http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Synthesis and Antibacterial Activity of Novel 5-(heteroaryl)isoxazole Derivatives
RamaRao, R. Janaki,Rao, A.K.S. Bhujanga,Sreenivas, N.,Kumar, B. Suneel,Murthy, Y. L. N. Korean Chemical Society 2011 대한화학회지 Vol.55 No.2
Isoxazole계 화합물을 합성하고 항균활성연구를 수행하였다. 3-Di(alkylamino)acryloalkanones을 hydroxylamine hydrochloride 또는 hydroxylamine-O-sulphonic acid와 반응시켜서 target isoxazole계 화합물을 합성하였다. The synthesis, characterization and antibacterial activity of novel isoxazole derivatives were reported. 3-Di (alkylamino)acryloalkanones were prepared and used as synthons to get the target isoxazole derivatives via reaction with hydroxylamine hydrochloride or hydroxylamine-O-sulphonic acid.
Malathy, P.,Sharmila, P.,Srinivasan, J.,Manickam, Bakthadoss,Aravindhan, S. The Basic Science Institute Chosun University 2016 조선자연과학논문집 Vol.9 No.2
The crystal structure of the potential active Methyl 8-bromo-3-phenyl-5a,9a-dihydro-3H-chromen [4,3-c][1,2] isoxazole-3a(4H)-carboxylate ($C_{18}H_{15}BrNO_4$) has been determined from single crystal X-ray diffraction technique. The title compound crystallizes in the triclinic space group Pī with unit cell dimension a=8.3129 (3) ${\AA}$, b=9.5847 (4) ${\AA}$ and c=11.1463(4) ${\AA}$ [${\alpha}=98.457(3)^{\circ}$, ${\beta}=102.806(2)^{\circ}$ and ${\gamma}=105.033(5)^{\circ}$]. Single crystals suitable for X-ray diffraction were obtained by slow evaporation method, the isoxazole and six membered pyran rings adopts envelope conformation. In the crystal, molecules are linked via pairs of inter molecular $C-H{\ldots}O$ hydrogen bonds to form dimmers.
Govindaraj Saravanan,Veerachamy Alagarsamy,Pandurangan Dineshkumar 대한약학회 2021 Archives of Pharmacal Research Vol.44 No.8
A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterizedby FT-IR, 1H NMR, mass spectroscopy and bases of elementalanalysis with the aim of developing potent analgesic,anti-inflammatory and antimicrobial agents. Tailflicktechnique, carrageenan-induced foot paw edema testand agar streak dilution test were performed for screeninganalgesic, anti-inflammatory and in vitro antimicrobialactivity respectively. Moreover all compounds wereexamined for its ulcerogenicity. Results revealed that entireseries of compounds exhibited mild to good analgesic, antiinflammatoryand antimicrobial activity with low to moderateulcer index. The relationship between the functionalgroup variation and the biological activity of the evaluatedcompounds was discussed. Out of various synthesizedcompounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl)isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was foundto be the most active compound.
Antidepressant-like Effects of the Gastrodia elata Bl Extract in Mice
( Soon Sang Hong ),( Seung Hun Cho ) 대한한방신경정신과학회 2013 동의신경정신과학회지 Vol.24 No.3
Objectives : A growing body of evidence has suggested that the dysfunction of glutamatergic systems plays a pivotal role in major depressive disorder (MDD). This study was performed to investigate the antidepressant-like effects of the ethanolic extract of Gastrodia elata Bl (GE) in mouse models and to investigate the role of α-amino-3-hydroxy-5-methyl-4- isoxazole-propionic acid (AMPA) receptors in producing these antidepressant-like effects. Methods : The forced swim test (FST) and tail suspension test (TST) were used to investigate GE`s behavioral effects in mice. Additional biochemical and behavioral experiments with NBQX, an AMPA receptor antagonist, were undertaken to determine whether the antidepressant-like properties of GE are involved in AMPA receptor throughput. Results : Oral administration of GE extract (1,600 mg/kg) 1h prior to testing significantly reduced the immobility times in the FST and TST. These antidepressant-like effects of GE extract were increased dose-dependently. Pre-treatment with NBQX significantly attenuated the reduction in immobility time induced by the GE extract in the FST and TST. Conclusions : The ethanolic extract of GE may exert antidepressant-like effects with involvement of AMPA receptor.
Antidepressant-like Effects of the Gastrodia elata Bl Extract in Mice
홍순상,조성훈 대한한방신경정신과학회 2013 동의신경정신과학회지 Vol.24 No.3
Objectives :A growing body of evidence has suggested that the dysfunction of glutamatergic systems plays a pivotal role in major depressive disorder (MDD). This study was performed to investigate the antidepressant-like effects of the ethanolic extract of Gastrodia elata Bl (GE) in mouse models and to investigate the role of α-amino-3-hydroxy-5-methyl-4- isoxazole-propionic acid (AMPA) receptors in producing these antidepressant-like effects.Methods :The forced swim test (FST) and tail suspension test (TST) were used to investigate GE's behavioral effects in mice. Additional biochemical and behavioral experiments with NBQX, an AMPA receptor antagonist, were undertaken to determine whether the antidepressant-like properties of GE are involved in AMPA receptor throughput.Results :Oral administration of GE extract (1,600 mg/kg) 1h prior to testing significantly reduced the immobility times in the FST and TST. These antidepressant-like effects of GE extract were increased dose-dependently. Pre-treatment with NBQX significantly attenuated the reduction in immobility time induced by the GE extract in the FST and TST.Conclusions :The ethanolic extract of GE may exert antidepressant-like effects with involvement of AMPA receptor.
Il Soo Moon(문일수),Dae-Hyun Seog(석대현) 한국생명과학회 2009 생명과학회지 Vol.19 No.8
α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) 수용체는 중추신경계에 널리 발현하며, 연접부위에서 글루타메이트에 의한 흥분성 신경전달의 역할을 행한다. 이러한 수용체의 조절은 학습과 기억에 관여한다. 본 연구에서는 AMPA receptor subunit glutamate receptor-interacting protein 1 (GRIP1)과 결합하는 단백질로 armadillo family인 p0071/plakophilin-4을 분리하였다. GRIP1 단백질은 p0071/plakophilin-4 단백질의 C-말단과 결합하며, armadillo family 단백질 중 p0071/plakophilin-4 과만 결합한다. 효모 two-hybrid assay에서 GRIP1의 Postsynaptic density-95/Discs large/Zona occludens-1 (PDZ) 영역이 p0071/plakophilin-4 단백질과의 결합에 관여하며, p0071/plakophilin-4 단백질의 C-말단 아미노산인 “S-X-V” 배열이 결합에 필수적이었다. 이러한 결합은 뇌 균질액에서 Glutathione S-transferase (GST) pull-down assay와 공면역침강법으로 확인하였다. 이러한 결과들은 AMPA 수용체가 연접후막에 안정적으로 위치하는 새로운 역할을 시사한다. α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptors are widespread throughout the central nervous system and appear to serve as synaptic receptors for fast excitatory synaptic transmission mediated by glutamate. Their modulation is believed to affect learning and memory. To identify the interaction proteins for the AMPA receptor subunit glutamate receptor-interacting protein 1 (GRIP1), GRIP1 interactions with armadillo family protein p0071/plakophilin-4 were investigated. GRIP1 protein bound to the tail region of p0071/plakophilin-4 but not to other armadillo family protein members in a yeast two-hybrid assay. The “S-X-V” motif at the carboxyl (C)-terminal end of p0071/plakophilin- 4 is essential for interaction with GRIP1. p0071/plakophilin-4 interacted with the Postsynaptic density-95/Discs large/Zona occludens-1 (PDZ) domains of GRIP1 in the yeast two-hybrid assay, as is indicated also by Glutathione S-transferase (GST) pull-down, and co-immunoprecipitated with GRIP1 antibody in brain fraction. The findings of this study provide evidence that p0071/plakophilin-4 is an interactor of GRIP1.