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신관석(Kwan Seog Sin),남재우(Jae Woo Nam),이창규(Chang Kiu Lee),전종갑(Jong Gab Jun) 대한약학회 1993 약학회지 Vol.37 No.3
A new series of 7-deazapurine derivatives[7,8] as purine antagonists was prepared. Diethyl 4-cyano-N-(diphenylmethylene)-3-arylglutamate[3] were synthesized by LDA-catalyzed Michael addition of N-(diphenylmethylene)glycine ethyl ester with (E)-2-cyano-3-arylacrylate. Deprotection yields diethyl 4-cyano-3-arylglutamate, which were easily cyclized to 4-cyano-2-ethoxycarbonyl-5-oxo-3-arylpyrrolidine[4]. The compounds[4] were treated with NaBH4 and then with (C2H5)3OBF4 to give 4-cyano-5-ethoxy-2H-2-ethoxymethyl-3-aryl-3,4-dihydropyrrole[6], which were converted to 7-aryl-6-amino-8-ethoxymethyl-7,8-dihydro-7(3H, 9H)-deazapurine-2-thione[7] and 7-aryl-2,6-diamino-8-ethoxymethyl-7,8-dihydro-7(9H)-deazapurine[8] with possible activity against neoplastic disease.
신관석(Kwan Seog Sin),성선영(Sun Young Sung),남재우(Jae Woo Nam),최상운(Sang Un Choi),이정옥(Chong Ock Lee) 대한약학회 1992 약학회지 Vol.36 No.4
A new series of methotrexate analogues was prepared in which the beta-position of the glutamic acid moiety is substituted by the aryl groups. The glutamic acid moiety was modified in order to enhance the lipophilic property. Reaction of N-acetylglicine ester[1] with ethyl 3-arylacrylate derivatives[2] produced trans-3-aryl-2-carboxy-5-pyrrolidone derivatives[3], which were hydrolyzed to give beta-aryl-glutamic acid derivatives[4]. The compounds[4] were treated with the p-aminobenzoic acid moiety and then with the pteridine ring moiety to give beta-arylmethotrexate derivatives[6,7]. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against murine leukemias and against human tumor cell lines in vitro. Several compounds showed significant antibacterial activity.
신관석(Kwan Seog Sin),김남호(Nam Ho Kim),이주헌(Joo Heon Lee),성선영(Sun Young Sung),Peter Pachaly 대한약학회 1997 약학회지 Vol.41 No.2
A series of 7-deazahypoxanthine and 7-deazaadenine derivatives[6,7.8.9.10,13] as purine antagonists was prepared. The pyrrolidine-5-one derivatives[4,11] were treated vith (C2H5)3OBF4 to give 3-aryl-5-ethoxy-2H-3,4-dihydropyrrole[5,12], which were converted to 7-aryl-7,8-dihydro-7(9H)-deazahy-poxanthine[6,7,8,9,10] and 7-phenyl-2-methyl-7,8- dihydro-7(9H)-deazaadenine[13].
8-아미노우고닌 유도체의 Prostaglandin $E_2$ 생성에 대한 저해작용
장진희,신관석,김현표,박해일,Jang, Jin-Hee,Sin, Kwan-Seog,Kim, Hyun-Pyo,Park, Hae-Il 대한약학회 2008 약학회지 Vol.52 No.1
8-Acyl and 8-sulfonylamidowogonin analogues were synthesized as potential anti-inflammatory agents. Nitration of 5,7-dihydroxyflavone (chrysin) followed by methylation of phenol groups and reduction of nitro group yielded 8-aminowogonin analogues. Acylation and sufonylation of 8-aminowogonin followed by demethylation reactions gave the title compunds. The synthesized wogonin analogues showed much reduced inhibitory activity on prostaglandin $E_2\;(PGE_2)$ production.
철쭉나무 (Rhododendron schlipenbachii) 잎의 Flavonoid성분
김기범,신관석,김창민,권용수 한국생약학회 2006 생약학회지 Vol.37 No.3
compounds were isolated from EtOAc soluble fraction of the leaves of Rhododenderon schlipenbachii. On thebasis of spectral data, they were identified as quercetin (1), juglanin (2), avicularin (3), quercitrin (4), afzelin (5), and hirsutrin(6), respectively.Key wordsRhododenderon schlipenbachii, Ericaceae, flavonoids.... (Ericaceae). Rhododendron. ... ...... .. ... 1200. .. .... ... ......1), ...... ... .. .... ... . 20
개선된 HPLC분석법을 이용한 세파클러 모노하이드레이트 250 mg 캡슐의 생물학적동등성
김태완,한선영,송옥경,신관석,강성하,이범진,Kim, Tae-Wan,Cao, Qing-Ri,Han, Sun-Young,Song, Ok-Kyoung,Sin, Kwan-Seog,Kang, Sung-Ha,Lee, Beom-Jin 한국임상약학회 2005 한국임상약학회지 Vol.15 No.1
A bioequivalence study of CKD $Cefaclor^{(R)}$ capsule (Chong Kun Dang Pharm Co., Ltd) to $Ceclor^{(R)}$ capsule (Lilly Korea Co., Ltd.) was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korean volunteers received each medicine at the cefaclor dose of 250 mg in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. An improved high-performance liquid chromatorgraphy (HPLC) analytical method with UV detection was used to determine plasma cefaclor concentration in human volunteers for 8 hr after oral drug administration. The area under the plasma concentration-time curve from time zero to 8 hr ($AUC_{0-8hr}$) was calculated by the linear trapezoidal rule. the $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_{0-8hr}\;and\;C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the cross-over design was properly performed. The $90{\%}$ confidence intervals of the $AUC_{0-8hr}$ ratio and the $C_{max}$ ratio for CKD $Cefaclor^{(R)}$ and $Ceclor^{(R)}$ were $0.9400{\leq}{\delta}{\leq}1.0345$ and $0.8858{\leq}{\delta}{\leq}1.1021$, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the of CKD $cefaclor^{(R)}$ capsule was bioequivalent to $Cefaclor^{(R)}$ capsule with respect to its bioavailability.
고경수(Kyeong-Soo Ko),신관석(Kwan-Seok Shin),김창민(Chang-Min Kim) 한국생약학회 1983 생약학회지 Vol.14 No.4
The composition of the phenolic compounds of 14 species, 2 varieties and 1 taxon of the Sedum plant in Korea were studied to identify their inter-specific relationships and their taxonomical position. The phenograms and contour diagrams obtained from the HPLC of EtOAc soluble fraction of these plants were classified into 7 alliences according to their chemical patterns. These chemical patterns agreed with Satake`s classification except for Sedum aizoon. These plants were subdivided into 5 alliences in the Sedum section and 2 alliences in the Hylotelephium section. 1 type of the Sedum spectabile showed a difference in the number of stamens, it could be trated as another category above variety according to this result.