112450-33-6Relevant academic research and scientific papers
Synthesis, in-vitro evaluation, molecular docking, and kinetic studies of pyridazine-triazole hybrid system as novel α-glucosidase inhibitors
Moghimi, Setareh,Salarinejad, Somayeh,Toolabi, Mahsa,Firoozpour, Loghman,Esmaeil Sadat Ebrahimi, Seyed,Safari, Fatemeh,Madani-Qamsari, Fatemeh,Mojtabavi, Somayeh,Faramarzi, Mohammad Ali,Karima, Saeed,Pakrad, Roya,Foroumadi, Alireza
, (2021)
In this study, we reported the discovery of pyridazine based 1,2,3-triazole derivatives as inhibitors of α-glucosidase. All target compounds exhibited significant inhibitory activities against yeast and rat α-glucosidase enzymes compared to positive control, acarbose. The most potent compound 6j, ethyl 3-(2-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)ethyl)-5,6-diphenylpyridazine-4-carboxylate exhibited IC50 values of 58, and 73 μM. Docking studies indicated the responsibility of hydrophobic and hydrogen bonding interactions in the ligand-enzyme complex stability. The in-vitro safety against the normal cell line was observed by toxicity evaluation of the selected compounds.
Design and synthesis of novel pyridazine N-aryl acetamides: In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies
Faramarzi, Mohammad Ali,Firoozpour, Loghman,Foroumadi, Alireza,Moghimi, Setareh,Mojtabavi, Somayeh,Sadat Ebrahimi, Seyed Esmaeil,Safari, Fatemeh,Salarinejad, Somayeh,Toolabi, Mahsa
, (2020/07/21)
We herein applied the four step-synthetic route to prepare the pyridazine core attached to the various N-aryl acetamides. By this approach, a new series of pyridazine-based compounds were synthesized, characterized and evaluated for their activities against α-glucosidase enzyme. In-vitro α-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited α-glucosidase with the IC50 value of 70.1 μM. The most potent compounds showed no cytotoxicity against HDF cell line. Molecular docking and kinetic studies were performed to determine the modes of interaction and inhibition, respectively.
Design and synthesis of some thieno[2,3-c]pyridazine derivatives of expected anticancer activity
El-Ansary, Afaf K.,Kamal, Aliaa M.,Al-Ghorafi, Mokhtar Abdhafiz
, p. 2589 - 2601 (2013/07/26)
Design and synthesis of some new thienopyridazine derivatives as anticancer agents were the goal of this work. Accordingly, a series of novel compounds were synthesized via reacting thienopyridazine carboxylic acid hydrazide with different organic reagents. Twelve novel compounds were selected by National Cancer Institute for a full anticancer screening assay where seven of the investigated compounds showed non-selective broad spectrum and promising activity almost against all cancer cell lines. One of the most active compounds was chosen to be evaluated against 60-cell line panel at five concentration levels and revealed a remarkable growth inhibition activity.
Synthesis of novel thieno[2,3-c]pyridazines and related heterocycles
Radwan, Shaban M.,Bakhite, Etify A.
, p. 1117 - 1128 (2007/10/03)
The reaction of ethyl 2,3-dihydro-5,6-diphenyl-3-thioxopyridazine-4-carboxylate with ω-bromoacetophenones, chloro-N-arylacetamides, chloroacetonitrile, ethyl chloroacetate, or chloroacetone furnished the corresponding 4,5-diphenyl-3-hydroxy thieno [2,3-c]pyridazines. 2-Cyano-, 2-ethoxycabonyl-, and 2-acetyl-4,5-diphenyl-3-hydroxythieno[2,3-c]pyridazines were employed as precursors in the synthesis of some novel furo [2′,3′:4,5]thieno[2,3-c]pyridazines, pyrano-[2′,3′:4,5]thieno[2,3-c]pyridazines, and thieno[2,3-c]pyridazines. The antibacterial and antifungal activities of some of the compounds are reported.
