• 대한화학회지
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• 제37권1호
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• pp.172-177
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• 1993

• Applied Biological Chemistry
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• 제39권3호
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• pp.235-240
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• 1996

제초성 비치환(H) benzenesulfonyl urea 분자, 1은 sulfonyl group 인접의 amino group과 pyrimidinyl group의 N원자 사이에 회합(H-결합)된 형태(II-keto)가 제일 안정하였으며 phenyl 치환$(R_2$ 및 $R_3)$유도체, 2는 전자를 밀수록$(\sigma<0)$ LUMO(ev.)는 음의 값으로 증가하여 물 분자의 HOMO(ev.)사이에 궤도 조절반응(p<0)에따른 전형적인 친핵 반응성을 나타낸다. N-(4,6-이치환-pyrimidine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-fluoro)ethylbenzenesulfonamides, 3 및 N-(4,6-이치환-triazine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-리uoro)ethylbenzenesulfonamide, 4 유도체의 4,6-이치환기(X 및 Y) 와 헤테로 고리의 변화에 따른 올챙이고랭이(Scirpus juncodies.) 에 대한 제초활성은 소수성$((log\;P)_{opt.}=0.89)$이 가장 큰 영향을 미치는 요인이었다. 또한, pyrimidine-치환체, 3이 triazine-치환체, 4보다 양호한 제초활성을 나타내었으며 dimethoxypyrimidine-치환체, 3a가 가장 큰 제초활성을 보였다.

• Archives of Pharmacal Research
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• 제29권11호
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• pp.1006-1017
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• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• 대한화장품학회지
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• 제41권2호
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• pp.143-150
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• 2015

본 연구는 3,7-diarylpyrazolo [1,5-${\alpha}$]pyrimidines의 효과적인 one-pot regioselective 합성을 보여준다. 더욱이, 그 유도체는 뛰어난 CB1R 저해 활성을 나타냈다. 3,7-position에 diaryl group이 치환된 pyrazolo [1,5-${\alpha}$]pyrimidine은 CB1R 후보로서 가능성 있는 pharmacophore이다.

• Bulletin of the Korean Chemical Society
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• 제25권7호
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• pp.991-996
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• 2004

New series of 6-(arylthio)uracils, 6-(4-substituted-1-piperazinyl)uracils, 2,4,5-trioxo-1H,3H-benzothiopyrano[2,3-d]pyrimidine and 5-aryl-2,4-dioxo-1H,3H-pyrimido[5,4-f]benzo[1,4]thiazepines have been prepared and screened for their in vitro activity against herpes simplex-1 virus (HSV-1) and human immunodeficiency virus-1 (HIV-1). The in vitro cytotoxic activity was also evaluated. The results of biological testing revealed that compound 5b showed marginal activity against HSV-1, while compounds 5b and 5f exhibited marginal activity against HIV-1. The rest of the tested compounds were found devoid of antiviral activity against both HSV-1 and HIV-1.

• Archives of Pharmacal Research
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• 제27권9호
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• pp.885-892
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• 2004

Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo［b］ thieno［2,3-d］pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

• Archives of Pharmacal Research
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• 제26권12호
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• pp.990-996
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• 2003

A novel carboacyclic nucleoside analogue, 9-[2-bromo-4-hydroxy-3-hydroxymethyl-2-butenyl] adenine, and its derivatives were designed and synthesized as open-chain analogues of neplanocin A. The syntheses were accomplished via the coupling of adenine or pyrimidine bases to the key intermediate allylic bromide 7. The bromide 7 was prepared from epichlorohydrin in a seven step process in a 54% overall yield. The synthesized compounds were evaluated for their antiviral activity against the polio virus, HSV and HIV.

• 대한화학회지
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• 제56권1호
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• pp.68-73
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• 2012

In the present study, we have synthesized novel Isopropyl 2-(4-substitutedbenzylidene)-5-methyl-3-oxo-7-phenyl-3,7-dihydro-2H-thiazolo[3,2-a]-pyrimidine-6-carboxylate derivatives (6a-j). Elemental analysis, IR, $^1H$ NMR and mass spectral data elucidated structure of newly synthesized compounds. The newly synthesized compounds were screened for antiinflammatory and anti microbial studies. Their biological activity data of the 10 compounds indicates that two compounds posses potent anti-inflammatory and five have antimicrobial activities.

• 약학회지
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• 제32권4호
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• pp.245-250
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• 1988

Naphthoquinone derivatives have been found to be anticoagulant. In this report, several new 2-chloro-3-(N-arylamino)-naphthoquinone derivatives were synthesized in oder to develope mild anticoagulant. 2, 3-dichloro-1, 4-naphthoquinone was reacted with p-aminobenzoic acid, m-aminobenzoic acid, toluidine, m-nitroaniline, sulfanilamide, sulfathiazole, sulfaguanidine, phenetidine, 2-aminopyrimidine and 3-amino-5-methylisoxazole in EtOH or AcOH afford 2-chloro-3-(p-carboxy anilino)-naphthoquinone (1), 2-chloro-3-(m-carboxyanilino)-naphthoquinone (2),2-chloro-3-(toluidino)-naphthoquinone (3),2-chloro-3-(m-nitroanilino)-naphthoquinone (4), 2-chloro-3-(4-sulfanilanilino)-naphthoquinone (5), 2-chloro-3-(4-sulfathiazolino)-naphthoquinone (6),2-chloro-3-(4-sulfaguanidino)-naphthoquinone (7),2-chlro-3-(phenetidino)-naphthoquinone (8), 2-chloro-3-(pyrimidine-2-amino)-naphthoquinone (9) and 2-chloro-3-(5-methylisoxazole-3-amino)-naphthoquinone (10) in good yield.

• 약학회지
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• 제56권4호
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• pp.230-235
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• 2012

Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with ${\alpha}$-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.