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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].
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.
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.
홍석기(Seog Ki Hong),남재우(Jae Woo Nam),이경태(Kyung Tae Lee),신관석(Kwan Seog Sin) 대한약학회 1993 약학회지 Vol.37 No.2
6beta-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl)acetamidopenicillanic acid(7a~7c) and 7beta-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl)acetamidocephalosporanic acid(8a~8c) were synthesized and tested in vitro antibacterial activity. Of these new penicillins exhibited good antibacterial activity against Gram-positive bacteria whereas none of the compounds possessed the activity against Gram-negative bacteria at the concentration tested.
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.
개선된 사람 혈장중 세파클러 농도 정량법을 이용한 세파클러 캡슐의 생체이용률 측정
김태완,송옥경,한선영,Cao, Qing-Ri,박미진,강성화,신관석,Cui, Jing-Hao,이범진 한국약제학회 2005 Journal of Pharmaceutical Investigation Vol.35 No.2
After establishing improved HPLC analytical method ofcefaclor in human plasma samples, a bioavailability study of cefaclor capsules was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). The standard calibration curve using an HPLC with UV detector was constructed in a range of 0.0324--16 μg/m1. The 6% perchloric acid instead of 6% trichloroacetic acid was used to precipitate plasma protein. The HPLC chromatograms were precisely and accurately resolved when spiked with human plasma spiked with cefaclor and cephalexin (internal standard). Twenty healthy male Korean volunteers received two commercial cefaclor capsules, Neocef ' capsule (Jinyang Pharm. Co., Ltd) or Ceclor" capsule {Lilly Korea. Co., Ltd.) at the 250 mg cefaclor in a 2 x 2 crossover study. There was a one-week washout period between the doses. Plasma concentrations of cefaclor were monitored for 8 hours after oral drug administration. AUC, the area under the plasma concentration-time curve from time zero to 8 hr (13 points), was calculated by the linear trapezoidal rule method. C,,,a" (maximum plasma drug concentration) and Tmax (time to reach Cma,) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC, and Cmax. 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, ratio and the Cmax ratio for Neocer/Ceclor" were 0.9049 S S < 1.0304 and 0.9776 5 S 1.226, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the bioequivalence of Neocef"/Ceclor" with respect to the extent of absorption.