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Article ; Online: Coumarin linked thiazole derivatives as potential α-glucosidase inhibitors to treat diabetes mellitus.

Ichale, Rushikesh / Kanhed, Ashish M / Vora, Amisha

2023

Abstract: Diabetes is a leading cause of kidney failure, blindness, heart attacks and lower limb amputation. Prevalence of diabetes is rising globally. α-glucosidase is validated target for controlling hyperglycemia because of its role in catalysing hydrolysis of ... ...

Abstract	Diabetes is a leading cause of kidney failure, blindness, heart attacks and lower limb amputation. Prevalence of diabetes is rising globally. α-glucosidase is validated target for controlling hyperglycemia because of its role in catalysing hydrolysis of carbohydrates to glucose in GIT. In an attempt to find novel safe and effective α-glucosidase inhibitors, coumarin linked thiazole was identified as potential scaffold on the basis of its interactions with the active site of α-glucosidase studied in silico. A series of coumarin linked thiazole derivatives were synthesized and analyzed for α-glucosidase inhibitory potential in an in-vitro assay. The synthesized molecules showed potent inhibition of α-glucosidase with IC50 values ranging from 0.14 to 9.38 μM. The most potent compound 2-[(4-bromophenyl) amino)-N-(4- (2-oxo-2H-chromen-3-yl) thiazol-2-yl] acetamide was further docked with α-glucosidase and molecular dynamics studies were carried out for 100 ns which suggested the stability of protein and ligand in the protein active site over the simulation period and role of hydrophobic interactions slightly more than the electrostatic/polar interactions in ligand- receptor stability. In summary, our results demonstrate efficacy of coumarin-linked thiazole as potential leads for further optimization and development.
Language	English
Publishing date	2023-04-29
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1376507-3
ISSN	1573-501X ; 1381-1991
ISSN (online)	1573-501X
ISSN	1381-1991
DOI	10.1007/s11030-023-10652-4
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Article ; Online: Effects of active compounds from

Peerzada, Zoya / Kanhed, Ashish M / Desai, Krutika B

RSC advances

2022 Volume 12, Issue 24, Page(s) 15196–15214

Abstract: Pseudomonas ... ...

Abstract	Pseudomonas aeruginosa
Language	English
Publishing date	2022-05-18
Publishing country	England
Document type	Journal Article
ISSN	2046-2069
ISSN (online)	2046-2069
DOI	10.1039/d1ra08351a
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Article: Effects of active compounds from Cassia fistula on quorum sensing mediated virulence and biofilm formation in Pseudomonas aeruginosa

Peerzada, Zoya / Kanhed, Ashish M. / Desai, Krutika B.

RSC advances. 2022 May 18, v. 12, no. 24

2022

Abstract: Pseudomonas aeruginosa infections are attributed to its ability to form biofilms and are difficult to eliminate with antibiotic treatment. Biofilm formation is regulated by quorum sensing (QS), an intracellular bacterial communication mechanism that ... ...

Abstract	Pseudomonas aeruginosa infections are attributed to its ability to form biofilms and are difficult to eliminate with antibiotic treatment. Biofilm formation is regulated by quorum sensing (QS), an intracellular bacterial communication mechanism that allows the activation of numerous virulence factors and secondary metabolites. Targeting the QS pathway is a potential approach that prevents QS-controlled phenotypes and biofilm formation. For the first time, the current work has identified antiquorum sensing activity in the partially purified four fractions from the hot ethyl acetate extract of Cassia fistula fruit pods. Of the four fractions, only fraction-1 gave decreased AHL activity; the phytoconstituents in this fraction were identified as rhein, 3-aminodibenzofuran, 5-(hydroxymethyl)-2-(dimethoxymethyl)furan, and dihydrorhodamine. Fraction-1 (1 mg ml⁻¹) and rhein (0.15 mg ml⁻¹) showed 63% and 42.7% reduction in short-chain AHL production, respectively, without hindering the bacterial growth. Fraction-1 inhibited QS-mediated extracellular virulence factors viz. protease, elastase, pyocyanin, and rhamnolipid (p < 0.05). Quantitative analysis of biofilm formation showed 77% & 62.4% reduction by fraction-1 (1 mg ml⁻¹) and rhein (0.15 mg ml⁻¹) respectively. Confocal laser microscopy (CLMS) & scanning electron microscopy (SEM) confirmed the reduction of biofilm formation in Pseudomonas aeruginosa upon treatment with fraction-1 and rhein. Moreover, the in vivo study displayed that fraction-1 and rhein (standard) significantly enhanced the survival of Caenorhabditis elegans by suppressing the potency of virulence factors of Pseudomonas aeruginosa. Quantitative real-time polymerase chain reaction results demonstrated the down-regulation of QS-related genes, lasI, lasR, rhlI, and rhlR. In addition, in silico analysis divulged that a component identified by GC-MS displayed a strong affinity towards LasI and LasR. These findings suggest that potent phytochemicals from fraction-1, including rhein, could serve as novel phytotherapeutics in controlling emerging infections of antibiotic-resistant bacterial pathogens like Pseudomonas aeruginosa.
Keywords	Caenorhabditis elegans ; Cassia fistula ; Pseudomonas aeruginosa ; antibiotic resistance ; antibiotics ; bacterial growth ; biofilm ; chemical constituents of plants ; computer simulation ; confocal laser scanning microscopy ; elastase ; ethyl acetate ; furans ; phytochemicals ; phytotherapy ; pyocyanin ; quantitative analysis ; quantitative polymerase chain reaction ; rhamnolipids ; secondary metabolites ; virulence
Language	English
Dates of publication	2022-0518
Size	p. 15196-15214.
Publishing place	The Royal Society of Chemistry
Document type	Article
ISSN	2046-2069
DOI	10.1039/d1ra08351a
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Identification of potential Mpro inhibitors for the treatment of COVID-19 by using systematic virtual screening approach.

Kanhed, Ashish M / Patel, Dushyant V / Teli, Divya M / Patel, Nirav R / Chhabria, Mahesh T / Yadav, Mange Ram

Molecular diversity

2020 Volume 25, Issue 1, Page(s) 383–401

Abstract: The Corona virus Disease (COVID-19) is caused because of novel coronavirus (SARS-CoV-2) pathogen detected in China for the first time, and from there it spread across the globe creating a worldwide pandemic of severe respiratory complications. The virus ... ...

Abstract	The Corona virus Disease (COVID-19) is caused because of novel coronavirus (SARS-CoV-2) pathogen detected in China for the first time, and from there it spread across the globe creating a worldwide pandemic of severe respiratory complications. The virus requires structural and non-structural proteins for its multiplication that are produced from polyproteins obtained by translation of its genomic RNA. These polyproteins are converted into structural and non-structural proteins mainly by the main protease (Mpro). A systematic screening of a drug library (having drugs and diagnostic agents which are approved by FDA or other world authorities) and the Asinex BioDesign library was carried out using pharmacophore and sequential conformational precision level filters using the Schrodinger Suite. From the screening of approved drug library, three antiviral agents ritonavir, nelfinavir and saquinavir were predicted to be the most potent Mpro inhibitors. Apart from these pralmorelin, iodixanol and iotrolan were also identified from the systematic screening. As iodixanol and iotrolan carry some limitations, structural modifications in them could lead to stable and safer antiviral agents. Screenings of Asinex BioDesign library resulted in 20 molecules exhibiting promising interactions with the target protein Mpro. They can broadly be categorized into four classes based on the nature of the scaffold, viz. disubstituted pyrazoles, cyclic amides, pyrrolidine-based compounds and miscellaneous derivatives. These could be used as potential molecules or hits for further drug development to obtain clinically useful therapeutic agents for the treatment of COVID-19.
MeSH term(s)	Antiviral Agents/therapeutic use ; COVID-19/virology ; Coronavirus 3C Proteases/antagonists & inhibitors ; Drug Evaluation, Preclinical/methods ; Humans ; Mass Screening/methods ; Molecular Docking Simulation ; Pandemics/prevention & control ; Protease Inhibitors/pharmacology ; SARS-CoV-2/drug effects ; SARS-CoV-2/metabolism ; Viral Nonstructural Proteins/antagonists & inhibitors ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; Protease Inhibitors ; Viral Nonstructural Proteins ; Coronavirus 3C Proteases (EC 3.4.22.28)
Keywords	covid19
Language	English
Publishing date	2020-07-31
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1376507-3
ISSN	1573-501X ; 1381-1991
ISSN (online)	1573-501X
ISSN	1381-1991
DOI	10.1007/s11030-020-10130-1
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Article ; Online: Carbazole-based semicarbazones and hydrazones as multifunctional anti-Alzheimer agents.

Patel, Kishan B / Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Gandhi, Bhumi / Shah, Bhavik S / Chaudhary, Bharat N / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

Journal of biomolecular structure & dynamics

2021 Volume 40, Issue 20, Page(s) 10278–10299

Abstract: With the aim to combat a multi-faceted neurodegenerative Alzheimer's disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and ... ...

Abstract	With the aim to combat a multi-faceted neurodegenerative Alzheimer's disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (
MeSH term(s)	Humans ; Cholinesterase Inhibitors/pharmacology ; Cholinesterase Inhibitors/chemistry ; Acetylcholinesterase/chemistry ; Semicarbazones/pharmacology ; Hydrazones ; Molecular Docking Simulation ; Carbazoles/pharmacology ; Carbazoles/chemistry ; Chelating Agents/pharmacology ; Chelating Agents/chemistry ; Antioxidants/pharmacology ; Antioxidants/chemistry ; Alzheimer Disease/drug therapy ; Structure-Activity Relationship
Chemical Substances	Cholinesterase Inhibitors ; Acetylcholinesterase (EC 3.1.1.7) ; hydrazinecarbothioamide ; Semicarbazones ; Hydrazones ; Carbazoles ; Chelating Agents ; Antioxidants
Language	English
Publishing date	2021-07-02
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	49157-3
ISSN	1538-0254 ; 0739-1102
ISSN (online)	1538-0254
ISSN	0739-1102
DOI	10.1080/07391102.2021.1942212
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Article ; Online: Discovery of novel N-methyl carbazole tethered rhodanine derivatives as direct inhibitors of Mycobacterium tuberculosis InhA.

Shaikh, Mahamadhanif S / Kanhed, Ashish M / Chandrasekaran, Balakumar / Palkar, Mahesh B / Agrawal, Nikhil / Lherbet, Christian / Hampannavar, Girish A / Karpoormath, Rajshekhar

Bioorganic & medicinal chemistry letters

2019 Volume 29, Issue 16, Page(s) 2338–2344

Abstract: InhA (Enoyl-ACP reductase) plays a crucial role in the biosynthetic pathway of cell wall synthesis in Mycobacterium tuberculosis (Mtb). Isoniazid (INH) is an important first-line drug, which inhibits InhA. The rapid increase in resistance to INH and ... ...

Abstract	InhA (Enoyl-ACP reductase) plays a crucial role in the biosynthetic pathway of cell wall synthesis in Mycobacterium tuberculosis (Mtb). Isoniazid (INH) is an important first-line drug, which inhibits InhA. The rapid increase in resistance to INH and currently marketed drugs as well as emergence of MDR-TB and XDR-TB has complicated the diagnosis and treatment of Mtb with ever increasing threat to human kind. Herein, we report novel N-methyl carbazole derivatives as potential anti-TB compounds acting directly via InhA inhibition. All the synthesized final compounds were screened against Mtb virulent cell line H
MeSH term(s)	Antitubercular Agents/chemical synthesis ; Antitubercular Agents/chemistry ; Antitubercular Agents/pharmacology ; Carbazoles/chemistry ; Carbazoles/pharmacology ; Dose-Response Relationship, Drug ; Drug Discovery ; Microbial Sensitivity Tests ; Molecular Structure ; Mycobacterium tuberculosis/drug effects ; Mycobacterium tuberculosis/enzymology ; Rhodanine/chemistry ; Rhodanine/pharmacology ; Structure-Activity Relationship
Chemical Substances	Antitubercular Agents ; Carbazoles ; carbazole (0P2197HHHN) ; Rhodanine (7O50LKL2G8)
Language	English
Publishing date	2019-06-14
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2019.06.015
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Article ; Online: Identification of potential Mpro inhibitors for the treatment of COVID-19 by using systematic virtual screening approach

Kanhed, Ashish M. / Patel, Dushyant V. / Teli, Divya M. / Patel, Nirav R. / Chhabria, Mahesh T. / Yadav, Mange Ram

Molecular Diversity ; ISSN 1381-1991 1573-501X

2020

Keywords	Physical and Theoretical Chemistry ; Inorganic Chemistry ; Organic Chemistry ; Molecular Biology ; Drug Discovery ; Catalysis ; Information Systems ; General Medicine ; covid19
Language	English
Publisher	Springer Science and Business Media LLC
Publishing country	us
Document type	Article ; Online
DOI	10.1007/s11030-020-10130-1
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Further Studies on Triazinoindoles as Potential Novel Multitarget-Directed Anti-Alzheimer's Agents.

Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Patel, Kishan B / Gandhi, Pallav M / Patel, Sagar P / Chaudhary, Bharat N / Shah, Dharti B / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

ACS chemical neuroscience

2020 Volume 11, Issue 21, Page(s) 3557–3574

Abstract: The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel ... ...

Abstract	The inadequate clinical efficacy of the present anti-Alzheimer's disease (AD) drugs and their low impact on the progression of Alzheimer's disease in patients have revised the research focus from single targets to multitarget-directed ligands. A novel series of substituted triazinoindole derivatives were obtained by introducing various substituents on the indole ring for the development of multitarget-directed ligands as anti-AD agents. The experimental data indicated that some of these compounds exhibited significant anti-AD properties. Among them, 8-(piperidin-1-yl)-
MeSH term(s)	Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Amyloid beta-Peptides/metabolism ; Animals ; Blood-Brain Barrier/metabolism ; Cholinesterase Inhibitors/pharmacology ; Drug Design ; Humans ; Ligands ; Mice ; Pharmaceutical Preparations ; Rats ; Structure-Activity Relationship
Chemical Substances	Amyloid beta-Peptides ; Cholinesterase Inhibitors ; Ligands ; Pharmaceutical Preparations ; Acetylcholinesterase (EC 3.1.1.7)
Language	English
Publishing date	2020-10-19
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.0c00448
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Article ; Online: Novel carbazole-stilbene hybrids as multifunctional anti-Alzheimer agents.

Patel, Dushyant V / Patel, Nirav R / Kanhed, Ashish M / Teli, Divya M / Patel, Kishan B / Joshi, Prashant D / Patel, Sagar P / Gandhi, Pallav M / Chaudhary, Bharat N / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

Bioorganic chemistry

2020 Volume 101, Page(s) 103977

Abstract: Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer's ... ...

Abstract	Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer's disease, a novel series of carbazole-based stilbene derivatives were designed by the fusion of carbazole ring with stilbene scaffold. The designed compounds were synthesized and evaluated for their anti-AD activities including cholinesterase inhibition, Aβ aggregation inhibition, antioxidant and metal chelation properties. Amongst them, (E)-1-(4-(2-(9-ethyl-9H-carbazol-3-yl)vinyl)phenyl)-3-(2-(pyrrolidin-1-yl)ethyl)thiourea (50) appeared to be the best candidate with good inhibitory activities against AChE (IC
MeSH term(s)	Alzheimer Disease/drug therapy ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Stilbenes/therapeutic use ; Structure-Activity Relationship
Chemical Substances	Stilbenes
Language	English
Publishing date	2020-05-26
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2020.103977
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Article ; Online: Indoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents.

Kanhed, Ashish M / Patel, Dushyant V / Patel, Nirav R / Sinha, Anshuman / Thakor, Priyanka S / Patel, Kishan B / Prajapati, Navnit K / Patel, Kirti V / Yadav, Mange Ram

Journal of biomolecular structure & dynamics

2020 Volume 40, Issue 6, Page(s) 2498–2515

Abstract: To confront a disease like Alzheimer's disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for ... ...

Abstract	To confront a disease like Alzheimer's disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for Alzheimer's disease, a series of indoloquinoxaline derivatives were designed and synthesized. In vitro cholinesterase inhibition studies revealed that all the synthesized compounds exhibited moderate to good cholinesterase inhibitory activity. 6-(6-(Piperidin-1-yl)hexyl)-6
MeSH term(s)	Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Amyloid beta-Peptides ; Cholinesterase Inhibitors/chemistry ; Cholinesterases/metabolism ; Drug Design ; Humans ; Ligands ; Molecular Docking Simulation ; Structure-Activity Relationship
Chemical Substances	Amyloid beta-Peptides ; Cholinesterase Inhibitors ; Ligands ; Acetylcholinesterase (EC 3.1.1.7) ; Cholinesterases (EC 3.1.1.8)
Language	English
Publishing date	2020-10-28
Publishing country	England
Document type	Journal Article
ZDB-ID	49157-3
ISSN	1538-0254 ; 0739-1102
ISSN (online)	1538-0254
ISSN	0739-1102
DOI	10.1080/07391102.2020.1840441
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