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Jeon Raok,Kim Yoon-Jung,Cheon Ye-Jin,Ryu Jae-Ha The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.5
Benzothiazole derivatives of thiazolidinediones (TZD) were synthesized using a modified Mitsunobu reaction of 2-(benzothiazol-2-ylmethylamino)ethanol (2) with 5-(4-hydroxybenzyl)-3-triphenylmethylthiazolidine-2,4-dione and assayed for activity on peroxisome proliferator-activated receptor (PPAR) subtypes and inhibitory activity of NO production in lipopolysaccharide-activated macrophages. Most of the tested compounds were identified as potent $PPAR_\gamma$ agonists, indicating their potential as drug candidates for diabetes.
Tetrahydroquinoline을 포함하는 Thiazolidinedione의 합성
전라옥 숙명여자대학교 약학연구소 2005 약학논문집-숙명여자대학교 Vol.22 No.-
Thiazolidinedione analog is one of the potential antidiabetic drug that binds and activates PPARγ, which is the member of nuclear hormone receptors superfamily and enhances insulin sensitivity. In an effort to develop a novel and effective antidiabetic thiazolidinedione analog, we have synthesized tetrahydroquinoline-linked thiazolidinedione analog 11 by Mitzunobu reaction of the hydrophobic segment, 2-(tetrahydroquinolinylmethylamino)ethanol 8 with hydroxybenzylthiazolidinedione 9.
3-(4-Hydroxyphenyl)-1-methyl-4(1H)-quinolinone의 합성
전라옥 숙명여자대학교 약학연구소 2003 약학논문집-숙명여자대학교 Vol.19 No.-
Isoflavonoids are abundant in natural products and reported with many synthetic variations. However, relatively few examples of quinolone analogs of isoflavones have been described. As part of our endeavor to pursue biologically active novel isoflavones, we have developed the efficient synthetic route to synthesize azaisoflavones. The key intermediate, 2'-aminochalocone was obtained from substituted aniline and cyclized to afford azaisoflavone.
4'-Bromoacetophenone-Pyrrolecarboxamide 의 DNA 절단활성
전라옥 숙명여자대학교 약학연구소 2002 약학논문집-숙명여자대학교 Vol.18 No.-
광에 의해 활성화 되어 반응성 높은 탄소 라디칼을 형성하는 genotoxic prodrug으로 제안된 4'-bromoacetophenone에 높은 DNA친화도를 갖는 pyrrolecarboxamides를 연결하여 DNA 절단활성을 검사하였다. 4'-Bromoacetophenone-pyrrolecarboxamide의 DNA 절단할 성능은 전배양 시간의 변화에 대해서는 뚜렷한 차이를 보이지 않았으나 반응시간의 증가에 대해서는 비례적으로 상승함을 관찰하였으며, DNAse footprinting실험을 통하여 DNA결합부위와 절단부위가 일치함을 확인하였다.