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전라옥,Yoon-Jung Kim,Yejin Cheon,류재하 대한약학회 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 lipopolysaccharideactivated macrophages. Most of the tested compounds were identified as potent PPARγ agonists, indicating their potential as drug candidates for diabetes.
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.
Haloacetophenone의 광분해와 DNA 절단활성
전라옥 숙명여자대학교 약학연구소 2001 약학논문집-숙명여자대학교 Vol.17 No.-
The photolytic behaviors and DNA cleaving activities of the haloacetophenones; 4'-, and 2'-bromoacetophenones, 4'-chloroacetophenone, and bromofluoroacetophenones, which are phenyl radical precursors upon irradiation, have been investigated. Bromofluoroacetophenones revealed their potential as new photoinducible DNA cleaving agents comparing with 4'-bromoacetophenone.
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.
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.
전라옥,이지혜,정상헌 대한약학회 2003 약학회지 Vol.47 No.5
Isoflavonoids are abundant in natural products and reported with many synthetic variations. However, relatively few quinolone analogs of isoflavonoids have been described. As part of our endeavor to pursue biologically active novel isoflavonoids, we report an efficient synthetic route for quinolone analogs of isoflavonoids. The key intermediate, 2'-aminochalcone 2 was obtained from substituted aniline and cyclized to afford quinolones 6, 8a, and 8b.
PPARΥ의 선택적 리간드로서 Thiazolidinedione 유도체의 합성
이수미,전라옥 숙명여자대학교 약학연구소 2004 약학논문집-숙명여자대학교 Vol.20 No.-
Thiazolidinedione analog is one of the potential antidiabetic drug that binds and activates PPARY, which is the member of nuclear hormone receptors superfamily and enhances insulin sensitivity. In an effort to develop a novel and effective antidiabetic thiazolidindione analog, we have synthesized tolyl-linked thiazolidinedione analog 11 by coupling reaction of the hydrophobic segment, methyl-p-tolylaminoethanol 4 with hydroxybenzylthiazolidinedione 9.
Synthesis of Polymeric Thiazolidinedione and Fibrate Conjugates
김윤정,전라옥,Bomi Kang 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.2
Pioglitazone is a thiazolidinedione (TZD) class of antidiabetic drug acting mainly through activation of PPARγ which is a member of family of ligand activated nuclear hormone receptors. Clofibrate is an antilipemic drug acting through activation of PPARα. Despite the impressive antidiabetic activity of TZD, several side effects are implicated to use of this drug on some patient. Dual acting PPARα/γ agonists have received increased attention to improve the profiles of the PPARγ agonists. Hence, we describe here synthesis of TZD and/or fibrate derivatives- containing homo- or copolymers, poly(TZD) 7, poly(TZD-MAA) 8, poly(TZD-FA) 9, poly(FA) 10, and poly(FA-MAA) 11. The contents of TZD unit in copolymers, poly(TZD-MAA) 8 and poly (TZD-FA) 9 were 25 and 19 mol %, respectively. The number average molecular weights of the polymers determined by GPC were in range from 466 to 12600 and the polydispersity indices were in the range of 1.2~13.3