339067-38-8Relevant articles and documents
Synthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agents
Luan, Tian,Jin, Chunmei,Jin, Chun-Mei,Quan, Zhe-Shan,Gong, Guo-Hua
, p. 761 - 772 (2019)
Ursolic acid (UA), a plant-derived compound, has many properties beneficial to health. In the present study, we synthesised three series of novel UA derivatives and evaluated their anti-Toxoplasma gondii activity both in vitro and in vivo. Most derivative
[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
Selective CDK4/6 inhibition of novel 1,2,3-triazole tethered acridinedione derivatives induces G1/S cell cycle transition arrest via Rb phosphorylation blockade in breast cancer models
Praveenkumar,Gurrapu, Nirmala,Kolluri, Prashanth Kumar,Shivaraj,Subhashini,Dokala, Appaji
, (2021/10/12)
CDK4 & CDK6 are essential regulators of initial cell cycle phases and are always considered an exciting choice for anti-cancer therapy. In the present study, we presented the structure-based rational design & synthesis of a new class of 1,2,3-triazole tet
[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-
Mesoionic Carbene Cobalt Complexes as Multipurpose Catalyst Precursors for Hydrosilylation and Dihydropyrimidinone Synthesis
Albrecht, Martin,Bertini, Simone
, (2021/11/09)
Metalation of CH2OH-substituted triazolium salts with CoCl2 under basic conditions affords C,O-bidentate chelating carbene Co(III) complexes (3a, 3b), while analogous phenyl-substituted triazolium salts produce monodentate carbene Co(II) complexes (3c, 3d). The distinct substituent-induced properties of the metal centers were demonstrated by electrochemical measurements and catalytic activities in two specific processes. The complexes showed appreciable activity in the reduction of C=O bonds through hydrosilylation, with methoxybenzene-functionalized triazolylidene Co(III) complex 3a achieving a high selectivity towards aldehydes vs. ketones with turnover frequencies (TOFs) up to 200 h?1. The C,O-chelate systems were also active catalysts in the Biginelli process, a one-step three-component reaction for efficient dihydropyrimidinone synthesis. Optimization of reaction conditions provides high activity with complex 3a, reaching TOFs of 800 h?1, the highest activity known for cobalt NHC complexes to date.
Synthesis and bioevaluation of α,α’-bis(1H-1,2,3-triazol-5-ylmethylene) ketones
Deshmukh, Tejshri R.,Krishna, Vagolu S.,Sriram, Dharmarajan,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.
, p. 809 - 820 (2019/09/06)
Abstract: Curcumin is an active component of turmeric that has poor solubility, stability and bioavailability. The monocarbonyl curcumin analogues were modified from curcumin to achieve more stable and active compounds as compared to curcumin. Therefore,
Synthesis, characterization and photodynamic activity against bladder cancer cells of novel triazole-porphyrin derivatives
Gomes, Ana T.P.C.,Fernandes, Rosa,Ribeiro, Carlos F.,Tomé, Jo?o P.C.,Neves, Maria G.P.M.S.,da Silva, Fernando de C.,Ferreira, Vítor F.,Cavaleiro, José A.S.
, (2020/04/10)
Novel triazole-porphyrin derivatives (TZ-PORs) were synthesized through the Heck reaction and then incorporated into polyvinylpyrrolidone (PVP) micelles. After verifying that this incorporation did not compromise the photophysical and chemical features of
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