14737-89-4Relevant articles and documents
Cinnamoyl-memantine hybrids: Synthesis, X-ray crystallography and biological activities
Chochkova, Maya,Jiang, Hailun,Kyoseva, Radoslava,Stoykova, Boyka,Tsvetanova, Elina,Alexandrova, Albena,Liu, Rui,Li, Zhuorong,Mitrev, Yavor,Dimitrova-Sbirkova, Hristina,?tícha, Martin,Shivachev, Boris
, (2021)
Herein, framework combinations of antioxidant substituted cinnamic acids and memantine (N-methyl-D-aspartate receptor antagonist) in a new multi-targeted chemical entity were described. The amide bond formation of the memantine hybrids 1–5 was performed by EDC/HOBt coupling reaction. The chemical structures of the synthesized compounds were confirmed by means of melting points, UV, IR, 1H NMR, 13C NMR, and HRMS. Additionally, the crystal structures of memantine hybrids (2–5) were also studied by single-crystal X-ray diffraction. The single-crystal X-ray analysis revealed that the compounds 2, 5 crystallize in a centrosymmetric manner both in monoclinic space group (SG) P21/c, (No 14) and in a non-centrosymmetric manner for compounds 3 and 4, SG R3, (No 146) and SG P212121, (No 19), respectively. Furthermore, preliminary in vitro screenings of their neuroprotective and radical scavenging activities were performed. The radical scavenging activity of synthesized memantine hybrids was measured against 1,1-diphenyl-2-picrylhydrazyl (DPPH●), hydroxyl (OH●) and superoxide (O2●?) radicals and compared with the standard antioxidants (ferulic and sinapic acids). Radical scavenging activity studies show that amongst the tested hybrids, N-sinapoyl amide of memantine (3) emerges as the most potent antioxidant in all tests. Moreover, in vitro evaluation of anti-Alzheimer effects showed that the obtained memantine hybrids displayed neuroprotection in the moderate levels. Generally, they possess a little weaker activity as compared to the positive control memantine. Taken together, our findings reveal that the N-sinapoylamide of memantine (3) can be considered as a promising neuroprotective agent for Alzheimer's disease, acting as well as a potent radical scavenger.
ARBORTRISTOSIDE A AND B, TWO IRIDOID GLUCOSIDES FROM NYCTANTHES ARBOR-TRISTIS
Purushothaman, Kozhiparambil K.,Venkatanarasimhan, Mathuram,Sarada, Ayyappath
, p. 773 - 776 (1985)
Two new iridioid glucosides, arbortristoside A and B have been isolated from the seeds of Nychtanthes arbortristis.The structures of the two new compounds were determined by spectroscopic methods and chemical reactions. - Key Word Index - Nyctanthes arbor-tristis; Oleaceae; iridoid glucosides; arbortristosides A and B.
Effect of solvent and hydrogen during selective hydrogenation
Maki, Shojiro,Harada, Yasuhiro,Matsui, Ryo,Okawa, Makiko,Hirano, Takashi,Niwa, Haruki,Koizumi, Megumi,Nishiki, Yoshinori,Furuta, Tsuneto,Inoue, Hiroshi,Iwakura, Chiaki
, p. 8323 - 8327 (2001)
Described is the solvent effect for the chemoselective hydrogenation of alkenes having a benzyloxy group (Bn-O-) using a hydrogenation system employing atomic hydrogen permeating through a Pd sheet electrode.
Oleanolic acid caffeate from the outer bark of Betula davurica
Odinokova, L. E.,Denisenko, V. A.,Pokhilo, N. D.,Uvarova, N. I.
, p. 255 - 256 (1985)
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Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum
Baruch, Yifat,Gopas, Jacob,Kadosh, Yael,Kumar, Rajendran Saravana,Kushmaro, Ariel,Muthuraman, Subramani,Yaniv, Karin
supporting information, (2021/05/28)
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections.
NOVEL SMALL MOLECULES THAT BIND AND/OR MODULATE DIFFERENTFORMS OF TAU OLIGOMERS
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Page/Page column 34; 35, (2020/11/03)
The present invention relates to novel small molecules of Formulas I, II, III, Ilia, Illb, and IV and pharmaceutically acceptable salts thereof, as well as the preparation and the use thereof.