- Synthesis and Activity of 1,2,3-Triazole Aminopyrimidines against Cyanobacteria as PDHc-E1 Competitive Inhibitors
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Cyanobacteria harmful algal blooms are of global concern, but all currently available algicides in the market are nonselective and have potential side effects on nontarget species. In the present work, two series of compounds (4 and 6) comprising 16 novel
- Zhou, Yuan,Feng, Jiangtao,Feng, Lingling,Xie, Dan,Peng, Hao,Cai, Meng,He, Hongwu
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p. 12538 - 12546
(2019/11/13)
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- Stereospecific Ring Opening and Cycloisomerization of Aziridines with Propargylamines: Synthesis of Functionalized Piperazines and Tetrahydropyrazines
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Stereospecific Cu-catalyzed nucleophilic ring opening of N-sulfonylaziridines with propargylamines and subsequent hydroamination afford piperazines, which leads to double-bond isomerization to furnish tetrahydropyrazines. Optically active aziridines can be cross-coupled with high enantiomeric purities (>98% ee).
- Das, Bijay Ketan,Pradhan, Sourav,Punniyamurthy, Tharmalingam
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supporting information
p. 4444 - 4448
(2018/08/07)
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- Design, synthesis and antibacterial evaluation of novel 1,2,3-triazole derivatives incorporating 3′-deoxythymidine
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A series of novel 1,2,3-triazole derivatives incorporating 3′-deoxythymidine were designed, synthesised and characterised. Antibacterial activity against Escherichia coli and Staphylococcus aureus was evaluated for all of the synthesised compounds and com
- Mao, Long-Fei,Xu, Gui-Qing,Sun, Bin,Jiang, Yu-Qin,Dong, Wen-Pei,Zhang, Shu-Ting,Shen, Jia-Xuan,He, Xing
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p. 645 - 649
(2017/12/26)
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- Anti-methicillin resistant Staphylococcus aureus activity, synergism with oxacillin and molecular docking studies of metronidazole-triazole hybrids
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MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistance against the currently available drugs. Interestingly, a series of 35 metronidazole-triazole hybrids on screening against MRSA were found to be active. Compound 22 was found to be effective at 4 μg/mL concentration against nine strains of MRSA. The inhibitory activity was further enhanced upto 1 μg/mL when this compound was used in combination with oxacillin in 1:1 ratio. All the compounds were found to be non-toxic in THP-1 cell line upto a concentration of 50 μM. The time-kill kinetics studies suggested bacteriostatic nature of the compounds. In silico studies show that these compounds interact with Thr600, Ser598, Asn464, His583 and Tyr446 in the active site of PBP2a crystal structure from MRSA.
- Negi, Beena,Kumar, Deepak,Kumbukgolla, Widuranga,Jayaweera, Sampath,Ponnan, Prija,Singh, Ramandeep,Agarwal, Sakshi,Rawat, Diwan S.
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p. e426 - e437
(2016/04/19)
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- AgNO2 as the NO Source for the Synthesis of Substituted Pyrazole N-Oxides from N-Propargylamines
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A straightforward method for synthesizing the pyrazole N-oxides from N-propargylamines and AgNO2 through oxidation/cyclization reaction had been developed. AgNO2 was used as the NO source for the first time to synthesize pyrazole N-o
- Yuan, Bingxiang,Zhang, Fuming,Li, Zhuomei,Yang, Shenghua,Yan, Rulong
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supporting information
p. 5928 - 5931
(2016/11/29)
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- A microwave-assisted three-component synthesis of arylaminomethyl ?acetylenes: A facile access to terminal alkynes
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A simple, rapid, one-pot synthesis of arylaminomethyl acetylenes is achieved under microwave-assisted conditions (power? =? 5 W) using aromatic boronic acids, aqueous ammonia, propargyl halides, copper(I) oxide and water as the solvent. The reactions are complete within ten minutes affording good to excellent yields of the products. Georg Thieme Verlag Stuttgart. New York.
- Jiang, Yubo,Huang, Shaojun
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supporting information
p. 407 - 410
(2014/03/21)
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- One-pot synthesis of N-aryl propargylamine from aromatic boronic acid, aqueous ammonia, and propargyl bromide under microwave-assisted conditions
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A facile, one-pot synthesis of N-aryl propargylamine from aromatic boronic acid, aqueous ammonia, and propargyl bromide has been achieved under microwave-assisted conditions. The reactions can be smoothly completed within a total 10 min through a two-step procedure, including copper-catalyzed coupling of aromatic boronic acids with aqueous ammonia and following propargylation by propargyl bromide.
- Jiang, Yu-Bo,Zhang, Wen-Sheng,Cheng, Hui-Ling,Liu, Yu-Qi,Yang, Rui
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p. 779 - 782
(2014/06/09)
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- 2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes
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Based on our previous results on the ascertained potent growth inhibition effect against a panel of 60 human tumors cell lines at National Cancer Institute of Bethesda (NCI), we have synthesized a novel series of thirty-one 2-[N-methyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines (1-31). The lead compound 1 was previously reported to be endowed with significant inhibition against hDHFR enzyme, with a Ki of 0.2 μM. Docking studies were performed on compound 1 and here reported to predict its binding conformation to human dihydrofolate reductase (hDHFR). All compounds (1-31) were assayed versus hDHFR and human thymidylate synthase (hTS). From the screening emerged that all compounds inhibited hDHFR with Ki values included between 0.2 and 11 μM, while only a few (6, 21, 24, 27, 29) showed great activity and selectivity towards hTS. Evaluation of the anticancer activity was performed by NCI, first against the three cell line panel, and only the most active compounds (17, 21, 24, 26, 27) were evaluated on a panel of 60 human tumor cell lines. Compound 21 was the most active against all cell lines with log GI50 equal to -5.49 and log LC50 equal to -4.19 and maintained significant percent of growth inhibition on seven cancer cell lines at the concentration of 1 μM. Compound 17 was the second most active and moreover showed interesting selectivity against some cell lines (Lung cancer: A549/ATCC, Melanoma: UACC-257, Ovarian Cancer: ovcar-8 and Renal cancer: RXF 393) at all concentration examined (100-0.01 μM).
- Piras, Sandra,Carta, Antonio,Briguglio, Irene,Corona, Paola,Paglietti, Giuseppe,Luciani, Rosaria,Costi, Maria Paola,Ferrari, Stefania
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p. 169 - 183
(2014/03/21)
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- Direct and selective N-monoalkynylation and N-monoalkenylation of anilines with alky(e)nyl methanesulfonates using methylmagnesium bromide as a base
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Several anilines were directly N-monoalkynylated and N-monoalkenylated with alkynyl methanesulfonates and alkenyl methanesulfonates, respectively, using methylmagnesium bromide as a base in good yields with high selectivities.
- Yoshida, Yoshihiro,Tanabe, Yoo
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p. 533 - 535
(2007/10/03)
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- Intramolecular aromatic substitution and amino-claisen rearrangement in substituted N-(2-propynyl)anilines on electron impact
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N-(2-Propynyl)anilines undergo amino-Claisen rearrangement to a minor extent in the ion source, losing a molecule of HCN under electron impact conditions. However, metastable molecular ions with energies closer to threshold undergo Claisen rearrangement g
- Ramana,Sudha
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p. 1028 - 1033
(2007/10/03)
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