41580-73-8Relevant academic research and scientific papers
Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis andin vitrodisaggregation
Maqbool, Mudasir,Gadhavi, Joshna,Singh, Anju,Hivare, Pravin,Gupta, Sharad,Hoda, Nasimul
supporting information, p. 1589 - 1603 (2021/03/01)
A series of triazole-based compounds was synthesized using a click chemistry approach and evaluated for the inhibition of α-synuclein (α-syn) fibrillogenesis and its disaggregation. CompoundsTr3,Tr7,Tr12,Tr15, andTr16exhibited good effect in inhibiting α-
Molecular docking studies on COVID-19 and antibacterial evaluation of newly synthesized 4-(methoxymethyl)-1,2,3-triazolean analogues derived from (E)-1-phenyl-3-(2-(piperidin-1-yl)quinolin-3-yl) prop-2-en-1-one
Jalapathi, P.,Nagamani, M.,Srinivas, M.,Vishnu, T.
, (2021/08/18)
A series of novel quinolone-based 4-(methoxymethyl)-1,2,3-triazole derivatives were synthesized, and their structures were characterized by 1H, 13C NMR and mass spectroscopy. The compounds (IXa-l) were screened in vitro antibacterial
Synthesis of Spirobicyclic Pyrazoles by Intramolecular Dipolar Cycloadditions/[1s, 5s] Sigmatropic Rearrangements
Dimirjian, Christine A.,Casti?eira Reis, Marta,Balmond, Edward I.,Turman, Nolan C.,Rodriguez, Elys P.,Di Maso, Michael J.,Fettinger, James C.,Tantillo, Dean J.,Shaw, Jared T.
supporting information, p. 7209 - 7212 (2019/10/02)
The formation of fused pyrazoles via intramolecular 1,3-dipolar cycloadditions of diazo intermediates with pendant alkynes is described. A subsequent thermal [1s, 5s] sigmatropic shift of these pyrazole systems resulted in a ring contraction, forming spirocyclic pyrazoles. The limitations of this rearrangement were explored by changing the substituents on the nonmigrating aromatic ring and by using substrates lacking an aromatic linkage to the propargyl group.
A strategic approach to the synthesis of ferrocene appended chalcone linked triazole allied organosilatranes: Antibacterial, antifungal, antiparasitic and antioxidant studies
Singh, Gurjaspreet,Arora, Aanchal,Kalra, Pooja,Maurya, Indresh Kumar,Ruizc, Cristobal Espinosa,Estebanc, M. Angeles,Sinha, Shweta,Goyal, Kapil,Sehgal, Rakesh
, p. 188 - 195 (2018/12/11)
A series of ferrocene appended chalcone allied triazole coupled organosilatranes (FCTSa 7–FCTSa 12) were synthesised with the aim of amalgamating the pharmacological action of the constituting moieties into a single molecular scaffold. All the synthesised
Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase
Kumar, Bhupinder,Kumar, Vijay,Prashar, Vikash,Saini, Suresh,Dwivedi, Ashish Ranjan,Bajaj, Beenu,Mehta, Devashish,Parkash, Jyoti,Kumar, Vinod
, p. 221 - 234 (2019/06/05)
Alzheimer's disease (AD) is a multifactorial neurological disorder involving complex pathogenesis. Single target directed drugs proved ineffective and since last few years' different pharmacological strategies including multi-targeting agents are being ex
Synthesis, Biological Evaluation and Molecular Modeling Studies of Propargyl-Containing 2,4,6-Trisubstituted Pyrimidine Derivatives as Potential Anti-Parkinson Agents
Kumar, Bhupinder,Kumar, Mohit,Dwivedi, Ashish Ranjan,Kumar, Vinod
, p. 705 - 712 (2018/03/21)
Monoamine oxidase B (MAO-B) inhibitors are potential drug candidates for the treatment of various neurological disorders including Parkinson's disease. A total of 20 new propargyl-containing 2,4,6-trisubstituted pyrimidine derivatives were synthesized and
Design and synthesis of new 1,2,3-triazole-pyrazole hybrids as antimicrobial agents
Pervaram,Ashok,Rao,Sarasija,Reddy
, p. 2454 - 2461 (2017/11/24)
In the present study, a series of novel 1,2,3-triazoles derivatives (4a–4c) were synthesized by the 1,3-dipolar cycloaddition (click-reaction) of 1-phenyl-3-[2-(prop-2-yn-1-yloxy)phenyl substituted]-1H-pyrazole-4-carbaldehyade (3a–3c) with various aryl az
Construction of 2,3-quaternary fused indolines from alkynyl tethered oximes and diaryliodonium salts through a cascade strategy of N-arylation/cycloaddition/[3,3]-rearrangement
Ma, Xiao-Pan,Li, Kun,Wu, Si-Yi,Liang, Cui,Su, Gui-Fa,Mo, Dong-Liang
supporting information, p. 5761 - 5766 (2017/12/26)
A variety of 2,3-quaternary fused indolines could be prepared in good yields with high diastereoselectivity from alkynyl tethered oximes and diaryliodonium salts under mild metal-free conditions. The reaction initially goes through a selective N-arylation to provide alkynyl tethered nitrones and regioselectively undergoes an intramolecular (3 + 2) cycloaddition followed by a [3,3]-sigmatropic rearrangement to afford 2,3-quaternary fused indolines in a one-pot fashion. The method features easily available cheap materials, multiple bond formation, gram scalable preparation and diversity of fused indoline scaffolds.
1,2,3-Triazole tethered acetophenones: Synthesis, bioevaluation and molecular docking study
Shaikh, Mubarak H.,Subhedar, Dnyaneshwar D.,Khedkar, Vijay M.,Jha, Prakash C.,Khan, Firoz A. Kalam,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.
, p. 1058 - 1063 (2016/07/29)
A small focused library of eighteen new 1,2,3-triazole tethered acetophenones has been efficiently prepared via click chemistry approach and evaluated for their antifungal and antioxidant activity. The antifungal activity was evaluated against five human pathogenic fungal strains: Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger, and Cryptococcus neoformans. Among the synthesized compounds, 9c, 9i, and 9p found to be more potent antifungal agents that the reference standard. These 1,2,3-triazole based derivatives were also evaluated for antioxidant activity, and compound 9h was found to be the most potent antioxidant as compared to the standard drug. Furthermore, molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C. albicans enzyme P450 cytochrome lanosterol 14α-demethylase. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential as good oral drug candidates.
Photochemistry of aroyloxiranes: Substituent effect on oxepinones and hydroxyalkenones formation
Dalal, Aarti,Khanna, Radhika,Berar, Urmila,Kamboj, Ramesh C.
, p. 238 - 245 (2016/07/22)
The photo-irradiation of some aroyloxiranes with Pyrex filtered UV-light from 125?W medium pressure Hg lamp has been described. These compounds furnished the 2-aryl-4,10-dihydrofuro[3,2-c][1]benzoxepin-10-ones and the hydroxyalkenones by the photochemical irradiation. The product(s) formation/distribution in terms of oxepinones and the hydroxyalkenones largely depended upon the nature of the substituent: the oxiranes having electron-donating groups in their benzoyl moiety gave the hydroxyalkenones while oxiranes having electron-withdrawing groups furnished the oxepinones as the major products. The formation of oxepinones has been envisaged to occur through the heterolytic [Formula presented] bond cleavage of epoxide to give carbonyl ylide intermediates followed by the furo-oxepinone ring formation via [3+2] cycloaddition and of hydroxyalkenones through the initial β-H abstraction followed by epoxide ring opening. The structures of all the compounds (substrates and photoproducts) have been determined on the basis of their spectral data (IR, NMR and Mass).
