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase, and α-glycosidase enzymes inhibitors: The novel N,N'-bis-cyanomethylamine and alkoxymethylamine derivatives.
April 2018, Journal of biochemical and molecular toxicology,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Synthesis of diaryl ethers with acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase inhibitory actions.
January 2016, Journal of enzyme inhibition and medicinal chemistry,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Novel coumarin-chalcone derivatives: Synthesis, characterization, antioxidant, cyclic voltammetry, molecular modelling and biological evaluation studies as acetylcholinesterase, α-glycosidase, and carbonic anhydrase inhibitors.
September 2023, Chemico-biological interactions,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Design, synthesis, characterization, biological evaluation, and molecular docking studies of novel 1,2-aminopropanthiols substituted derivatives as selective carbonic anhydrase, acetylcholinesterase and α-glycosidase enzymes inhibitors.
January 2022, Journal of biomolecular structure & dynamics,
Serdar Burmaoglu, and Ali O Yilmaz, and Parham Taslimi, and Oztekin Algul, and Deryanur Kilic, and Ilhami Gulcin
Synthesis of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds - Determination of their carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase and α-glycosidase inhibition properties.
October 2020, Bioorganic chemistry,
Copied contents to your clipboard!