1234-17-9Relevant academic research and scientific papers
A chalcone-based fluorescent responsive probe for selective detection of nitroreductase activity in bacteria
Wangngae, Sirilak,Pewklang, Thitima,Chansaenpak, Kantapat,Ganta, Phongsakorn,Worakaensai, Suphanida,Siwawannapong, Kittipan,Kluaiphanngam, Surayut,Nantapong, Nawarat,Lai, Rung-Yi,Kamkaew, Anyanee
supporting information, p. 11566 - 11573 (2021/07/11)
A new chalcone-based fluorescent turn-on probe (3c) responsive to nitroreductase (NTR) activity and its application toward the detection of bacteria are presented. The probe exhibits turn-on fluorescence at 535 nm in response to NTR activity and its optic
Unexpected solvent/substitution-dependent inversion of the enantioselectivity in Michael addition reaction using chiral phase transfer catalysts
Kottala Vijaya, Ponmuthu,Murugesan, Sepperumal,Siva, Ayyanar
supporting information, p. 5209 - 5212 (2015/08/19)
New cinchonium salts bearing 5,5′-bis(methyl)-2,2′-bipyridine 1 group show solvent/substitution-dependent reversal of enantioselectivity. When used as chiral phase transfer catalyst in the asymmetric Michael addition of chalcones with diethylmalonate within two hours these catalysts result in high chemical yield (up to 98%) and enantiomeric excess (up to 99%) under lower concentrations of base and cold conditions.
Biologically active 1,3-bis-aromatic-prop-2-en-1-ones, 1,3-bis-aromatic-propan-1-ones, and 1,3-bis-aromatic-prop-2-yn-1-ones
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, (2008/06/13)
The invention relates to the use of 1,3-bis-aromatic-prop-2-en-1-ones (chalcones), 1,3-bis-aromatic-propan-1-ones (dihydrochalcones), and 1,3-bis-aromatic-prop-2-yn-1-ones for the preparation of pharmaceutical compositions for the treatment or prophylaxis of a number of serious diseases including i) conditions relating to harmful effects of inflammatory cytokines, ii) conditions involving infection by Helicobacter species, iii) conditions involving infection by viruses, iv) neoplastic disorders, and v) conditions caused by microorganisms or parasites. The invention also relates to novel chalcones and dihydrochalcones (especially alkoxy substituted variants) having advantageous substitution patterns with respect to their effect as drug substances, and to methods of preparing them, as well as to pharmaceutical compositions comprising the novel chalcones. Moreover, the present invention relates to a method for the isolation of Leishmania fumarate reductase, QSAR methodologies for selecting potent compounds for the above-mentioned purposes.
Antileishmaniai chalcones: Statistical design, synthesis, and three- dimensional quantitative structure-activity relationship analysis
Nielsen, Simon Feldb?k,Christensen, S?ren Br?gger,Cruciani, Gabriele,Kharazmi, Arsalan,Liljefors, Tommy
, p. 4819 - 4832 (2007/10/03)
A large number of substituted chalcones have been synthesized and tested for antileishmanial and lymphocyte-suppressing activities. A subset of the chalcones was designed by using statistical methods. 3D-QSAR analyses using 67 (antileishmanial activity) and 63 (lymphocyte-suppressing activity) of the compounds for the training sets and 9 compounds as an external validation set were performed by using the GRID/GOLPE methodology. The Smart Region Definition procedure with subsequent region selection as implemented in GOLPE reduced the number of variables to approximately 1300 yielding 3D-QSAR models of high quality (lymphocyte-suppressing model, R2 = 0.90, Q2 = 0.80; antileishmanial model, R2 = 0.73, Q2 = 0.63). The coefficient plots indicate that steric interactions between the chalcones and the target are of major importance for the potencies of the compounds. A comparison of the coefficient plots for the antileishmanial effect and the lymphocyte- suppressing activity discloses significant differences which should make it possible to design chalcones having a high antileishmanial activity without suppressing the proliferation of lymphocytes.
Synthesis and Biological Activity of Some New 10-phenothiazines
Jaiswal, Neelam,Jaiswal, R. K.,Barthwal, J. P.,Kishor, K.
, p. 252 - 253 (2007/10/02)
Fourteen 10-phenothiazines (IV) have been synthesized via condensation of 10-hydrazino-acetylphenothiazine with substituted benzalacetophenones.These compounds inhibit 33-86percent in vitro activity of rat brain pyruvate oxidase and afford protection against pentylenetetrazol induced seizures in albino mice.However, their anticonvulsant properties are found to be independent of their pyruvate oxidase inhibitory activity.
