Phytochemical Analysis, Antioxidant, Anticholinergic, Antidiabetic, and Antiglaucoma Potentials of Sage (Salvia adiyamanensis) DOI
Ahmet Zafer Tel, Kübra Aslan, İlhami Gülçın

et al.

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: April 10, 2025

Abstract In this study, the antioxidant effect of ethanolic extracts were prepared from aerial part Salvia adiyamanensis was investigated through five methods, including DPPH⋅, ABTS, and Fe3+, Cu2+, Fe3+-TPTZ reducing assays. The IC50 values extract determined as 35.40 ± 8.35 29.50 5.12 µg/mL for DPPH ABTS radicals scavenging enzyme inhibition property against α-glycosidase, acetylcholinesterase, butyrylcholinesterase, human carbonic anhydrase I, II, a result, IC50 30.78, 191.3, 8.02, 32.68 54.82 µg/mL, respectively. LC-MS/MS revealed that S. compromised characteristic phenolics rosmarinic acid, chlorogenic luteolin, quercetin, apigenin, caffeic acid Salvia genus. These findings strongly suggest has potential to be natural medicine treatment metabolic diseases such diabetes, Alzheimer’s disease, or glaucoma.

Language: Английский

Carboranes in drug discovery, chemical biology and molecular imaging DOI
Anita Marfavi, Poya Kavianpour, Louis M. Rendina

et al.

Nature Reviews Chemistry, Journal Year: 2022, Volume and Issue: 6(7), P. 486 - 504

Published: June 23, 2022

Language: Английский

Citations

121
Ligand based pharmacophore modelling and integrated computational approaches in the quest for small molecule inhibitors against hCA IX DOI Creative Commons
Venkatesan Saravanan, Bharath Kumar Chagaleti,

Shakthi Devi Packiapalavesam

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(5), P. 3346 - 3358

Published: Jan. 1, 2024

An integrated computational approach in search of potent hCA IX inhibitors.

Language: Английский

Citations

29
Synthesis, biological evaluation, and in silico studies of phenyl naphthalene-2-sulfonate derived thiosemicarbazones as potential carbonic anhydrase inhibitors DOI

Javeria Eshal,

Hafiza Zara Tariq, Jing Li

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 155, P. 108118 - 108118

Published: Jan. 4, 2025

Language: Английский

Citations

2
Discovery of new carbonic anhydrase IX inhibitors as anticancer agents by toning the hydrophobic and hydrophilic rims of the active site to encounter the dual-tail approach DOI
Haytham O. Tawfik,

Andrea Petreni,

Claudiu T. Supuran

et al.

European Journal of Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 232, P. 114190 - 114190

Published: Feb. 12, 2022

Language: Английский

Citations

48
Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII DOI Creative Commons

Tarfah Al‐Warhi,

Mostafa M. Elbadawi, Alessandro Bonardi

et al.

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 37(1), P. 2635 - 2643

Published: Sept. 22, 2022

In this work, different series of benzothiazole-based sulphonamides 8a-c, 10, 12, 16a-b and carboxylic acids 14a-c were developed as novel SLC-0111 analogues with the goal generating potent carbonic anhydrase (CA) inhibitors. The adopted strategy involved replacing 4-fluorophenyl tail in a benzothiazole motif that attached to ureido linker produce compounds 8c its regioisomers 8a-b. addition, spacer was elongated by methylene or ethylene groups afford counterparts 10 12. turn, primary sulfamoyl zinc binding group (ZBG) either substituted replaced acid functionality order provide secondary sulphonamide-based 16a-b, derivatives 14a-c, respectively. All (8a-c, 16a-b) tested for their ability inhibit CA isoforms I, II, IX XII. Additionally, vitro anticancer properties CAIs evaluated.

Language: Английский

Citations

33
Molecular mechanisms of topiramate and its clinical value in epilepsy DOI Creative Commons

Yun-Fei Bai,

Chang Zeng,

Miaomiao Jia

et al.

Seizure, Journal Year: 2022, Volume and Issue: 98, P. 51 - 56

Published: April 4, 2022

Language: Английский

Citations

30
Design and synthesis of 6-arylpyridine-tethered sulfonamides as novel selective inhibitors of carbonic anhydrase IX with promising antitumor features toward the human colorectal cancer DOI
Wagdy M. Eldehna, Eslam Essam Mohammed, Ghada H. Al-Ansary

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 258, P. 115538 - 115538

Published: June 1, 2023

Language: Английский

Citations

20
Carboxylate‐ and Sulfonate‐Containing Quinazolin‐4(3H)‐one Rings: Synthesis, Characterization, and Carbonic Anhydrase I–II and Acetylcholinesterase Inhibition Properties DOI
Feyzi Sinan Tokalı, Zuhal Alım, Ümit Yırtıcı

et al.

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(8)

Published: Feb. 21, 2023

Abstract Quinazolines are a group of bioactive heterocyclic compounds with wide range biological activities and have gained an important place in the design active drugs various targets due to their pharmacological properties. Carbonic anhydrase (CA) acetylcholinesterase (AChE) inhibitors very pharmacologically. In this study, inhibition effects newly synthesized quinazolin‐4(3 H )‐one derivatives on human erythrocyte CA‐I (hCA‐I) CA‐II (hCA‐II) isoenzyme AChE activity were investigated. The structures novel characterized by fourier‐transform infrared (FTIR), nuclear magnetic resonance (NMR), high‐resolution mass spectroscopy (HRMS). All molecules showed strong inhibitory effect all three enzymes. 4‐[(4‐Oxo‐2‐(phenoxymethyl)quinazolin‐3(4 )‐ylimino)methyl]phenyl furan‐2‐carboxylate for hCA‐I (IC 50 : 205 nM), 4‐[(4‐oxo‐2‐(phenoxymethyl)quinazolin‐3(4 isobutyrate hCA‐II 209 propionate 14.2 nM) that strongest effect. Molecular docking studies carried out elucidate possible interaction mechanism site affinity scores most hCA‐I, hCA‐II, determined as −134.765, −147.423, −175.354 MolDock Score, respectively.

Language: Английский

Citations

17
The potential of carbonic anhydrase enzymes as a novel target for anti-cancer treatment DOI
Xiaoqun Zhou, Xian‐Li Ma, Nur Syamimi Ariffin

et al.

European Journal of Pharmacology, Journal Year: 2024, Volume and Issue: 976, P. 176677 - 176677

Published: May 31, 2024

Language: Английский

Citations

7
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold DOI
Yie Kie Chong,

Yee Swen Ong,

Keng Yoon Yeong

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(6), P. 1798 - 1827

Published: Jan. 1, 2024

Decades ago, the application of cyclic sulfonamide (sultam) and its derivatives primarily focused on their antibacterial properties. However, recent years have seen a shift in research attention towards exploring potential as anticancer, anti-inflammatory, antidiabetic, antiviral agents. Despite this broadening scope, only few sultam drugs made it to commercial market, much sultams remains discovery phase. This class compounds holds significant promise pertinent pharmaceutical research. Due sultam's relevance growing importance drug discovery, review paper aims consolidate examine biological activities ranging from 4 8-membered ring structures.

Language: Английский

Citations

6