Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer’s disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase

Riaz, Sadaf; Khan, Islam Ullah; Bajda, Marek; Ashraf, Muhammad; Quratulain, -; Shaukat, Ayesha; Rehman, Tanzeel U.; Mutahir, Sadaf; Hussain, Sajjad; Mustafa, Ghulam; Yar, Muhammad

doi:10.1016/j.bioorg.2015.09.008

Cited by 61 publications

(26 citation statements)

References 31 publications

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“…19) exhibited the most potent activity against tested enzymes such as AChE (IC 50 50.2 mM) and BChE (IC 50 43.8 mM). Overall the compound 219 bearing phenyl group was found to be active against all these tested enzymes [146]. On the other hand, Ulus et al described acridine-sulfonamide hybrids as potent acetylcholinesterase inhibitor for the treatment of Alzheimer's disease.…”

Section: Alzheimer's Disease (Ad)mentioning

confidence: 99%

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Zhao

Rakesh

Ravidar

et al. 2019

European Journal of Medicinal Chemistry

451

183

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a b s t r a c tSulfur (S VI ) based moieties, especially, the sulfonyl or sulfonamide based analogues have showed a variety of pharmacological properties, and its derivatives propose a high degree of structural diversity that has established useful for the finding of new therapeutic agents. The developments of new less toxic, low cost and highly active sulfonamides containing analogues are hot research topics in medicinal chemistry. Currently, more than 150 FDA approved Sulfur (S VI )-based drugs are available in the market, and they are widely used to treat various types of diseases with therapeutic power. This comprehensive review highlights the recent developments of sulfonyl or sulfonamides based compounds in huge range of therapeutic applications such as antimicrobial, anti-inflammatory, antiviral, anticonvulsant, antitubercular, antidiabetic, antileishmanial, carbonic anhydrase, antimalarial, anticancer and other medicinal agents. We believe that, this review article is useful to inspire new ideas for structural design and developments of less toxic and powerful Sulfur (S VI ) based drugs against the numerous death-causing diseases.

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Section: Alzheimer's Disease (Ad)mentioning

confidence: 99%

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Zhao

Rakesh

Ravidar

et al. 2019

European Journal of Medicinal Chemistry

451

183

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“…The increasing mortality rate, complexities in disease and the limited option of drugs for the curing of AD, demand new and more effective pharmacological products. Keeping these factors in view researchers is aiming to develop new potential drugs …”

Section: Introductionmentioning

confidence: 99%

Organocatalyzed Solvent Free and Efficient Synthesis of 2,4,5‐Trisubstituted Imidazoles as Potential Acetylcholinesterase Inhibitors for Alzheimer's Disease

Pervaiz

Mutahir

Ullah

et al. 2020

Chemistry & Biodiversity

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The catalytic potential of pyridine‐2‐carboxlic acid has been evaluated for efficient, green and solvent free synthesis of 2,4,5‐trisubstituted imidazole derivatives 3a–3m. The compounds 3a–3m were synthesized by one pot condensation reaction of substituted aromatic aldehydes, benzil, and ammonium acetate in good to excellent yields (74–96 %). To explore the potential of these compounds against Alzheimer's disease, their inhibitory activities against acetylcholinesterase (AChE) were evaluated. In this series of compounds, compound 3m, bearing one ethoxy and a hydroxy group on the phenyl ring on 2,4,5‐trisubstituted imidazoles, proved to be a potent AChE inhibitor (102.56±0.14). Structure–activity relationship (SAR) of these compounds was developed. Molecular dockings were carried out for the compounds 3m, 3e, 3k, 3c, 3a, 3d, 3j, and 3f in order to further investigate the binding mechanism. The inhibitor molecule was molecularly docked with acetylcholinesterase to further study its binding mechanism. The amino group of the compound 3m forms an H‐bond with the oxygen atom of the residue (i. e., THR121) which has a bond length of 3.051 Å.

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“…Sulfonamides, being antibacterial, having the prominent mechanism of action including attachment of sulfonamides with the dihydropteroate synthetase (DHPS) enzyme and alteration of bacterial pathways of folic acid synthesis in few eukaryotic cells, but in human beings, this mechanism is not followed [3,4]. The sulfonamides have been recognized due to various reported biological activities such as anticancer [5][6][7][8][9], anti-Alzheimer [10,11], anti-tubercular [12,13], antimicrobial [14][15][16][17], anti-inflammatory [18], carbonic anhydrase inhibitors [19][20][21][22], antidiabetic [11], anticonvulsant [23], and antimalarial [24][25][26].…”

Section: Introductionmentioning

confidence: 99%

“…Due to these facts, there is a prime need to shorten the duration of therapy and ascertain newer antimicrobial agents to avert the emergence of resistance. In continuation of our efforts dedicated toward development of antimicrobials, we have screened compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18) reported by Thakral and Singh [27] for antimicrobial potential along with QSAR and computational studies.…”

Section: Introductionmentioning

confidence: 99%

Biological Evaluation, Qsar and Molecular Modeling Studies of 2,4-Dichlorobenzoic Acid Derivatives as Antimicrobial Agents

Thakral

Singh

2019

Asian J Pharm Clin Res

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Objective: The aim of this study was to evaluate 2,4-dichlorobenzoic acid derivatives as antimicrobial agents through in vitro, QSAR and molecular docking studies. Methods: The compounds were subjected to in vitro antimicrobial screening by test tube dilution method and the structural characteristics governing the antimicrobial potential were studied using QSAR methodology. These compounds were also screened for docking simulation to find out binding confirmation of reported compounds with PDB 1aj0 and 5fsa using AutoDock tools and discovery studio. Results: The antimicrobial evaluation data indicated that compounds 13 and 18 were found to be the most effective against all the bacterial strains and Aspergillus niger while compounds 1 and 14 exhibited more antifungal potential against Candida albicans. QSAR studies confirmed the role of molar refractivity and Balaban index (J) as controlling parameters for antimicrobial potential. Molecular modeling study revealed that compounds interact with the active site of PDB by hydrophobic, hydrogen bonding, and Van der Wall interactions. Conclusion: These test compounds were identified as potent candidates for the control of microbial strains tested, and structural relationship with activity may provide valuable information for further design and synthesis of compounds with antimicrobial potential.

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Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer’s disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase

Cited by 61 publications

References 31 publications

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Organocatalyzed Solvent Free and Efficient Synthesis of 2,4,5‐Trisubstituted Imidazoles as Potential Acetylcholinesterase Inhibitors for Alzheimer's Disease

Biological Evaluation, Qsar and Molecular Modeling Studies of 2,4-Dichlorobenzoic Acid Derivatives as Antimicrobial Agents

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