의약품으로 개발된 Pyridazine 유도체

권순경 德成女子大學校 藥學硏究所 2000 藥學論文誌 Vol.11 No.1

Although the first pyridazine was obtained in 1886, this heterocycle was not thoroughly investigated such isomers as pyrimidine and pyrazine especially in the field of drug development because pyridazine derivatives do not occur as natural products. Recently medicinal chemists have an growing interest in the pyridazine derivatives, since many pyridazine derivatives were found to possess various potential therapeutic activities. In this paper sixty-eight pyridazine derivatives, which are already introduced as medicines or are being developed as drugs were classified according to their pharmacological activities, reviewed since 1995 and the relationship of structure-activities was discussed.

중ㆍ고등학생의 약물남용실태 조사 및 대책에 관한 연구

권순경 德成女子大學校 1989 德成女大論文集 Vol.18 No.-

With the increasing concern about drug abuse among young people, information is needed that will help to assess the incidence and the nature of drug abuse in Korea. There are only a few studies of drug use among junior and senior high school students and this report was planned to add another sample. The author performed a questionnaire survey on drug use among 4201 junior and senior high school students in Seoul. He found that 20.1% of the students had used drugs at least once in the past and stimulants were used most extensively. The author also found that the students with a bad home background and had school record and juvenile delinquents had used more drugs.

1,2-디아진 유도체 합성

권순경 德成女子大學校 藥學硏究所 1996 藥學論文誌 Vol.7 No.1

Although the first pyridazine was obtained in 1886, this heterocycle was not thoroughly investigated as pyrimidines and pyrazines especially in the field of drug development because pyridazines do not occur as natural products. Recently medicinal chemists have an growing interest in the pyridazine derivatives, since many pyridazine derivatives were found to possess various potential therapeutic activities. Among the biological activities antihypertensive and cardiotonic activities are most popular. In this paper syntheses of all pyridazine derivatives which are used as drugs or under development as antihypertensive and cardiotonic therapeutics were reviewed since 1976 and the relationship of structure-activities was discussed.

Aryloxyallylthiopyridazine 유도체 합성

권순경,김미경 德成女子大學校 藥學硏究所 2002 藥學論文誌 Vol.13 No.1

Allylthio group of the sulfur compounds of garlic oil plays an important role for prevention and treatment of hepatic diseases induced by toxic substances or carbon tetrachloride. Thus allylthio group as pharmacologically active group was introduced into pyridazine heterocycle ring. Aryloxyallylthiopyridazine derivatives were synthesized and their hepatoprotective activities were screened in rat. The activities of these compounds were weaker than alkoxyallylthiopyridazine derivatives, which exhibit a superior hepatprotective effect.

COX-2 억제제의 구조-활성

권순경 德成女子大學校 藥學硏究所 2001 藥學論文誌 Vol.12 No.1

Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachidonic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet appregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDs) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAIDs. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.

1,5-Diphenylhydantoins을 위한 새로운 Methyl α-Anilinophenylacetate 유도체의 합성

권순경,최희전,박명숙 德成女子大學校 藥學硏究所 2001 藥學論文誌 Vol.12 No.1

For the development of new COX-2 inhibitor, novel key intermediates (2∼4) synthesized through esterification, bromination and α-substitution from phenylacetic acid. The methyl phenylacetate 2 was synthesized through reflux phenylacetic acid with sulfuric and methanol. The methyl α-bromophenylacetate 3 was produced through radical bromination using N-bromosuccinimide from 2. The optical amination to introduce anilino group was contolled under 80℃ in DME. The bromo intermediate was converted to the final methyl α-anilinophenylacetate 4 through reaction with aniline.

Ethyl 2-Methyl-3-Pyrazinyl-3-oxopropionate의 합성과 케토-엔올 토토머화현상

권순경,박명숙,박해선 德成女子大學校 藥學硏究所 2002 藥學論文誌 Vol.13 No.1

Ethyl 2-methyl-3-pyrazinyl-3-oxopropionate is a key intermediate for the development of new drugs and can be synthesized through Claisen condensation from methyl pyrazine carboxylate and ethyl propionate. Even though in β-diketones esters in general the amount of enol form present at equilibrium is far higher than keto form, this key compound showes that the keto concentration is high. It can be explained because of the electron-releasing effect of α-methyl group.

4,5-치환 3-alkoxy-6-allythiopyridazine 유도체 합성

권순경 德成女子大學校 藥學硏究所 2002 藥學論文誌 Vol.13 No.1

Through a modification of allicin structure a disagreeable odor and chemical instability of allicin can be improved. 3-Alkoxy-6-allylthiopyridazine derivatives exhibit a superior effect for prevention and treatment of hepatic diseases induced by carbon tetrachloride and aflatoxin B1 and for prevention of human tissues from radiation. These compounds inhibit also efficiently SK-Hep-1 cell proliferation through induction of apoptosis. So another 4,5-mono-or di-substituted 3-alkyloxy-6-allythiopyridazine derivatives were synthesized on purpose to find out SAR of allylthiopyridazine in hepatoprotective and hepatotherapeutic acitivitis and to develop more effective drug candidate.

중고등학생의 에이즈 豫防敎育을 통한 에이즈 知識과 性意識 變化에 關한 硏究

권관우,이경무,김정순 韓國學校保健學會 1999 韓國學校保健學會誌 Vol.12 No.1

AIDS is worldwide problem. It has threatens societies and is potentially a big problem among youth. UNAIDS has warned that collective global responses are necessary; with half of the newly infected being children and young people in 1998, educating youth below age 24 is essential. Because of both their unexpected, strong sexual activities and an easjer tendency to change their behavior than adults, UNAIDS emphasizes the importance of prevention education leer youth. In Korea, 4 cases of HIV infection have officially been reported among high school students. Considering the potential seriousness of HIV inflection among youth, the Korean Anti- AIDS Federation (KAAF) began an education programme for Korean youth (middle & high school pupils) as one intervention method in 1993. The purpose of this study is to evaluate the impact of the education programs performed and to develop a better programme. The intervention method used in this study was mainly a lecture in a big or small auditorium or through broadcasting systems using audio-visual teaching aids. The period of this survey was from Nov. 10 to Dec. 26. in 1998. The subjects surveyed were 792 pupils who were sampled from 12 different middle and high schools in Seoul by a two-stage cluster sampling. Self recording the structured questionnaire was used far data collection. Data were analyzed by using a paired t-test to compare the knowledge difference before and after the interrention method. A chi-square test to compare the consciousness difference between pre-post-education results was used, and an ANOVA was used to compare the knowledge difference among the selected groups. Major results of this study are summarized as follows: (1) AIDS knowledge significantly changed after AIDS prevention education. (2) The direct lecture in a big or small auditorium is more effective than an indirect lecture through a broadcasting system or through audio-visual teaching aids. (3) Those who had not seen obscene materials (e.g. pornography films, magazines etc.) acquired much more knowledge than others after AIDS prevention education. (4) Those who had no girlfriend/or boyfriend acquired much more knowledge than the others after AIDS prevention education. (5) As to the attitudes toward chastity, more girls than boys and students who had not seen obscene materials rather than those who already had were liable to support the state ment: "all should remain chase" and their consciousness on "being chaste" changed much more than that of others after intervention. (6) As to the individual evaluation of lectures, 23.1% shows "very good" , 44.1% "good" , 26.9% "normal"'-'thus, the positive evaluation was to 94.2%. The negative response was 5.8%. (7) As to the desire fur AIDS education sponsored by KAAF in the future, more than몫90.5% showed a positive reaction. (8) As to the educators in future education methods, pupils wanted lecturers from outside their schood. (9) Students from vocational high schools have seen obscene materials much more than other groups and the percentage of these who had a girlfriend/or boyfriend was higher than that of the ethers as wello. (10) 90% of those who watched obscene materials responded that they experienced these materials while at middle school and 100% before reaching the second grade of high school. (11) The number of boys who have experienced obscene materials is twice as many as that of girls. (12) The percentage of boys who have a girlfriend is much higher than the percentage of girls who have a boyfriend. (13) Among those who have friends of the opposite sex, 11.1% say that they hare had sexual contact and 20.8% hare experienced kissing and caressing.

마늘의 유기유황성분과 생리활성

권순경 德成女子大學校 藥學硏究所 2003 藥學論文誌 Vol.14 No.1

Garlic (Allium sativum L) is one of the oldest cultivated plants and has been used throughout the world as food supplement and folk medicine for thousands of years. In modern times a number of garlic derived products are introduced on the market as health food supplement in ever growing scale. In 1844 German chemist Wertheim investigated the garlic first time chemically and thereafter many kinds of organosulfur compounds were isolated and their biological activities were elucidated scientifically. The main biological activities are antibacterial, antifungal, antithrombotic, cholesterol-lowering, antineoplastic and hepatoprotective activities. Chemical works as well as therapeutic and preventive effects of garlic are reviewed.