863609-14-7Relevant academic research and scientific papers
[HDBU][HSO4]-catalyzed facile synthesis of new 1,2,3-triazole-tethered 2,3-dihydroquinazolin-4[1H]-one derivatives and their DPPH radical scavenging activity
Akolkar, Satish V.,Khedkar, Vijay M.,Nagargoje, Amol A.,Pisal, Parshuram M.,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.,Siddiqui, Madiha M.
, (2022/01/19)
A simple and efficient protocol has been developed for the synthesis of new1,2,3-triazole-2,3-dihydroquinazolin-4[1H]-one (DHQ) conjugates(6a?j) via ultrasound-assisted, solvent-free ionic liquid [HDBU][HSO4]-catalyzed reaction in good to excellent yields. This non-conventional, ultrasound-assisted route has taken the reactions over the conventional reflux method to provide good to excellent yields of the corresponding products (6a?j) in a very short time. In addition, mild reaction conditions, tolerance to functionalized substrates, ease of product isolation, prevention of its over oxidation and reusability of catalyst [HDBU][HSO4] are some key striking features of the methodology. The newly synthesized derivatives (6a?j) were screened for antioxidant activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) assay and are found to be a potent scavenger. The compounds 6b, 6c, 6d, 6e and 6i showed significant antioxidant activity. Molecular docking studies showed significant binding affinity in the active site of myeloperoxidase (MPO) enzyme and hence scavenged by inhibition of MPO. In silico ADMET and pharmacokinetic studies of the conjugates are very promising; a cumulative body of evidence suggests their medicinal value as a potential orally active drug candidate. Graphical abstract: [Figure not available: see fulltext.]
Design, synthesis and effect of triazole derivatives against some toxic activities of Bothrops jararaca venom
da Silva, Aldo R.,da Silva, Ana Cláudia R.,Donza, Marcio Roberto H.,de Aquino, Gabriel Alves S.,Kaiser, Carlos R.,Sanchez, Eladio F.,Ferreira, Sabrina B.,Fuly, André L.
, p. 182 - 195 (2020/10/26)
According to the World Health Organization, snakebite envenoming is a neglected disease that affects around 5.4 million people worldwide each year. In Brazil, in 2019 there were 29,000 cases of accidents, with 104 deaths. The genus Bothrops was responsibl
[Et3NH][HSO4] catalyzed solvent-free synthesis of new 1,2,3-triazolidene-indolinone derivatives
Nagargoje, Amol A.,Pisal, Parshuram M.,Raza, Akram K.,Shingate, Bapurao B.,Siddiqui, Madiha M.
, (2022/02/03)
A series of new 1,2,3-triazolidene-indolinone derivatives (17a-j) were designed and synthesized via [Et3NH] [HSO4] catalyzed solvent-free approach. The synthesis strongly relied on Knoevenagel condensation of 1,4-disubstituted 1,2,3-
New 1,2,3-triazole-linked tetrahydrobenzo[b]pyran derivatives: Facile synthesis, biological evaluation and molecular docking study
Khare, Smita P.,Deshmukh, Tejshri R.,Akolkar, Satish V.,Sangshetti, Jaiprakash N.,Khedkar, Vijay M.,Shingate, Bapurao B.
, p. 5159 - 5182 (2019/07/04)
Abstract: An efficient ultrasound-promoted one-pot three-component synthesis of a series of new 1,2,3-triazole-linked tetrahydrobenzo[b]pyran derivatives as antifungal and antioxidant agents using NaHCO3 has been described for the first time. T
Ultrasound assisted rapid synthesis, biological evaluation, and molecular docking study of new 1,2,3-triazolyl pyrano[2,3-c]pyrazoles as antifungal and antioxidant agent
Khare, Smita P.,Deshmukh, Tejshri R.,Sangshetti, Jaiprakash N.,Khedkar, Vijay M.,Shingate, Bapurao B.
, p. 2521 - 2537 (2019/07/15)
In search of new generation of triazole based antifungal agents, synthesis of series of new 1,2,3-triazolyl pyrano[2,3-c]pyrazoles under ultrasonic irradiation using NaHCO3 has been reported. The bioevaluation results indicate that, the compoun
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia
Xu, Qiaoling,Dai, Baozhu,Li, Zhiwei,Xu, Le,Yang, Di,Gong, Ping,Hou, Yunlei,Liu, Yajing
supporting information, (2019/08/27)
FMS-like tyrosine kinase 3 (FLT3) was an important therapeutic target in acute myeloid leukemia (AML). We synthesized two series of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives possessing the semicarbazide moiety and 2,2,2-trifluoro-N,N′-dimeth
One-Pot Synthesis of 1-Monosubstituted 1,2,3-Triazoles from Propargyl Alcohol
Han, Chunmei,Dong, Suping,Zhang, Wensheng,Chen, Zhen
supporting information, p. 673 - 677 (2018/03/10)
A one-pot synthesis of 1-monosubstituted-1,2,3-triazoles from propargyl alcohol and various aryl azides was achieved. This simple method provides concise and efficient access to various 1-monosubstituted 1,2,3-triazole derivatives through a three-step one
Triazole-diindolylmethane conjugates as new antitubercular agents: synthesis, bioevaluation, and molecular docking
Danne, Ashruba B.,Choudhari, Amit S.,Chakraborty, Shakti,Sarkar, Dhiman,Khedkar, Vijay M.,Shingate, Bapurao B.
supporting information, p. 1114 - 1130 (2018/08/01)
We describe the synthesis of novel triazole-incorporated diindolylmethanes (DIMs) using a molecular hybridization approach. The in vitro antitubercular activity of the DIMs against Mycobacterium tuberculosis H37Ra (ATCC 25177) was tested in the active and
Design and synthesis of novel dehydroepiandrosterone analogues as potent antiproliferative agents
Huang, Xing,Shen, Qing-Kun,Zhang, Hong-Jian,Li, Jia-Li,Tian, Yu-Shun,Quan, Zhe-Shan
, (2018/09/12)
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hel
