Antihyperglycemic Activity of Phenyl and Ortho-Hydroxy Phenyl Linked Imidazolyl Triazolo Hydroxamic Acid Derivatives

Pal, Dilipkumar; Kumar, Singh Anil; Saha, Supriyo

doi:10.22159/ijpps.2017v9i12.22086

Cited by 7 publications

(3 citation statements)

References 16 publications

(13 reference statements)

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“…The cytotoxic activity study was performed at different concentrations (10,20,30,40, and 50 µg/mL) against lung cancer cell line (A549) by in vitro MTT cell viability assay. In present study, untreated A549 cells were considered as control group, whereas cis-platin treated A549 cells were considered as positive control.…”

Section: In Vitro Cytotoxic Activitymentioning

confidence: 99%

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Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives

et al. 2022

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Beta-aryl keto hexanoic acids (5a-l) were synthesized efficiently, followed by esterification that afforded beta-aryl keto methylhexanoates (6a-l). The chemo-selective ketoxime beta-aryl methyl hexanoates (7a-l) were isolated in good yields. Spectroscopic methods were used to characterize the obtained moieties. The antioxidant, anti-inflammatory, and antibacterial properties of the effectively synthesized compounds 7a-l were also investigated. The anti-inflammatory activity of the compounds 7c, 7f, 7i, and 7l was excellent, with a low IC50 value at micromolar concentration, which was much better than the reference diclofenac. All synthesized compounds 7a-l were assessed for their in vitro antibacterial activity against S. aureus, B. subtilis and E. coli. Most of the compounds exhibited promising activity against Gram-positive bacterial strain, compound 7i showed excellent activity compared to standard streptomycin and in the case of E. coli, compounds 7b, 7c, 7j, 7k and 7l have shown moderate activity. Further, the cytotoxic activities of the compounds were assessed against lung cancer cells (A549) by using MTT assay. The possible interaction mechanism of the molecules 7c and 7g with Gram-negative strain E. coli DNA gyrase B in complex with PDB ID: 4DUH was studied.

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Section: In Vitro Cytotoxic Activitymentioning

confidence: 99%

“…Oximes of carbonyl group compounds are significant not only for shielding, refining, and structural identification but also for converting a wide range of functional groups [8]. When an oxime is made with a keto-carbonyl group and the introduction of oxime group in a molecule, its biological activity increases considerably [9,10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives

et al. 2022

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“…In US, variants like B.1.1.7 (α), B.1.351 (β), B.1.617.2 (δ) and P.1 (γ) were concerned as variants of concern without any variants of high consequence 6,7 . Variants of interest were certain genetic markers that hampered viral transmission, diagnosis, and response towards therapeutic dose; variants of concern created a high impact on the response towards diagnosis, treatment regime with a possible increment of viral transmission, disease condition, and response towards vaccination whereas variants with less response towards diagnosis, treatment and vaccination 8,9 10 . When a patient is hospitalized, only some FDA-approved drugs were administered to cure the patient.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2023

IJPSR

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We are in the half past of 2022, but still, we are facing the coronavirus pandemic situation. When a patient is hospitalized, only some FDAapproved drugs were administered to cure the patient. In treating coronavirus infection, nitazoxanide, granulocyte-macrophage colony-stimulating factor inhibitors, and various monoclonal antibodies are present. But all the molecules used in the treatment were not so effective in fully curing the patient. So, to break this jinx to develop of newer generation anti-SARS-CoV-2 drug molecules, computational approaches played an essential role. 2D QSAR studies related to anti-SARS-CoV-2 molecule development, some QSAR models observed with good statistical parameters such as R 2 : 0.748, cross-validated Q 2 (LOO): 0.628, external predicted R 2 : 0.723 and another model suggested with R 2 : 0.764, Q 2 : 0.627 and R m 2 : 0.610, Q 2 (F 1 ): 0.727, Q 2 (F 1 ): 0.652, MAE score: 0.127. We developed a new 2D QSAR model with a higher number of molecules and greater statistical parameters. A dataset of 84 anti-SARS-CoV2 molecules was obtained from literature followed by descriptor calculation PADEL software; the QSAR model was generated using the Modelability index, dataset pretreatment, division, MLR equation, validation, and Y randomization test. The model was pIC50 = -1.79268(+/-0.3652) +0.07995(+/-0.03551) naaaC -0.4051(+/-0.09672) nsssN -0.45945(+/-0.11025) SHsOH +1.23189(+/-0.28144) ETA_BetaP with R 2 and Q 2 values were 0.87028 and 0.70493 with MAE fitness score value: 0.14298. Atoms E-state and electronic features of the molecules directly related to anti-SARS-CoV-2 drug activity. It can be easily concluded that we want to develop a small molecule effective against SARS-CoV-2 disease in the near future.

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Elicitor Signal Transduction Leading to the Production of Plant Secondary Metabolites

Saha¹,

Pal

2020

Advanced Structured Materials

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Antihyperglycemic Activity of Phenyl and Ortho-Hydroxy Phenyl Linked Imidazolyl Triazolo Hydroxamic Acid Derivatives

Cited by 7 publications

References 16 publications

Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives

Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives

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Elicitor Signal Transduction Leading to the Production of Plant Secondary Metabolites

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