Inhibitory effects of the chalcones towards carbonic anhydrase I, II and acetylcholinesterase enzymes
Mehtap Tuğrak,Cem Yamali,Halise Inci Gul,Yeliz Demir +3 more
- Vol. 13, Iss: 3, pp 1138-1146
TLDR
The bioassay results showed that the compounds can be considered as the main frame to design novel chalcone-based enzyme inhibitors and the compounds 1, 3 and 5 were the best inhibitors against hCA I, hCA II, and AChE, respectively.Abstract:
Chalcones are known as versatile, innovative and bioactive chemical scaffolds in drug development studies. In this study, a series of poly-methoxylated chalcones (1-8) were synthesized by Claisen-Schmidt condensation under the basic condition and their carbonic anhydrase (CA) I/II and acetylcholinesterase (AChE) inhibitory effects were firstly evaluated in this study. CA isoenzymes I and II were inhibited in nanomolar concentration with Ki values of 8.75±0.64 - 37.64±2.38 nM (hCA I) and 11.47±3.31- 45.97±4.67 nM (hCA II). The compounds inhibited the AChE enzyme in the range of 34.14±20.79 - 53.65±13.25 nM. The compounds 1, 3 and 5 were the best inhibitors against hCA I, hCA II, and AChE, respectively. The bioassay results showed that the compounds can be considered as the main frame to design novel chalcone-based enzyme inhibitors.read more
Citations
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Design, Synthesis, and Biological Evaluation Studies of Novel Naphthalene-Chalcone Hybrids As Antimicrobial, Anticandidal, Anticancer, and VEGFR-2 Inhibitors
TL;DR: In this article , a series of 10 naphthalene-chalcone derivatives were synthesized and their anticancer-antibacterial-antifungal properties were investigated, and compound 2j showed activity against the A549 cell line with an IC50 = 7.835 ± 0.598 μM.
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.
Journal ArticleDOI
Carbonic anhydrases: novel therapeutic applications for inhibitors and activators
TL;DR: The biological rationale for the novel uses of inhibitors or activators of CA activity in multiple diseases is discussed, and progress in the development of specific modulators of the relevant CA isoforms is highlighted, some of which are now being evaluated in clinical trials.
Journal ArticleDOI
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
Chalcone Derivatives: Promising Starting Points for Drug Design.
Marcelo N. Gomes,Eugene N. Muratov,Maristela Pereira,Josana de Castro Peixoto,Lucimar Pinheiro Rosseto,Pedro Cravo,Carolina Horta Andrade,Bruno J. Neves,Bruno J. Neves +8 more
TL;DR: This review summarizes current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design) and presents successful examples of the use of chalcones.
Journal ArticleDOI
Designing of Novel Carbonic Anhydrase Inhibitors and Activators.
TL;DR: The use of such CA inhibitors (CAIs) as antiglaucoma drugs will be discussed in detail, together with the recent developments that led to isozyme-specific and organ-selective inhibitors.