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에폭시드 고리 개환에 의한 옥사졸리딘티온의 합성 및 항바이러스 활성
황규자,이희경,한호규 숙명여자대학교 약학연구소 1998 약학논문집-숙명여자대학교 Vol.15 No.-
A synthesis and antiviral actvity of new oxazolidinthiones are discribed. Based on the structure-activity relationship from UC38 and UC84, 4-chloro-3-isopropyloxycarbonylphenylamino moiety is found to be a essential pharmacophore for activity. The oxazolidines, which are cyclic thiocarbamate of a 5-membered ring were designed by molecular modification of UC38. Nucleophilic attack of substituted aniline to epoxide by using lithiumperchlorate as a catalyst gave 2-aminoalcohols in good yields. Treatment of 2-aminoalcohol either with thiophosgen or with thionyl chloride gave oxazolidinthiones and 5-chloromethyl-N-phenyl-1,2,3-oxathiazolidin-2-oxide, respectively. Screening results of the 8 oxazolidinthiones against the typical three kinds of viruses(HSV-l, VSV, HIV-1) showed lower activity than those of the UC84 and UC38.
성낙도,유성재,남기달,장기혁,한호규 충남대학교 생물공학연구소 1999 생물공학연구지 Vol.7 No.-
기질(S) 화합물로 30종의 5,6-dihydro-2-trifluoromethyl-1,4-oxathiin carboxanilide 유도체들을 합성하고 벼 잎집무늬 마름병균(Rhizoctonia solani)과 밀 붉은 녹병균(Puccinia recondita)에 대한 항균활성(in vivo) 값(pI_50)을 측정하였다. (S)는 잘록병균보다 밀 붉은녹병균에 대하여 보다 큰 항균활성을 나타내었으며 두 종의 균에 대하여 3-methoxy, 11, 3-iso-propyloxy, 13 및 3-iso-propyl 치환체, 25가 제일 큰 활성을 보였다. 그리고 치환(X)-phenylcarbamoyl group의 변화에 따른 물리-화학 파라미터와 항균활성(pI_50)으로부터 구조-활성관계(SAR)를 검토 한 결과, 벼 잎집무늬 마름병균에 대하여는 공명효과에 따른 전자밀게(R<0)의 소수성이 큰(π>0) m-alkyl 치환기(X)가, 그리고 밀 붉은녹병균에 대하여는 분자 분극율(Sp.Po1.)과 분자의 음하전(ABSQ<0)을 위시하여 HOMO에너지(e.v.)가 클수록(HOMO<0) 높은 항균활성을 나타내었다. 또한, 전하-조절 반응에 의한 수용체-(S)간의 상호작용과 높은 활성발현 조건들이 검토되었다.(1998년 2월 3일 접수, 1998년 12월 1일 수리) New thirty derivatives of 5,6-dihydro-2-trifluoromethyl-1,4-oxathiin carboxanilide as substrate(S) were synthesized and their fungicidal activities in vivo against rice sheath blight(Rhizoctonia solani) and wheat leaf rust(Puccinia recondita) were examined. The structure activity relationships(SAR) between the activities(pI_50) and a physicochemical parameters of substituents(X) at the phenylcarbamoyl group were analyzed using the adaptive regression analysis method. The 3-methoxy, 11, 3-isopropyloxy, 13 and 3-isopropyl substituent, 25 as X on the phenylcarbamoyl group exhibited the most highest fungicidal activity against the two fungi. The fungicidal potency of the (S) against Puccinia recondita was higher than Rhizoctonia solani. In case of Rhizoctonia solani, the molecular hydrophobicity(π>0) and resonance effect(R<0) by meta-alkyl substitutents with electron donating were important factors in determining fungicidal activity. And the HOMO energy(HOMO>0), ABSQ, sum of absolute values of the atomic charges on each atom and specific polarizability(Sp.Pol<0) of (S) were significantly influential towards fungicidal activity against Puccinia recondita. The interaction between (S) and receptor against from the based on SAR studies proceeds through charge-control reaction, and conditions to show higher activity has been also discussed.
Two Class Approximation of TLB (Tomato Late Blight) Activity Data
Hoh Gyu Hahn(한호규),Ashek Ali MD,Seung Joo Cho(조승주) 한국농약과학회 2005 농약과학회지 Vol.9 No.2
Quantitative Structure Activity Relationship (QSAR) assumes the relatedness between physical property and biological activity. However, activity data measured at single concentration such as percent activity have not been used extensively for modeling purpose. This probably comes from the fact that these values are qualitative instead of quantitative. To utilize percent activity data for molecular modeling, we classified the whole data into two classes. One class represents the active while the other signifies the inactive. The percent activity data of β? Ketoacetoanilides measured for TLB (Tomato Late Blight) were investigated. CoMFA (Comparative Molecular Field Analysis) was used as a discriminant function. Using CoMFA provides 3D (three dimensional) information, which is crucial for chemical insight. It can also serve as a predictive model. The resultant model classified the given data correctly (98%). When LOO (leave?one?out) crossvalidation procedure was applied, the classification accuracy was 69%. Therefore two class approximation of percent activity data with CoMFA can be utilized to understand the relationship between chemical structure and biological activity and design subsequent chemical analogs.
Korean Study-Abroad Students`s Retrospective Narratives of Adjustment Experience on the Host Country
( Hoh Sung Choe ) 21세기영어영문학회 2014 영어영문학21 Vol.27 No.3
This study investigates two Korean study abroad students’ adjustment process, highlighting their linguistic, academic, and emotional issues. Retrospective narrative was used as a methodological framework to reconstruct their life and experience in the host country. Autobiographies, personal conversations, and interviews are the primary data source. The participants were asked to write an autobiography focusing on their study-abroad experience. Personal conversations took place occasionally and field notes were kept during the conversations. Each participant was interviewed every other month, a total of six times distributed over a year. Data analysis reveals that they faced linguistic, academic, and emotional struggle when they arrived in the host country, and that the successful adjustment can be achieved only when all three types of struggles are eliminated. For instance, one was linguistically and emotionally well adjusted, but his unsuccessful academic life forced him to return. The other suffered from the emotional struggle, which was a serious obstacle to integration into the life in the host society.