Click synthesis of 1,2,3-triazole based imidazoles: Antitubercular evaluation, molecular docking and HSA binding studies

Kumar, C.B. Pradeep; Prathibha, B.S.; Prasad, K. N. N.; Raghu, M.S.; Prashanth, M.K.; Jayanna, B.K.; Alharthi, Fahad A.; Chandrasekhar, S.; Revanasiddappa, H. D.; Kumar, K. Deva Arun

doi:10.1016/j.bmcl.2021.127810

Cited by 35 publications

(8 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The 1,2,3-triazole pharmacophore unit contains some drugs present in the market, that is, carboxyamidotriazole, cefatrizine, and tazobactam, as shown in Figure . Triazole is a medicinally important pharmacophore unit showing various biological activities including antitubercular, antiproliferative, antibacterial, anticancerous, α-glucosidase inhibiting, antioxidant, and antifungal activities.…”

Section: Introductionmentioning

confidence: 99%

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

et al. 2021

View full text Add to dashboard Cite

The present work describes design of a small library of new 1,2,3-triazole-appended bis-pyrazoles by using a molecular hybridization approach, and the synthesized hybrids were evaluated for their antifungal activity against different fungal strains, namely, Candida albicans, Cryptococcus neoformans, Candida glabrata, Candida tropicalis, Aspergillus niger, and Aspergillus fumigatus. All the compounds exhibited broad-spectrum activity against the tested fungal strains with excellent minimum inhibitory concentration values. The molecular docking study against sterol 14α-demethylase (CYP51) could provide valuable insights into the binding modes and affinity of these compounds. Furthermore, these compounds were also evaluated for their antioxidant activity, which also resulted in promising data.

show abstract

Section: Introductionmentioning

confidence: 99%

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

et al. 2021

View full text Add to dashboard Cite

show abstract

“…The observed values of K q were higher than the bimolecular limiting diffusion rate constant of 2.0 × 10 10 M −1 s −1 , thereby confirming that the fluorescence of HSA was quenched by the static quenching mechanism. 34…”

Section: Biological Activitymentioning

confidence: 99%

“…The observed values of K q were higher than the bimolecular limiting diffusion rate constant of 2.0 Â 10 10 M À1 s À1 , thereby confirming that the fluorescence of HSA was quenched by the static quenching mechanism. 34 The following equation was used to calculate the values of the binding constant (K) and the number of binding sites: The binding constant of 4g-HSA was calculated from the intercept of the log (F 0 À F)/F vs. log[Q] plot and found to be 1.01 Â 10 4 M À1 . The value of n was obtained from the slope of the plot and calculated to be 0.861.…”

Section: Evaluation Of the Quenching Mechanism And Binding Constantmentioning

confidence: 99%

Fluorenone–thiazolidine-4-one scaffolds as antidiabetic and antioxidant agents: design, synthesis, X-ray crystal structures, and binding and computational studies

Doddagaddavalli

Kalalbandi²,

Naik³

et al. 2023

New J. Chem.

View full text Add to dashboard Cite

show abstract

“…[3] They consists of H-bonding and dipole interactions and thus it is pound to be an effective scaffold in pharma industry, and furthermore, triazole has high affinity toward the preparation of therapeutically important biological targets. [4] They exhibit pharmaceutical activities like antitubercular, [5] antiproliferative, [6] antibacterial, [7] anticancerous, [8] α-glucosidase inhibiting, [9] antioxidant, [10] antifungal, [11] antimalarial, [12] and antiviral. [13] Some important triazole biological active compounds are shown in Figure 1.…”

Section: Introductionmentioning

confidence: 99%

Preparation of novel pyrazole substituted triazole libraries and estimation of their biological activity

Laxminarayana,

Balha,

Tamminana

2023

ChemistrySelect

View full text Add to dashboard Cite

We have constructed a new library of 1,2,3-triazole tethered pyrazole derivatives (6 a-h & 7 a-h) from propargyl alcohol through simultaneous click process, oxidation, condensation, and rearrangement under mild reaction conditions. The final products were obtained in moderate to good yields. All the compound structures were characterized by analytical and spectral ( 1 H NMR, 13 C NMR & HRMS) studies. Furthermore, the evaluation of biological activity of newly synthesized molecules was done against three human cancer cell lines, such as HeLa (Human cervical cancer), A549 (Human alveolar adenocarcinoma), MCF-7 (Human breast adenocarcinoma). Compound 7 e has showed good anti-proliferation activity with HeLa (IC 50 0.13 � 0.02 μM), MCF-7 (IC 50 2.7 � 0.3 μM), while compounds 6 a and 6 g gave favourable anti-proliferation against above three human cancer cell lines, compared with the standard drug Doxorubicin.

show abstract

Click synthesis of 1,2,3-triazole based imidazoles: Antitubercular evaluation, molecular docking and HSA binding studies

Cited by 35 publications

References 33 publications

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking

Fluorenone–thiazolidine-4-one scaffolds as antidiabetic and antioxidant agents: design, synthesis, X-ray crystal structures, and binding and computational studies

Preparation of novel pyrazole substituted triazole libraries and estimation of their biological activity

Contact Info

Product

Resources

About