Journal ArticleDOI
Cholinesterases, α-glycosidase, and carbonic anhydrase inhibition properties of 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives: Synthetic analogues for the treatment of Alzheimer's disease and diabetes mellitus
TLDR
The inhibition type of the 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives at the receptors was determined and the data obtained in this work was evaluated.About:
This article is published in Bioorganic Chemistry.The article was published on 2020-04-01. It has received 43 citations till now. The article focuses on the topics: Carbonic Anhydrase I & Butyrylcholinesterase.read more
Citations
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Journal ArticleDOI
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
TL;DR: The recent strategies of various researchers related to the development of carbonic anhydrase inhibitors belonging to different structural classes like pyrimidine, pyrazoline, selenourea, isatin, indole, etc are compiled.
Journal ArticleDOI
Synthesis of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds - Determination of their carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase and α-glycosidase inhibition properties.
İlhami Gülçin,Boris A. Trofimov,Ruya Kaya,Parham Taslimi,Lyubov N. Sobenina,Elena Yu. Schmidt,Olga V. Petrova,Svetlana F. Malysheva,Nina K. Gusarova,Vagif Farzaliyev,Afsun Sujayev,Saleh Alwasel,Claudiu T. Supuran +12 more
TL;DR: In this article, the synthesis of compounds of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds were evaluated against the human erythrocyte carbonic anhydrase I, and II isoenzymes, butyrylcholinesterase (BChE), and α-glycosidase enzymes.
Journal ArticleDOI
Synthesis and antioxidant activities of phenol derivatives from 1,6-bis(dimethoxyphenyl)hexane-1,6-dione.
TL;DR: The antioxidant activities of novel synthesized seventeen molecules were investigated by analytical methods like ABTS•+ and DPPH• scavenging and some of the molecules record powerful antioxidant profile when compared to putative standards.
Journal ArticleDOI
Novel inhibitors with sulfamethazine backbone: synthesis and biological study of multi-target cholinesterases and α-glucosidase inhibitors.
Cüneyt Türkeş,Suleyman Akocak,Mesut Işık,Nebih Lolak,Parham Taslimi,Mustafa Durgun,İlhami Gülçin,Yakup Budak,Şükrü Beydemir +8 more
TL;DR: The underlying cause of many metabolic diseases is abnormal changes in enzyme activity in metabolism as discussed by the authors, which is the cause of mutations in enzymes such as cholinesterases (ChEs; acetylcholinestersterase, AChE and b...
Journal ArticleDOI
Synthesis, characterization, molecular docking, and biological activities of coumarin-1,2,3-triazole-acetamide hybrid derivatives.
Nima Sepehri,Maryam Mohammadi-Khanaposhtani,Nafise Asemanipoor,Samanesadat Hosseini,Mahmood Biglar,Bagher Larijani,Mohammad Mahdavi,Haleh Hamedifar,Parham Taslimi,Nastaran Sadeghian,İlhami Gülçin +10 more
TL;DR: The novel coumarin–1,2,3‐triazole‐acetamide hybrids had effective inhibition profiles against all tested metabolic enzymes and are potential drug candidates to treat diseases such as epilepsy, glaucoma, type‐2 diabetes mellitus (T2DM), Alzheimer's disease (AD), and leukemia.
References
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Journal ArticleDOI
A new and rapid colorimetric determination of acetylcholinesterase activity.
TL;DR: A photometric method for determining acetylcholinesterase activity of tissue extracts, homogenates, cell suspensions, etc., has been described and Kinetic constants determined by this system for erythrocyte eholinesterases are presented.
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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).
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Esterase Activities of Human Carbonic Anhydrases B and C
TL;DR: The data gave no evidence for the presence of an acyl intermediate; if such an intermediate exists it must be very rapidly hydrolyzed, and the pH dependence curves appear to reflect the catalytic center activity.
Journal ArticleDOI
Recent global trends in the prevalence and incidence of dementia, and survival with dementia
Martin Prince,Gemma-Claire Ali,Gemma-Claire Ali,Maëlenn Guerchet,A. Matthew Prina,Emiliano Albanese,Yu-Tzu Wu +6 more
TL;DR: A systematic review of studies of trends in prevalence, incidence and mortality for people with dementia, conducted since 1980 found no evidence to suggest that the current assumption of constant age-specific prevalence of dementia over time is ill-founded.
Journal ArticleDOI
Rapid screening and identification of α-glucosidase inhibitors from mulberry leaves using enzyme-immobilized magnetic beads coupled with HPLC/MS and NMR
TL;DR: An approach to screening α-glucosidase inhibitors from medicinal plants using enzyme-coated magnetic bead suggested that enzyme- coated magnetic beads may be suitable for discovering active compounds from medicinal plant.