186507-11-9Relevant academic research and scientific papers
Stereoselective synthesis of highly functionalised pyrrolidines via 1,3-dipolar cycloaddition reactions on a solid support
Hollinshead, Sean P.
, p. 9157 - 9160 (1996)
Resin bound 3-hydroxyacetophenone 2 was condensed (NaOMe/MeOH/THF) with aryl aldehydes to afford α,β-unsaturated ketones 3a-e. Subsequent reaction with azomethine ylid 5 in the presence of LiBr/DBU provided pyrrolidines 6a-d. These were subsequently acylated and cleaved from the solid support to afford highly functionalised pyrrolidines 8a-d.
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity
Abdel-Halim, Mohammad,Sigler, Sara,Racheed, Nora A. S.,Hefnawy, Amr,Fathalla, Reem K.,Hammam, Mennatallah A.,Maher, Ahmed,Maxuitenko, Yulia,Keeton, Adam B.,Hartmann, Rolf W.,Engel, Matthias,Piazza, Gary A.,Abadi, Ashraf H.
supporting information, p. 4462 - 4477 (2021/05/04)
A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activit
Synthesis, spectroscopic, and photophysicochemical behavior of Zn(II) and Mg(II) phthalocyanine– chalcone conjugates
Aktas Kamiloglu, Ayse,Yalazan, Halise,Durmus, Mahmut,Celik, Gonca,Omero?lu, Ipek,Acar, Irfan,Kantekin, Halit
, p. 2491 - 2507 (2021/10/14)
Phthalonitrile derivatives (8, 9, and 10) bearing different chalcone groups and their zinc(II) (ZnPcs) (8a, 9a, and 10a) and magnesium(II) (MgPcs) (8b, 9b, and 10b) complexes were prepared. The new compounds (5, 8–10, 8a–10a, and 8b–10b) were characterize
Design, synthesis and evaluation of chalcones as H1N1 Neuraminidase inhibitors
Chintakrindi, Anand S.,Gohil, Devanshi J.,Kothari, Sweta T.,Chowdhary, Abhay S.,Kanyalkar, Meena A.
, p. 1013 - 1025 (2018/02/28)
A series of chalcone derivatives (1a–2i) were designed based on isoliquiritigenin (the most active natural chalcone non-competitive neuraminidase (NA) inhibitor). Molecular modeling studies revealed that isoliquiritigenin and its designed analogs occupied
Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors
Wang, Ling,Wang, Yu,Tian, Yiguang,Shang, Jinling,Sun, Xiaoou,Chen, Hongzhuan,Wang, Hao,Tan, Wen
, p. 360 - 371 (2016/12/22)
A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- a
Synthesis and biological evaluation of chalcone, dihydrochalcone, and 1,3-diarylpropane analogs as anti-inflammatory agents
Vijaya Bhaskar Reddy, Mopur,Hung, Hsin-Yi,Kuo, Ping-Chung,Huang, Guan-Jhong,Chan, Yu-Yi,Huang, Shiow-Chyn,Wu, Shwu-Jen,Morris-Natschke, Susan L.,Lee, Kuo-Hsiung,Wu, Tian-Shung
supporting information, p. 1547 - 1550 (2017/03/17)
Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in L
A kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application (by machine translation)
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Paragraph 0168; 0169; 0170, (2016/11/28)
The present invention discloses a kind of carbamate-koncar ketone choline esterase inhibitor and its preparation method and application, belongs to the field of medicinal chemistry. Cholinesterase inhibitors of the invention represented by general formula
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines
Ansari, Farzana Latif,Iftikhar, Fatima,Ihsan-ul-Haq,Mirza, Bushra,Baseer, Mohammad,Rashid, Umer
, p. 7691 - 7697 (2008/12/23)
Solid-phase synthesis of a parallel library of 3′-hydroxy-2,3-dihydrobenzothiazepines has been carried out through [4+3] annulation of α,β-unsaturated ketones with aminothiophenol, using Wang resin as solid support. The synthesized compounds were evaluated for their potential as antibacterial, tumor inhibitors as well as acetyl- and butyrylcholinesterase inhibitors. None of the compounds showed any significant antibacterial activity. However, quite a few compounds showed significant potential as crown gall tumor inhibitors. These results reflect a strong exploratory potential in search of new benzothiazepines as source of anticancer agents. The results of the inhibition of cholinesterase revealed that benzothiazepines have a greater potential as butyrylcholinesterase inhibitors as compared to acetylcholinesterase. Moreover, the substitution of hydroxy group at C-3 in ring A led to increased activity when compared to unsubstituted- and 2′-OH substituted benzothiazepines.
Synthesis, antimycobacterial activity evaluation, and QSAR studies of chalcone derivatives
Sivakumar,Seenivasan, S. Prabu,Kumar, Vanaja,Doble, Mukesh
, p. 1695 - 1700 (2007/10/03)
In order to develop relatively small molecules as antimycobacterial agents, twenty-five chalcones were synthesized, their activity was evaluated, and quantitative structure-activity relationship (QSAR) was developed. The synthesis was based on the Claisen
Synthesis and fungicidal evaluation of novel chalcone-based strobilurin analogues
Zhao, Pei-Liang,Liu, Chang-Ling,Huang, Wei,Wang, Ya-Zhou,Yang, Guang-Fu
, p. 5697 - 5700 (2008/03/14)
Strobilurin derivatives have become one of the most important classes of agricultural fungicide due to a novel action mode, wide fungicidal spectrum, lower toxicity toward mammalian cells, and environmentally benign characteristics. To discover new strobilurin analogues with high activity against resistant pathogens, a series of new chalcone-based strobilurin derivatives are designed and synthesized by integrating a chalcone scaffold with a strobilurin pharmacophore. The preliminary bioassay showed that some of the chalcone analogues exhibited good in vivo fungicidal activities against Pseudoperoniospora cubensis and Sphaerotheca fuliginea at the dosage of 200 μg mL-1. Two compounds, (£)-methyl 2-[2-({3-[(£)-3-(2- chlorophenyl)acryloyl]phenoxy}methyl)phenyl]-3-meth-oxyacrylate (1e) and (E)-methyl 2-[2-({3-[(E)-3-(3-bromophenyl)acryloyl]phenoxy}methyl)phenyl]-3- methoxyacrylate (11), were found to display higher fungicidal activities against P. cubensis (EC90 = 118.52 μg ml-1 for 1e and EC 90 = 113.64 μg mL-1 for 11) than Kresoxim-methyl (EC90 = 154.92 μg mL-1) and were identified as the most promising candidates for further study. The present work demonstrated that strobilurin analogues containing chalcone as a side chain could be used as a lead structure for further developing novel fungicides. To our knowledge, this is the first report about the syntheses and fungicidal activities of chalcone-based strobilurin derivatives.
