5651-87-6Relevant academic research and scientific papers
Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives
Nagarsenkar, Atulya,Guntuku, Lalita,Guggilapu, Sravanthi Devi,Danthi Bai,Gannoju, Srinivasulu,Naidu,Bathini, Nagendra Babu
, p. 782 - 793 (2016)
In our venture towards the development of effective cytotoxic agents, a panel of triazole linked 3-benzylidene isatin hybrids were synthesized and characterized by IR,1H NMR,13C NMR and Mass spectral analysis. All the newly synthesiz
Novel 1,2,3-triazolo phosphonate derivatives as potential antibacterial agents
Telu, Jhonsee Rani,Kuntala, Naveen,Kankanala, Kavitha,Banothu, Venkanna,Pal, Sarbani,Anireddy, Jaya Shree
, p. 969 - 982 (2021/02/26)
We describe the synthesis, characterization, and in vitro antibacterial evaluation of a library of novel compounds based on 1,2,3-triazolo phosphonate framework along with the evaluation of DNA gyrase inhibitory potential of a promising molecule in silico
Synthesis, antimicrobial evaluation and docking studies of oxazolone-1,2,3-triazole-amide hybrids
Kumar, Lokesh,Lal, Kashmiri,Kumar, Aman,Kumar, Ashwani
, p. 5079 - 5097 (2021/09/22)
In an attempt to develop quality antimicrobial agents, a series of oxazolone-1,2,3-triazole-amide hybrids were obtained from oxazolone tethered with a terminal alkyne and in situ generated 2-azido-N-phenylacetamides. All the synthesized compounds were characterized by using various spectroscopic techniques. The developed hybrids were evaluated for their in vitro antimicrobial activity toward three Gram-positive bacteria S. aureus, B. subtilis and S. gorodonii and three Gram-negative bacteria—E. coli, S. enterica and P. aeruginosa—and two fungi, viz. C. albicans and A. niger. Oxazolone-amide-1,2,3-triazoles (8a–e, 9a–e, 10a–e) exhibited almost 15 times better efficacy than alkyne precursors, i.e., oxazolone-linked terminal alkynes (6a–c). Compound 10d exhibited very good antimicrobial activity toward all the tested microorganisms. Docking studies of compounds 10d and 6c were also carried out in the binding site of enzyme sterol-14-α-demethylase of C. albicans, which supported the in vitro experimental results.
Design and synthesis of benzodiazepine-1,2,3-triazole hybrid derivatives as selective butyrylcholinesterase inhibitors
Mehrazar, Mehrdad,Hassankalhori, Mahdi,Toolabi, Mahsa,Goli, Fereshteh,Moghimi, Setareh,Nadri, Hamid,Bukhari, Syed Nasir Abbas,Firoozpour, Loghman,Foroumadi, Alireza
, p. 997 - 1013 (2019/12/24)
Abstract: A new series of compounds based on benzodiazepine-1,2,3-triazole were synthesized and evaluated as cholinesterase inhibitors by Ellman’s method. The compounds proved to be selective inhibitors of butyrylcholinesterase (BuChE) over acetylcholines
Design, synthesis, biological activity, molecular docking and computational studies on novel 1,4-disubstituted-1,2,3-Triazole-Thiosemicarbazone hybrid molecules
Ghule, Vikas D.,Kumar, Ashwani,Kumar, Lokesh,Kumar, Nikhil,Lal, Kashmiri,Naveen,Tittal, Ram Kumar
, (2020/02/29)
A library of some novel 1,4-disubstituted-1,2,3-triazole-thiosemicarbazone hybrid molecules were designed and synthesized from (4-Prop-2-ynyloxy-benzylidene)-thiosemicarbazone and aryl azides under Cu(I)-catalyzed cycloaddition reaction. All newly synthesized [4-(1-Benzyl-1H-[1,2,3]triazol-4-ylmethoxy)-benzylidene] -thiosemicarbazone hybrid molecules were efficiently characterized by IR, 1H NMR, 13C NMR, HRMS and structure of alkynes 3 & 12 were finally supported by X-ray crystallographic data. Compounds 5c, 5d, 9c, 9d 13c and 13d demonstrated excellent potency results for B. Subtilis and P. Aeruginosa bacterial strains with MIC values 0.0141, 0.0152, 0.0562, 0.0608, 0.0141, 0.0608, 0.0141, 0.0304, 0.0281, 0.0304, 0.0281, 0.0304, respectively as compared to reference drug Ciprofloxacin. Antibacterial activity results were supported by molecular docking and DFT studies.
Development of alkyne-BODIPYs as viscosity sensitive fluorescent probes for enumeration of bacterial cells
Prasannan, Dijo,Vasu, Suchithra Tharamel,Arunkumar, Chellaiah,Parameswaran, Pattiyil
, p. 1013 - 1020 (2020/06/17)
We report a series of alkyne-functionalized meso-aryl boron dipyrrin (BODIPY) molecular rotors sensitive to viscosity. The planar and twisted conformation within the molecular structure decides the viscosity-dependent behavior. The variations in fluorescence lifetime and intensity were appreciable to the local viscosity. Hence, the dye has been successfully employed in the enumeration of microbes by considering the proportionate fluorescence intensity of the BODIPYs as an index of the number of cells per mL. With increasing cells per mL, the viscosity of the bacterial solution is increased. Consequently, the fluorescence intensity of the sample containing BODIPY tends to increase due to the restricted rotation in the viscous medium. The BODIPY probe offers high sensitivity and is easier than other conventional techniques of colony-forming unit (CFU) determination. The theoretical studies indicate that intramolecular charge transfer is responsible for the enhanced fluorescence intensity in a highly viscous solvent.
Glaucocalyxin A (GLA)-biotin small-molecular probe, and preparation method and application thereof
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Paragraph 0044-0045, (2020/06/09)
The invention relates to a GLA small-molecular probe, and a preparation method and application thereof, belonging to the field of medicinal chemistry. The GLA small-molecular probe structurally comprises three parts, namely GLA, a linker and a reporter (b
A molybdenum based metallomicellar catalyst for controlled and chemoselective oxidation of activated alcohols in aqueous medium
Thiruvengetam, Prabaharan,Chakravarthy, Rajan Deepan,Chand, Dillip Kumar
, p. 123 - 133 (2019/07/19)
A surfactant based oxodiperoxo molybdenum complex, which could activate molecular oxygen, has been employed as a catalyst for controlled oxidation of benzylic alcohols to corresponding carbonyls. The oxidation reactions were carried out under aqueous environment, however, in the absence of any extraneous base or co-catalyst. Sensitive/oxidizable functional groups like cyano, sulfide, hydroxyl, aryl-hydroxyl, alkene (internal/terminal), alkyne (internal/terminal), and acetal were tolerated during the transformations. Such selectivity is attributed to the mild nature of the catalyst. The methodology could also be scaled-up for multi-gram synthesis and the protocol is likely to find practical use since it requires an inexpensive recyclable-catalyst and easily available oxidant (under green conditions). A plausible mechanism is proposed with the help of preliminary computational study.
Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies
Zengin Kurt, Belma,Sonmez, Fatih,Ozturk, Dilek,Akdemir, Atilla,Angeli, Andrea,Supuran, Claudiu T.
, (2019/09/30)
Carbonic anhydrases isoforms CA IX, and XII are known to be highly expressed in various human tissues and malignancies. CA IX is a prominent target for especially colorectal cancers, because it is overexpressed in colorectal cancer and this overexpression
4,6-Diphenylpyrimidine Derivatives as Dual Inhibitors of Monoamine Oxidase and Acetylcholinesterase for the Treatment of Alzheimer's Disease
Kumar, Bhupinder,Dwivedi, Ashish Ranjan,Sarkar, Bibekananda,Gupta, Sukesh Kumar,Krishnamurthy, Sairam,Mantha, Anil K.,Parkash, Jyoti,Kumar, Vinod
, p. 252 - 265 (2019/01/24)
Alzheimer's disease (AD) is a neurodegenerative disorder with multifactorial pathogenesis. Monoamine oxidase (MAO) and acetylcholinesterase enzymes (AChE) are potential targets for the treatment of AD. A total of 15 new propargyl containing 4,6-diphenylpy
