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, , , , , , and . 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.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8482464 | PMC |
| http://dx.doi.org/10.1021/acsomega.1c03734 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Exploring the synthetic potential of a g-CN·SOH ionic liquid catalyst for one-pot synthesis of 1,1-dihomoarylmethane scaffolds Knoevenagel-Michael reaction.
RSC Adv
April 2023
Synthetic Organic Chemistry Laboratory, Department of Chemistry, MLSU Udaipur-313001 Rajasthan India
A highly promising approach for the synthesis of functionalized 1,1-dihomoarylmethane scaffolds (bis-dimedones, bis-cyclohexanediones, bis-pyrazoles, and bis-coumarins) using g-CN·SOH ionic liquid Knoevenagel-Michael reaction has been developed and the synthesized derivatives were well characterized using spectral studies. The method involved the reaction of C-H activated acids with a range of aromatic aldehydes, in a 2 : 1 ratio catalyzed by a g-CN·SOH ionic liquid catalyst. The use of g-CN·SOH as a catalyst has several benefits, such as low cost, easy preparation, and high stability.
View Article and Find Full Text PDFNew 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking.
ACS Omega
September 2021
Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, Maharashtra, India.
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, , , , , , and . 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.
View Article and Find Full Text PDFNovel bis(pyrazole-benzofuran) hybrids possessing piperazine linker: Synthesis of potent bacterial biofilm and MurB inhibitors.
Bioorg Chem
September 2020
Chemistry Department, Faculty of Science, Cairo University, Giza 12613, Egypt. Electronic address:
Novel 1,4-bis[(2-(3-(dimethylamino)-1-oxoprop-2-en-1-yl)benzofuran-5-yl)methyl]piperazine was prepared and used as a key synthon for the this study. Therefore, 1,3-dipolar cycloaddition of this synthon with the appropriate hydrazonyl chlorides afforded a new series of bis(1,3,4-trisubstituted pyrazoles), linked via piperazine moiety. Furthermore, it reacted with hydrazine hydrate and phenyl hydrazine individually to afford the corresponding 1,4-bis[(2-(1H-pyrazolyl)benzofuran-5-yl)methyl]piperazines.
View Article and Find Full Text PDFOxone-DMSO Triggered Methylene Insertion and C(sp)-C(sp)-H-C(sp) Bond Formation to Access Functional Bis-Heterocycles.
J Org Chem
April 2020
Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India.
Metal-free insertion of a methylene group was achieved for the construction of a new C(sp)-C(sp)-H-C(sp) bond in order to prepare novel bis-heterocyclic scaffolds. The complete mechanistic investigations included experimental study and DFT calculations, and various symmetric and unsymmetric bis-pyrazoles as well as other pyrazole-based bis-heterocyclic molecules were prepared in moderate to high yields. Further modification of the bridged methylene group in the unsymmetric pyrazoles generated a chiral center to extend the scope of this method.
View Article and Find Full Text PDFBiologically active scaffolds: Synthesis, characterization and studies of oxino bis-pyrazoles by environmental friendly method.
Pak J Pharm Sci
March 2019
Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their α-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!