Synthesis, <scp>SAR</scp> and docking studies of substituted aryl phenylthiazolyl phenylcarboxamide as potential protein tyrosine phosphatase 1B (<scp>PTP</scp>1B) inhibitors

Varshney, Kanika; Gupta, Amit K.; Rawat, Arun K.; Srivastava, Rohit; Mishra, Akansha; Saxena, Mridula; Srivastava, Arvind K.; Jain, Sudha; Saxena, Anil Kumar

doi:10.1111/cbdd.13515

Cited by 6 publications

(2 citation statements)

References 24 publications

(35 reference statements)

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“…Acyl isothiocyanates are predominant bioactive compounds having many biological activities and are versatile precursors to the preparation of sulfur-containing heterocycles [1][2][3][4][5][6][7] .…”

Section: Introductionmentioning

confidence: 99%

Sebacoyl Isothiocyanate in the Synthesis of Bis (1,3,4-Thiadiazole, 1,3,4-Thiadiazolo[3,2-a]Pyridine, 4-Thiazolidinone, Chromenes, and Naphtho[1,2-b][1,4]Oxazine) Derivatives

Thabet¹

2020

Orient. J. Chem

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Section: Introductionmentioning

confidence: 99%

Sebacoyl Isothiocyanate in the Synthesis of Bis (1,3,4-Thiadiazole, 1,3,4-Thiadiazolo[3,2-a]Pyridine, 4-Thiazolidinone, Chromenes, and Naphtho[1,2-b][1,4]Oxazine) Derivatives

Thabet¹

2020

Orient. J. Chem

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“…Additionally, the interaction of compound 23 with Arg47 and Asp48 may explain its superior selectivity over homologous phosphatases. Compound 23 exhibited potential antihyperglycemic, antidyslipidemic, and insulin‐resistance‐reversing effects in vivo in the streptozotocin and db/db mice models (Varshney et al, 2019).…”

Section: Synthetic Ptp1b Inhibitorsmentioning

confidence: 99%

A comprehensive review on the research progress of PTP1B inhibitors as antidiabetics

Agrawal,

Dhakrey,

Pathak

2023

Chem Biol Drug Des

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Diabetes mellitus (DM) is a serious global health concern affecting over 500 million people. To put it simply, it is one of the most dangerous metabolic illnesses. Insulin resistance is the root cause of 90% of all instances of diabetes, all of which are classified as Type 2 DM. Untreated, it poses a hazard to civilization since it can lead to terrifying consequences and even death. Oral hypoglycemic medicines presently available act in a variety of ways, targeting various organs and pathways. The use of protein tyrosine phosphatase 1B (PTP1B) inhibitors, on the contrary, is a novel and effective method of controlling type 2 diabetes. PTP1B is a negative insulin signaling pathway regulator; hence, inhibiting PTP1B increases insulin sensitivity, glucose absorption, and energy expenditure. PTP1B inhibitors also restore leptin signaling and are considered a potential obesity target. In this review, we have compiled a summary of the most recent advances in synthetic PTP1B inhibitors from 2015 to 2022 which have scope to be developed as clinical antidiabetic drugs.

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A Library of Thiazolidin‐4‐one Derivatives as Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitors: An Attempt To Discover Novel Antidiabetic Agents

Patel

Pasha²,

Lunagariya³

et al. 2020

ChemMedChem

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Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin‐4‐one derivatives 8–22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5‐(Furan‐2‐ylmethylene)‐2‐(4‐nitrophenylimino)thiazolidin‐4‐one (17) exhibited potency with a competitive type of enzyme inhibition. structure–activity relationship studies revealed various structural facets important for the potency of these analogues. The findings revealed a requirement for a nitro group‐including hydrophobic heteroaryl ring for PTP1B inhibition. Molecular docking studies afforded good correlation with experimental results. H‐bonding and π–π interactions were responsible for optimal binding and effective stabilization of virtual protein‐ligand complexes. Furthermore, in‐silico pharmacokinetic properties of test compounds predicted their drug‐like characteristics for potential oral use as antidiabetic agents.Additionally, a binding site model demonstrating crucial pharmacophoric characteristics influencing potency and binding affinity of inhibitors has been proposed, which can be employed in the design of future potential PTP1B inhibitors.

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Synthesis, SAR and docking studies of substituted aryl phenylthiazolyl phenylcarboxamide as potential protein tyrosine phosphatase 1B (PTP1B) inhibitors

Cited by 6 publications

References 24 publications

Sebacoyl Isothiocyanate in the Synthesis of Bis (1,3,4-Thiadiazole, 1,3,4-Thiadiazolo[3,2-a]Pyridine, 4-Thiazolidinone, Chromenes, and Naphtho[1,2-b][1,4]Oxazine) Derivatives

Sebacoyl Isothiocyanate in the Synthesis of Bis (1,3,4-Thiadiazole, 1,3,4-Thiadiazolo[3,2-a]Pyridine, 4-Thiazolidinone, Chromenes, and Naphtho[1,2-b][1,4]Oxazine) Derivatives

A comprehensive review on the research progress of PTP1B inhibitors as antidiabetics

A Library of Thiazolidin‐4‐one Derivatives as Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitors: An Attempt To Discover Novel Antidiabetic Agents

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