Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents

Molecules, Journal Year: 2022, Volume and Issue: 27(13), P. 3994 - 3994

Published: June 21, 2022

For many decades, the thiazole moiety has been an important heterocycle in world of chemistry. The ring consists sulfur and nitrogen such a fashion that pi (π) electrons are free to move from one bond other bonds rendering aromatic properties. On account its aromaticity, reactive positions where donor–acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing ring, when entering physiological systems, behave unpredictably reset system differently. These molecules activate/stop biochemical pathways enzymes or stimulate/block receptors biological systems. Therefore, medicinal chemists have focusing their efforts on thiazole-bearing compounds order develop novel therapeutic agents for variety pathological conditions. This review attempts inform readers three major classes molecules: Thiazoles as treatment drugs, thiazoles clinical trials, preclinical developmental stages. A compilation is presented, brief synthetic description studies relating structure-based activity analysis. authors expect current succeed drawing attention finding new leads, which later be translated into drugs.

Language: Английский

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Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

RSC Advances, Journal Year: 2022, Volume and Issue: 12(31), P. 19764 - 19855

Published: Jan. 1, 2022

The present review focuses on various heterocyclic scaffolds and their role in designing developing new potential AChE BChE inhibitors to treat AD.

Language: Английский

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Exploration of 1,2,3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase

Bioorganic & Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 77, P. 117111 - 117111

Published: Nov. 29, 2022

Language: Английский

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Cytotoxic effect, enzyme inhibition, and in silico studies of some novel N-substituted sulfonyl amides incorporating 1,3,4-oxadiazol structural motif

Molecular Diversity, Journal Year: 2022, Volume and Issue: 26(5), P. 2825 - 2845

Published: April 9, 2022

Language: Английский

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Design, synthesis, biological evaluation and molecular docking studies of novel 1H-1,2,3-Triazole derivatives as potent inhibitors of carbonic anhydrase, acetylcholinesterase and aldose reductase

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1257, P. 132613 - 132613

Published: Feb. 10, 2022

Language: Английский

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Discovery of novel benzenesulfonamides incorporating 1,2,3-triazole scaffold as carbonic anhydrase I, II, IX, and XII inhibitors

International Journal of Biological Macromolecules, Journal Year: 2023, Volume and Issue: 239, P. 124232 - 124232

Published: March 29, 2023

Language: Английский

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Design, synthesis, characterization, in vitro and in silico evaluation of novel imidazo[2,1-b][1,3,4]thiadiazoles as highly potent acetylcholinesterase and non-classical carbonic anhydrase inhibitors

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 113, P. 105009 - 105009

Published: May 23, 2021

Language: Английский

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Synthesis, Characterization, and Inhibition Study of Novel Substituted Phenylureido Sulfaguanidine Derivatives as α‐Glycosidase and Cholinesterase Inhibitors

Chemistry & Biodiversity, Journal Year: 2021, Volume and Issue: 18(4)

Published: Feb. 23, 2021

Abstract A series of six N ‐carbamimidoyl‐4‐(3‐substituted phenylureido)benzenesulfonamide derivatives were synthesized by reaction sulfaguanidine with aromatic isocyanates. In vitro and in silico inhibitory effects the novel ureido‐substituted investigated spectrophotometric methods for α‐glycosidase (α‐GLY), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes associated diabetes mellitus (DM) Alzheimer's disease (AD). ‐Carbamimidoyl‐4‐{[(3,4‐dichlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide ( 2f ) showed AChE BChE effects, K I values 515.98±45.03 nM 598.47±59.18 nM, respectively, while ‐carbamimidoyl‐4‐{[(3‐chlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide 2e strong α‐GLY effect, 103.94±13.06 nM. The antidiabetic compounds are higher than their anti‐Alzheimer's because inhibition effect on diabetic enzyme is greater esterase enzymes. Indeed, metabolic important treatment DM AD.

Language: Английский

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Novel benzoic acid derivatives: Synthesis and biological evaluation as multitarget acetylcholinesterase and carbonic anhydrase inhibitors

Archiv der Pharmazie, Journal Year: 2020, Volume and Issue: 354(3)

Published: Nov. 6, 2020

Abstract Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced that human carbonic anhydrases (hCAs) serve as an important target for treatment. In this direction, the improvement new multitarget drugs, which can simultaneously modulate several mechanisms or targets included pathway, may be potent strategy to treat AD. light these data understanding developing AD‐related AChE hCAs inhibitors, study, novel methylene‐aminobenzoic acid tetrahydroisoquinolynyl‐benzoic derivatives ( 4a – g 6a ) were designed. synthesized analogs experimentally validated their effects vitro direct enzymatic tests. Also, compounds subjected silico monitoring with Schrödinger Suite software assign binding affinities potential based on Glide XP scoring, molecular mechanics‐generalized Born surface area computing, validation docking. results revealed 6c (1,3‐dimethyldihydropyrimidine‐2,4‐(1 H ,3 )‐dione‐substituted, K I value 33.00 ± 0.29 nM), 6e (cyclohexanone‐substituted, 18.78 0.09 6f (2,2‐dimethyl‐1,3‐dioxan‐4‐one‐substituted, 13.62 0.21 nM) from benzoic series most promising derivatives, they exhibited good multifunctional inhibition at all experimental levels against hCA I, II, AChE, respectively,

Language: Английский

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Molecular docking and inhibition studies of vulpinic, carnosic and usnic acids on polyol pathway enzymes

Journal of Biomolecular Structure and Dynamics, Journal Year: 2021, Volume and Issue: 40(22), P. 12008 - 12021

Published: Aug. 23, 2021

Aldose reductase (AR) and sorbitol dehydrogenase (SDH) are important enzymes of the polyol pathway. In current study, inhibitory effects vulpinic acid (VA) carnosic (CA) usnic (UA) on purified AR SDH were determined. These inhibition could be essential to prevent diabetic complications. from sheep kidney. Then, VA, CA UA tested in various concentrations against these activity vitro. KI values found as 1.46 ± 0.04, 5.13 0.25 11.71 0.27 μΜ for UA, respectively, AR. constants 15.32 0.34, 145.60 2.17 213.40 2.64 SDH. findings indicate that useful treatment complications.Communicated by Ramaswamy H. Sarma

Language: Английский

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