- Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis andin vitrodisaggregation
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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-
- Maqbool, Mudasir,Gadhavi, Joshna,Singh, Anju,Hivare, Pravin,Gupta, Sharad,Hoda, Nasimul
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supporting information
p. 1589 - 1603
(2021/03/01)
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- 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
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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
- Jalapathi, P.,Nagamani, M.,Srinivas, M.,Vishnu, T.
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- Synthesis of Spirobicyclic Pyrazoles by Intramolecular Dipolar Cycloadditions/[1s, 5s] Sigmatropic Rearrangements
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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.
- 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.
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supporting information
p. 7209 - 7212
(2019/10/02)
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- A strategic approach to the synthesis of ferrocene appended chalcone linked triazole allied organosilatranes: Antibacterial, antifungal, antiparasitic and antioxidant studies
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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
- Singh, Gurjaspreet,Arora, Aanchal,Kalra, Pooja,Maurya, Indresh Kumar,Ruizc, Cristobal Espinosa,Estebanc, M. Angeles,Sinha, Shweta,Goyal, Kapil,Sehgal, Rakesh
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p. 188 - 195
(2018/12/11)
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- Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase
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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
- Kumar, Bhupinder,Kumar, Vijay,Prashar, Vikash,Saini, Suresh,Dwivedi, Ashish Ranjan,Bajaj, Beenu,Mehta, Devashish,Parkash, Jyoti,Kumar, Vinod
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p. 221 - 234
(2019/06/05)
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- Synthesis, Biological Evaluation and Molecular Modeling Studies of Propargyl-Containing 2,4,6-Trisubstituted Pyrimidine Derivatives as Potential Anti-Parkinson Agents
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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
- Kumar, Bhupinder,Kumar, Mohit,Dwivedi, Ashish Ranjan,Kumar, Vinod
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p. 705 - 712
(2018/03/21)
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- Design and synthesis of new 1,2,3-triazole-pyrazole hybrids as antimicrobial agents
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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
- Pervaram,Ashok,Rao,Sarasija,Reddy
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p. 2454 - 2461
(2017/11/24)
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- 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
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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.
- Ma, Xiao-Pan,Li, Kun,Wu, Si-Yi,Liang, Cui,Su, Gui-Fa,Mo, Dong-Liang
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supporting information
p. 5761 - 5766
(2017/12/26)
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- 1,2,3-Triazole tethered acetophenones: Synthesis, bioevaluation and molecular docking study
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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.
- Shaikh, Mubarak H.,Subhedar, Dnyaneshwar D.,Khedkar, Vijay M.,Jha, Prakash C.,Khan, Firoz A. Kalam,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.
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p. 1058 - 1063
(2016/07/29)
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- Photochemistry of aroyloxiranes: Substituent effect on oxepinones and hydroxyalkenones formation
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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).
- Dalal, Aarti,Khanna, Radhika,Berar, Urmila,Kamboj, Ramesh C.
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p. 238 - 245
(2016/07/22)
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- Design, synthesis and biological evaluation of chalconyl blended triazole allied organosilatranes as giardicidal and trichomonacidal agents
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A series of chalconyl blended triazole allied silatranes (7a-g/8a-g/9a-g) were synthesized in good yields using a simple, economical and biocompatible synthetic route. The blend of three different pharmacologically active moieties into a single scaffold r
- Singh, Gurjaspreet,Arora, Aanchal,Mangat, Satinderpal Singh,Rani, Sunita,Kaur, Hargobinder,Goyal, Kapil,Sehgal, Rakesh,Maurya, Indresh Kumar,Tewari, Rupinder,Choquesillo-Lazarte, Duane,Sahoo, Subash,Kaur, Navneet
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p. 287 - 300
(2015/12/23)
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- Heteroaryl chalcone allied triazole conjugated organosilatranes: Synthesis, spectral analysis, antimicrobial screening, photophysical and theoretical investigations
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A series of heteroaryl tethered triazole conjoined organosilatranes were synthesized following an archetypal click reaction. The reaction sequence follows the initial generation of acetylinic Schiff bases (3a-3c, 4a-4c) which undergo 3 + 2 cycloaddition w
- Singh, Gurjaspreet,Arora, Aanchal,Rani, Sunita,Maurya, Indresh Kumar,Aulakh, Darpandeep,Wriedt, Mario
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p. 82057 - 82081
(2016/09/09)
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- Synthetic investigations and photo-physical properties of 1,2,3-triazole encapped chalconyl substituted organotriethoxysilanes
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Organotriethoxysilanes (OTES) play an impressive role in the designing of organic-inorganic hybrid materials. The highly efficient copper catalysed 'Click Silylation' is followed for the functionalization of 3-azidopropyltriethoxysilane (AzPTES) with a se
- Singh, Gurjaspreet,Arora, Aanchal,Mangat, Satinderpal Singh,Singh, Jandeep,Rani, Sunita,Kaur, Navneet
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- Synthesis of polyfunctional triethoxysilanes by 'click silylation'
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The copper-catalyzed 'click silylation' has been exploited for the chemical modification of γ-azidopropyltriethoxysilane (AzPTES) with a wide range of terminal alkynes (1a-1v) in a one-pot operation. The novel 1,2,3-triazole-triethoxysilane derivatives (2a-2v) were synthesized by this procedure and comprehensively characterized by IR spectra, 1H and 13C NMR, and HRMS studies.
- Singh, Gurjaspreet,Mangat, Satinderpal Singh,Singh, Jandeep,Arora, Aanchal,Sharma, Ramesh K.
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supporting information
p. 903 - 909
(2015/03/03)
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- Chalcomer assembly of optical chemosensors for selective Cu2+ and Ni2+ ion recognition
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The o-, m- and p-isomeric units of chalconyl triazole-based, caged organosilicon complexes were efficiently synthesized and explored for their cationic chemosensing activities. The UV-vis spectral studies performed show considerable variations in absorpti
- Singh, Gurjaspreet,Singh, Jandeep,Mangat, Satinderpal Singh,Singh, Jasbhinder,Rani, Sunita
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p. 12644 - 12654
(2015/02/19)
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- A domino synthetic approach for new, angular pyrazol- and isoxazol-heterocycles using [DBU][Ac] as an effective reaction medium
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O-Cinnamyloxy/geranyloxy/cyclohexenyloxy/cinnamoyloxy-acetophenones yielded pyrazol-heterocycles, all of which contained an angular methyl-attached pyranopyran unit with pyrazolones in the ionic liquid (IL), 1,8-diazabicyclo[5.4.0]undec-7-ene-8-ium acetat
- Sutariya, Tushar R.,Labana, Balvantsingh M.,Parmar, Bhagyashri D.,Parmar, Narsidas J.,Kant, Rajni,Gupta, Vivek K.
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p. 23519 - 23529
(2015/04/14)
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- Unprecedented synthesis of aza-bridged benzodioxepine derivatives through a tandem Rh(ii)-catalyzed 1,3-rearrangement/[3+2] cycloaddition of carbonyltriazoles
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Rh(ii)-catalyzed novel tandem intramolecular cycloisomerizations of aldehydes or ketones with 1-sulfonyl 1,2,3-triazoles have been disclosed, providing a facile protocol to access a series of functionalized aza-bridged benzodioxepine heterocycles.
- Zhang, Yong-Sheng,Tang, Xiang-Ying,Shi, Min
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supporting information
p. 15971 - 15974
(2015/01/08)
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- Synthesis of polyfunctional triethoxysilanes by 'click silylation'
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The copper-catalyzed 'click silylation' has been exploited for the chemical modification of γ-azidopropyltriethoxysilane (AzPTES) with a wide range of terminal alkynes (1a-1v) in a one-pot operation. The novel 1,2,3-triazole-triethoxysilane derivatives (2a-2v) were synthesized by this procedure and comprehensively characterized by IR spectra, 1H and 13C NMR, and HRMS studies.
- Singh, Gurjaspreet,Mangat, Satinderpal Singh,Singh, Jandeep,Arora, Aanchal,Sharma, Ramesh K.
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supporting information
p. 903 - 909
(2014/02/14)
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- Design, synthesis and molecular docking studies of novel N-benzenesulfonyl-1,2,3,4-tetrahydroisoquinoline-based triazoles with potential anticancer activity
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A novel series of N-benzenesulfonyl-1,2,3,4-tetrahydroisoquinolines (14-33) containing triazole moiety were designed and synthesized through rational cycloadditions using the modified Pictet-Spengler reaction and the Click chemistry. Antiproliferative act
- Pingaew, Ratchanok,Mandi, Prasit,Nantasenamat, Chanin,Prachayasittikul, Supaluk,Ruchirawat, Somsak,Prachayasittikul, Virapong
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p. 192 - 203
(2014/06/09)
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- Synthetic approach towards 'click' modified chalcone based organotriethoxysilanes; UV-Vis study
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The efficient linkage of a conjugate chalcone to n-propyltriethoxysilanes (nPTES) via a 1,2,3-triazole with good yields is reported. The synthesis involves a Claisen-Schmidt condensation reaction followed by a copper(i) catalyzed azide-alkyne cycloadditio
- Singh, Gurjaspreet,Singh, Jandeep,Mangat, Satinderpal Singh,Arora, Aanchal
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p. 60853 - 60865
(2015/02/19)
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- Regioselective synthesis of spiropyrrolidine/spiropyrrolizidine/ spirothiazolidine-grafted macrocycles through 1,3-dipolar cycloaddition methodology
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Synthesis of 13- and 16-membered macrocyclic enone with alkyl ether and triazole as a linker was achieved using intramolecular aldol condensation. The newly synthesized macrocyclic enone was successfully utilized as a dipolarophile in 1,3-dipolar cycloadd
- Purushothaman,Prasanna,Raghunathan
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p. 9742 - 9750
(2013/10/22)
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- Microwave-assisted copper azide alkyne cycloaddition (CuAAC) reaction using D-glucose as a better alternative reductant
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D-Glucose has been established as a reducing agent for the copper azide alkyne cycloaddition (CuAAC) reactions. Efficacy of this new reductant has been established against various phenyl acetylenes (14 examples) and aryl azides (16 examples). All reaction
- Kumar, Yogesh,Bahadur, Vijay,Singh, Anil K.,Parmar, Virinder S.,Singh, Brajendra K.
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p. 1893 - 1903
(2014/01/17)
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- Access to some angular aminochromeno[2,3-c]pyrazole Precursors by a domino knoevenagel-hetero-diels-alder reaction
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A new, solvent-free tetrabutylammonium-hydrogensulfate-catalysed one-pot procedure to synthesise angular benzopyran-annulated pyrazoles, all of which incorporate a tertiary ring-junction carbon, has been demonstrated. A typical intermediate Knoevenagel he
- Parmar, Narsidas J.,Pansuriya, Bhavesh R.,Labana, Balvantsingh M.,Sutariya, Tushar R.,Kant, Rajni,Gupta, Vivek K.
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supporting information
p. 5953 - 5964,12
(2020/09/02)
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- Synthesis, antimalarial and antitubercular activity of acetylenic chalcones
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A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy
- Hans, Renate H.,Guantai, Eric M.,Lategan, Carmen,Smith, Peter J.,Wan, Baojie,Franzblau, Scott G.,Gut, Jiri,Rosenthal, Philip J.,Chibale, Kelly
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supporting information; experimental part
p. 942 - 944
(2010/06/22)
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- High-throughput discovery of mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry
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A ~500-member library of bidentate inhibitors against protein tyrosine phosphatases (PTPs) was rapidly assembled using click chemistry. Subsequent high-throughput screening had led to the discovery of highly potent (K i as low as 150 nM) and se
- Tan, Lay Pheng,Wu, Hao,Yang, Peng-Yu,Kalesh, Karunakaran A.,Zhang, Xiaohua,Hu, Mingyu,Srinivasan, Rajavel,Yao, Shao Q.
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supporting information; experimental part
p. 5102 - 5105
(2010/03/24)
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- Synthesis of tricyclic aromatic compounds by the intramolecular Pauson-Khand reaction promoted by molecular sieves
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Pauson-Khand reactions are carried out with different substituted aromatic enynes, yielding tricyclic cyclopentenones related to natural products such as chromenes. Enynes are easily obtained in a two-step approximation from the corresponding salicylaldehydes. The reaction is promoted by dissolved TMANO (trimethylamine N-oxide) and/or 4 A molecular sieves. This new way of induction for the Pauson-Khand reaction increases yields remarkably, allowing the reaction of some substituted alkenes which fail to react in the absence of the zeolite. Isomerization of the double bond of the cyclopentenone ring is observed except when nonterminal triple bonds are used. For trisubstituted alkenes, an interrupted Pauson-Khand process is observed with moderate yields.
- Perez-Serrano, Leticia,Blanco-Urgoiti, Jaime,Casarrubios, Luis,Dominguez, Gema,Perez-Castells, Javier
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p. 3513 - 3519
(2007/10/03)
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