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정신분열병 환자의 도파민 $D_1$ 수용체 유전자형과 치료반응간의 연관
백종우,이민수,이충순,임동준,함원훈,Paik, Jong Woo,Lee, Min Soo,Rhee, Choong Soon,Lim, Dong Ju,Ham, Won Hun 대한생물정신의학회 2001 생물정신의학 Vol.8 No.1
Background : Dopamine receptors have been regarded as a strong candidate involved in etiology of schizophrenia and a target for various antipsychotic drugs. The purpose of our study was to investigate whether dopamine $D_1$ receptor(DRD1) gene polymorphisms would predict the treatment response to antipsychotics in schizophrenia. Method : One hundred thirty-four schizophrenic patients, who met DSM-IV criteria for schizophrenia were entered into a 48 -week study. The psychopathology of the patients was assessed at baseline, 12th, 24th 48th weeks of treatment by PANSS. Responders were defined by a 20% of the reduction in total PANSS score at end point. The genomic DNA fragment corresponding to nucleotides of dopamine $D_1$ receptor gene was amplified by polymerase chain reaction(PCR). Result: Neither allelic frequencies nor genotypes for dopamine $D_1$ receptor differed significantly between responders and non-responders. Also, there was no difference of changes of PANSS scores among three genotype groups of the dopamine $D_1$ receptor. Conclusion : Allelic variation in the dopamine $D_1$ gene is not associated with individual differences in antipsychotic response.
프로스타글란딘 유도체의 합성과 그의 생물학적 활성에 관한 연구 2. 위궤양과 위산분비에 대한 프로스타글란딘 유도체의 효과
조태순(Tai Soon Cho),이선미(Sun Mee Lee),함원훈(Won Hun Ham),이병무(Byung Mu Lee),김경례(Kyoung Rae Kim),지상철(Sang Cheol Chi),고준일(Jun Ill Ko),박인(In Park),오창영(Chang Young Oh),박호군(Ho Koon Park),김형자(Hyoung Ja Kim),이향우(H 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.1
The antiulcer effects of newly synthesized prostaglandin derivatives were investigated in various experimental ulcer models and on gastric secretion in rats. HK-3 and HK-4, PGE₂ derivatives, prevented the formation of acute gastric ulcer induced by ethanol or aspirin in pylorus-ligated rats. The ulcer formation was moderately inhibited by HK-1 and HK-2, PGF_(2α) derivatives, and aggravated by SK-1, SK-2 and SK-3, PGF_(2α) derivatives. HK-3 and HK-4 reduced the volume, acid output and pepsin output of gastric juice in pylorus-ligated rats. The gastric perfusion with physiologic saline(pH 6.0) showed relatively constant acid secretion and indomethacin increased the acid secretion. The acid secretion was markedly decreased by PGE₂ but PGF_(2α) caused little change. Prostaglandin derivatives, especially HK-3 and HK-4, significantly inhibited the acid secretion induced by indomethacin. The results show that, PGE₂ derivatives, HK-3 and HK-4, inhibit acid secretion and also have protective effects on gastric ulceration induced by ethanol or aspirin.
새로운 Quinolone 誘導體의 合成에 關한 硏究(Ⅱ)
함원훈,고윤석,배형준,이기영,정영훈 성균관대학교 약학연구소 1995 成均藥硏論文集 Vol.7 No.1
Abstract - Palladium catalyzed cross-coupling reactions of aryl halides with organo tin reagents and π-sufficient aromatic heterocycles proceeded easily and efficiently during carbon-carbon bond formation. We used this method for the anti bacterial agents, and synthesis of new quinolone derivatives which have C-C bond at C-7 position of general quinolone moieties. Quinolone moieties, and aryl tin or aromatic heterocycles in the presence of palladium catalyst were coupled to afford new quinolone derivatives. The synthesis and structure-activity relationship are presented.
α-Allenic alcohol의 Electrophile과의 반응에 관한 연구
함원훈,양재권,황현준,오창영,배형준 성균관대학교 약학연구소 1994 成均藥硏論文集 Vol.6 No.1
Electrophilic addition of the halogens and related X-Y reagents to alkenes and alkynes has been a standard procedure since the beginning of modern organic chemistry. Regio- and stereospecific addition of electrophiles to alkenes and alkynes have been used for many years for controlled introduction of special functional groups as well as for other more general synthetic purposes. More recently, electrophiles have been added to the list of synthetically useful reagents that undergo stereocontrolled addition to π-bonds. But, the study of allenes on electrophiles has not been attentioned so far. In this paper, we report allene's reactivity and its reaction pattern on electrophiles such as PhSeCl, p-TsOH, HG(OCOCF_3)_2 and NBS.
함원훈,임태균,정윤성,정윤호,양재권,최원철 성균관대학교 약학연구소 1993 成均藥硏論文集 Vol.5 No.1
Diltiazem and nifedipine, have been used throughout the world as an effective antianginal and antihypertensive agent. In order to increase the activity of these drugs, we synthesized the diltiazem-nifedipine coupling compounds. These compounds^(1-8) were tested for antihypertensive effect. Unfortunately, these compounds didn't show any promising activities.
Piperine 유도체 〔3-(3',4'-dihydroxyphenyl)-2-propenic acid amide〕의 합성에 관한 연구
林中基,咸元勳,김진영 성균관대학교 약학연구소 1990 成均藥硏論文集 Vol.2 No.1
Abstract-3,4-Methylenedioxyphenyl cinnamic acid was synthesized from the reaction of 3,4-methylenedioxy benzaldehyde with malonic acid, via Perkin reaction and it was added to SOCI_2. From acid chloride, many amide derivatives were synthesized, using various amines. In the final step, cleavage of 3,4-methylenedioxy group was not accomplished by the traditional method of halogenation with phosphorous pentachloride. And, protection of the OH-group of catechol with tosyl, acyl, methoxy methyl chloride or acetonide was failed. So, aryl benzyl ethers were prepared from a protocatechualdehyde by treating an alkaline solution of the protocatechualdehyde with a benzyl chloride. Amide derivatives were synthesized from the former ways. Benzyl group was readily removed by hydrogenolysis.
임중기,함원훈,박호군 성균관대학교 약학연구소 1990 成均藥硏論文集 Vol.2 No.1
Abstracts-Prostaglandins exhibit diverse pharmacological properties and are now recognized as local hormones that control a multitude of important physiological process. (R)-4-hydroxy-2-cyclope-ntenone is a very useful intermediate to synthesize the prostaglandin derivatives. The optically active cyclopentenone building blocks were synthesized in various ways ; by resoultion of the racemic hydroxy ketone ; by preparation from chiral natural products via resolved synthetic intermediates, by asymmetric synthesis, by microbial or enzymatic techniques, etc. The hydroxy ketone can be produced by preparation from chiral building block via microbial organisms. The key chiral building block is dimethyl-5-hydroxy-4R-hydroxy-2-oxopentane phosphate which can be synthesized the optically active cyclpentenone via Horner Emmon reaction. This paper describes the preparation of the chiral diol compound 2 in detail.
Piperine 誘導體[5-(3-methoxy-4-hydroxyphenyl)-2,4-pentadienoic acid amides]의 合成 硏究
林中基,咸元勳,崔然喆 성균관대학교 약학연구소 1990 成均藥硏論文集 Vol.2 No.1
Abstract-Some 5-(3-methoxy-4-hydroxyphenyl)-2,4-pentadienoic acid amides were synthesized for searching new anticonvulsant agents. The amides could be synthesized by condensation of protected vaniline with crotonic acid amides in the presence of sodium amide. A MOM Ether(methoxymethyl ether) was used to protect one phenolic hydroxyl group of vaniline. MOM Ether was selectively cleaved on exposure to 1 : 1 THF-6N hydrochloric acid.
Allene 화합물의 Pinacol Rearragemment에 관한 연구
임중기,함원훈,이미정,양재권,김기수 성균관대학교 약학연구소 1991 成均藥硏論文集 Vol.3 No.1
Abstracts-A effective and new approach to development of impressive methodology for the synthesis of carbocyclic ring system was investigated. It is sequential cationic cycliazationpinacol rearrangement of acetal-allenic derivatives. In order to investigate the acid-catalyzed rearrangement, aldehyde and ketone derivatives with acetal as electrophile were first prepared. And the allenes were synthesized by Yamamoto procedure. Carvocyclic rings were formed by cyclization-pinacol rearrangement from allenes under Lewis acid in pressence of excess trimethylsily trifluoromethane sulfonate.
임중기,이강노,함원훈,이상인 성균관대학교 약학연구소 1992 成均藥硏論文集 Vol.4 No.1
Melandrin, as a possible phytoalexin, which is expected to have the various pharmacological activities; antibacterial, antifungal and antiviral activity, was isolated in 1987 by Woo from Melandrin firmum (Caryophyllaceae). The synthesis of melandrin derivatives has been accomplished by the reaction of 5-hydroxy anthranilic acid ethyl ester with acid chlorides and then by hydrolysis of ethyl ester.