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Article ; Online: Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide.

Kumari, Ginna / Dhillon, Sudeep / Rani, Priyanka / Chahal, Mamta / Aneja, Deepak Kumar / Kinger, Mayank

ACS omega

2024 Volume 9, Issue 17, Page(s) 18709–18746

Abstract: Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide ... ...

Abstract	Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide alkaloids, metabolites, and cyclopeptides, have demonstrated a broad spectrum of pharmacological potentials. Given their profound biological significance, a plethora of thiazole-based hybrids have been synthesized through the conjugation of thiazole moieties with bioactive pyrazole and pyrazoline fragments. This review systematically presents a compendium of robust methodologies for the synthesis of thiazole-linked hybrids, employing the (3 + 2) heterocyclization reaction, specifically the Hantzsch-thiazole synthesis, utilizing phenacyl bromide as the substrate. The strategic approach of molecular hybridization has markedly enhanced drug efficacy, mitigated resistance to multiple drugs, and minimized toxicity concerns. The resultant thiazole-linked hybrids exhibit a myriad of medicinal properties
Language	English
Publishing date	2024-04-16
Publishing country	United States
Document type	Journal Article ; Review
ISSN	2470-1343
ISSN (online)	2470-1343
DOI	10.1021/acsomega.3c10299
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Unravelling the synthetic and therapeutic aspects of five, six and fused heterocycles using Vilsmeier-Haack reagent.

Chahal, Mamta / Dhillon, Sudeep / Rani, Priyanka / Kumari, Ginna / Aneja, Deepak Kumar / Kinger, Mayank

RSC advances

2023 Volume 13, Issue 38, Page(s) 26604–26629

Abstract: The aim of this review is to encapsulate the synthetic protocols and medicinal aspects of a wide range of heterocyclic compounds using the Vilsmeier-Haack (V. H.) reagent. These derivatives act as excellent precursors having different aryl ring ... ...

Abstract	The aim of this review is to encapsulate the synthetic protocols and medicinal aspects of a wide range of heterocyclic compounds using the Vilsmeier-Haack (V. H.) reagent. These derivatives act as excellent precursors having different aryl ring functionalities and could be used for the synthesis of a variety of heterocyclic scaffolds. The V. H. reagent, a versatile reagent in organic chemistry, is used to formylate various heterocyclic compounds of medicinal interest. Due to the different chemical interactions, efficacy, and potency of V. H. reagents, plenty of heterocyclic compounds can be synthesized which serve as a constituent in various novel medications and acts as a bridge between biology and chemistry. These carboxylate moieties can effectively cooperate as precursors for several multi-component reactions (MCR) including Strecker synthesis, Bucherer-Berg reaction and post-MCR cyclization, modified variants with various pharmaceutical applications such as anti-tumor, anti-convulsant, anti-chitosomal and so on.
Language	English
Publishing date	2023-09-05
Publishing country	England
Document type	Journal Article ; Review
ISSN	2046-2069
ISSN (online)	2046-2069
DOI	10.1039/d3ra04309f
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Article ; Online: Advances in Aβ imaging probes: a comprehensive study of radiolabelled 1,3-diaryl-2-propen-1-ones for Alzheimer's disease: a review.

Dhillon, Sudeep / Kinger, Mayank / Rani, Priyanka / Chahal, Mamta / Kumari, Ginna / Aneja, Deepak Kumar / Kim, Sang Wook / Choi, Eunseok / Kumar, Sushil

RSC advances

2023 Volume 13, Issue 51, Page(s) 35877–35903

Abstract: Alzheimer's disease (AD) is a formidable neurodegenerative disorder characterized by cognitive decline, memory impairment and inability to perform everyday tasks. In the pursuit of innovative diagnostic and therapeutic strategies, the synthesis and ... ...

Abstract	Alzheimer's disease (AD) is a formidable neurodegenerative disorder characterized by cognitive decline, memory impairment and inability to perform everyday tasks. In the pursuit of innovative diagnostic and therapeutic strategies, the synthesis and application of radiolabelled compounds have garnered significant attention. This review delves into the synthesis and biological significance of radiolabelled 1,3-diaryl-2-propen-1-ones, commonly known as chalcones, as Aβ imaging probes for AD. These versatile chalcone derivatives have demonstrated noteworthy potential as radiotracers for visualizing Aβ imaging probes, which are hallmark pathologies of AD. This review encompasses an exploration of chalcone synthesis
Language	English
Publishing date	2023-12-11
Publishing country	England
Document type	Journal Article ; Review
ISSN	2046-2069
ISSN (online)	2046-2069
DOI	10.1039/d3ra06258a
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Article ; Online: In Vitro Studies on a Microfluidic Sensor with Embedded Obstacles Using New Antibacterial Synthetic Compounds (1-TDPPO) Mixed Prop-2-en-1-one with Difluoro Phenyl.

Roh, Changhyun / Lee, Jaewoong / Kinger, Mayank / Kang, Chankyu

Sensors (Basel, Switzerland)

2017 Volume 17, Issue 4

Abstract: This paper describes the use of an analytical microfluidic sensor for accelerating chemo-repellent response and strong anti-bacterial 1-(Thien-2-yl)-3-(2, 6-difluoro phenyl) prop-2-en-1-one (1-TDPPO). The chemically-synthesized antimicrobial agent, which ...

Abstract	This paper describes the use of an analytical microfluidic sensor for accelerating chemo-repellent response and strong anti-bacterial 1-(Thien-2-yl)-3-(2, 6-difluoro phenyl) prop-2-en-1-one (1-TDPPO). The chemically-synthesized antimicrobial agent, which included prop-2-en-1-one and difluoro phenyl groups, was moving through an optically transparent polydimethylsiloxane (PDMS) microfluidic sensor with circular obstacles arranged evenly. The response, growth and distribution of fluorescent labeling
Language	English
Publishing date	2017-04-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2052857-7
ISSN	1424-8220 ; 1424-8220
ISSN (online)	1424-8220
ISSN	1424-8220
DOI	10.3390/s17040803
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Some Important Dietary Polyphenolic Compounds: An Anti-inflammatory and Immunoregulatory Perspective.

Kinger, Mayank / Kumar, Sushil / Kumar, Vinod

Mini reviews in medicinal chemistry

2017 Volume 18, Issue 15, Page(s) 1270–1282

Abstract: Inflammation plays an important role in maintaining the body's homeostasis. It repairs the damaged tissues of the body resulting from injury or infection. In addition, a diverse array of diseases like hepatitis, arthritis and colitis has been reported ... ...

Abstract	Inflammation plays an important role in maintaining the body's homeostasis. It repairs the damaged tissues of the body resulting from injury or infection. In addition, a diverse array of diseases like hepatitis, arthritis and colitis has been reported and described to be associated with inflammatory processes. Some autoimmune diseases like inflammatory bowel disease (IBD) emerge by the influence of numerous genes in complex environmental situations belong to inflammation. The currently available processes for curing inflammation and related disorders facilitate the use of non steroidal antiinflammatory drugs (NSAIDs). Moreover, intolerable side effects are also associated with the consumption of these medications. It is well known that phenolic compounds, largely present in vegetables and fruits, serve as an integral part of normal human diet besides having great medicinal value. These are considered to reflect a variety of anti-inflammatory properties, and can be used as an alternate natural source for the prevention of chronic inflammatory disorders. This mini-review summarized the antiinflammatory benefits of plants derived very prominent dietary polyphenolic compounds particularly, Oleocanthal, Curcumin, Resveratrol and Quercetin.
MeSH term(s)	Aldehydes/chemistry ; Aldehydes/therapeutic use ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Anti-Inflammatory Agents, Non-Steroidal/therapeutic use ; Autoimmune Diseases/pathology ; Autoimmune Diseases/prevention & control ; Curcumin/chemistry ; Curcumin/metabolism ; Curcumin/therapeutic use ; Diet ; Humans ; Neutrophils/drug effects ; Neutrophils/immunology ; Neutrophils/metabolism ; Phenols/chemistry ; Phenols/therapeutic use ; Polyphenols/chemistry ; Polyphenols/pharmacology ; Polyphenols/therapeutic use ; Quercetin/chemistry ; Quercetin/therapeutic use ; Resveratrol ; Stilbenes/chemistry ; Stilbenes/therapeutic use
Chemical Substances	Aldehydes ; Anti-Inflammatory Agents, Non-Steroidal ; Phenols ; Polyphenols ; Stilbenes ; Quercetin (9IKM0I5T1E) ; oleocanthal (AC7QO6038O) ; Curcumin (IT942ZTH98) ; Resveratrol (Q369O8926L)
Language	English
Publishing date	2017-02-09
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	2104081-3
ISSN	1875-5607 ; 1389-5575
ISSN (online)	1875-5607
ISSN	1389-5575
DOI	10.2174/1389557517666170208143410
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Zs.A 5891: Show issues

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Article ; Online: Synthesis and evaluation of curcumin-based near-infrared fluorescent probes for the in vivo optical imaging of amyloid-β plaques.

Park, Yong Dae / Kinger, Mayank / Min, Changho / Lee, Sang Yeob / Byun, Youngjoo / Park, Jin Woo / Jeon, Jongho

Bioorganic chemistry

2021 Volume 115, Page(s) 105167

Abstract: The abnormal self-assembly of amyloid-beta (Aβ) peptides into oligomers, as well as insoluble fibrils, has been identified as a key factor for monitoring the progression of Alzheimer's disease (AD). The noninvasive imaging of Aβ aggregates utilizing ... ...

Abstract	The abnormal self-assembly of amyloid-beta (Aβ) peptides into oligomers, as well as insoluble fibrils, has been identified as a key factor for monitoring the progression of Alzheimer's disease (AD). The noninvasive imaging of Aβ aggregates utilizing chemical probes can be a powerful and practical technique for accurately diagnosing and monitoring the progress of AD, as well as evaluating the effectiveness of therapeutic drug candidates in treating or managing it. Particularly, the near-infrared (NIR) fluorescence imaging of Aβ plaques is a potentially promising approach toward the efficient detection of the biomarker. In this study, we describe a new NIR fluorophore, which was based on curcumin derivatives. The fluorophore is equipped with desirable optical properties for in vivo brain imaging. The emission wavelength of the probe, 8b, is 667 nm, and its fluorescent intensity is significantly increased through binding with the Aβ aggregates. The probe allows the clear visualization of the Aβ plaques 10 min post administration, and the intensity of the fluorescent signal in the brain of a 5XFAD transgenic mouse model is more than three times higher than that of the normal control group. These results demonstrate that the designed probe can be an effective tool for visualizing Aβ plaques, as well as investigating the pathological progress of AD.
MeSH term(s)	Alzheimer Disease/metabolism ; Alzheimer Disease/pathology ; Amyloid beta-Peptides/chemistry ; Amyloid beta-Peptides/metabolism ; Animals ; Binding Sites ; Brain/diagnostic imaging ; Brain/metabolism ; Curcumin/chemistry ; Curcumin/metabolism ; Female ; Fluorescent Dyes/chemical synthesis ; Fluorescent Dyes/metabolism ; Humans ; Mice ; Mice, Transgenic ; Molecular Docking Simulation ; Optical Imaging/methods ; Protein Aggregates ; Spectroscopy, Near-Infrared
Chemical Substances	Amyloid beta-Peptides ; Fluorescent Dyes ; Protein Aggregates ; Curcumin (IT942ZTH98)
Language	English
Publishing date	2021-07-16
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.2021.105167
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 4207: Show issues

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Article ; Online: Synthesis and inhibitory effects of some novel 1,3-diarylprop-2-en-1-one analogues in Foxp3 expression: a novel class of anti-cancer candidates.

Kinger, Mayank / Park, Jeong Hoon / Hur, Min Goo / Kim, Sang Wook / Yang, Seung Dae

Medicinal chemistry (Shariqah (United Arab Emirates))

2013 Volume 9, Issue 8, Page(s) 1035–1040

Abstract: A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4(+)T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The ... ...

Abstract	A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4(+)T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The structure-activity relationship (SAR) of the R1 and R2 modification was studied to identify a candidate with the maximum potency. Of these compounds, 3d showed the highest inhibitory activity of FOX P3 gene expression and apoptosis (66.5 % inhibition at 10 μM). To the best of the authors' knowledge this is the first report of 1,3- diarylprop-2-en-1-ones as regulators of FOX P3 gene expression.
MeSH term(s)	Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/classification ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; CD4-Positive T-Lymphocytes/drug effects ; Cell Differentiation/drug effects ; Dose-Response Relationship, Drug ; Forkhead Transcription Factors/genetics ; Gene Expression Regulation/drug effects ; Gene Expression Regulation/genetics ; Male ; Mice ; Molecular Structure ; Propiophenones/chemical synthesis ; Propiophenones/chemistry ; Propiophenones/pharmacology ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Spleen/cytology ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; Forkhead Transcription Factors ; Foxp3 protein, mouse ; Propiophenones ; Pyrazoles
Language	English
Publishing date	2013-05-27
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1875-6638
ISSN (online)	1875-6638
DOI	10.2174/15734064113099990029
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Article: Design, synthesis, and anti-influenza viral activities of 1,3-diarylprop-2-en-1-ones: A novel class of neuraminidase inhibitors

Kinger, Mayank / Park, Yong Dae / Park, Jeong Hoon / Hur, Min Goo / Jeong, Hyung Jae / Park, Su-Jin / Lee, Woo Song / Kim, Sang Wook / Yang, Seung Dae

Archives of pharmacal research. 2012 Apr., v. 35, no. 4

2012

Abstract: A series of 1,3-diarylprop-2-en-1-one derivatives 3a-v have been synthesized and evaluated for their ability to inhibit neuraminidase (NA). Among the prepared compounds, the less lipophilic derivative 3k showed the most potent in vitro inhibitory ... ...

Abstract	A series of 1,3-diarylprop-2-en-1-one derivatives 3a-v have been synthesized and evaluated for their ability to inhibit neuraminidase (NA). Among the prepared compounds, the less lipophilic derivative 3k showed the most potent in vitro inhibitory activity against NA with an IC50 value of 1.5 ∝M.
Keywords	Orthomyxoviridae ; antiviral properties ; inhibitory concentration 50 ; organic compounds ; sialidase
Language	English
Dates of publication	2012-04
Size	p. 633-638.
Publishing place	Springer-Verlag
Document type	Article
ZDB-ID	447623-2
ISSN	0253-6269
ISSN	0253-6269
DOI	10.1007/s12272-012-0406-2
Database	NAL-Catalogue (AGRICOLA)

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Zs.B 3229: Show issues

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Article: Design, synthesis, and anti-influenza viral activities of 1,3-diarylprop-2-en-1-ones: a novel class of neuraminidase inhibitors.

Kinger, Mayank / Park, Yong Dae / Park, Jeong Hoon / Hur, Min Goo / Jeong, Hyung Jae / Park, Su-Jin / Lee, Woo Song / Kim, Sang Wook / Yang, Seung Dae

Archives of pharmacal research

2012 Volume 35, Issue 4, Page(s) 633–638

Abstract	A series of 1,3-diarylprop-2-en-1-one derivatives 3a-v have been synthesized and evaluated for their ability to inhibit neuraminidase (NA). Among the prepared compounds, the less lipophilic derivative 3k showed the most potent in vitro inhibitory activity against NA with an IC(50) value of 1.5 μM.
MeSH term(s)	Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Drug Design ; Humans ; Influenza A virus/enzymology ; Influenza B virus/enzymology ; Influenza, Human/drug therapy ; Influenza, Human/virology ; Molecular Structure ; Neuraminidase/antagonists & inhibitors ; Propiophenones/chemical synthesis ; Propiophenones/chemistry ; Propiophenones/pharmacology ; Structure-Activity Relationship
Chemical Substances	Antiviral Agents ; Propiophenones ; Neuraminidase (EC 3.2.1.18)
Language	English
Publishing date	2012-03
Publishing country	Korea (South)
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	447623-2
ISSN	1976-3786 ; 0253-6269
ISSN (online)	1976-3786
ISSN	0253-6269
DOI	10.1007/s12272-012-0406-2
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