• Bulletin of the Korean Chemical Society
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• v.31 no.1
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• pp.27-30
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• 2010

A series of thioureas were synthesized as inhibitors of NO production in lipopolysaccharide-activated macrophages. We investigated the effect of lipophilic moiety and N-substituents of the thioureas on the activity. Phenoxazine and carbazole-containing derivatives revealed higher activity than indole-containing thioureas. The appropriate spacer between lipophilic tail and thiourea head and methyl substituent at N3 position of thiourea brought beneficial effect on the inhibition of NO production. Among prepared compounds, phenoxazine-containing derivative 2a was the most potent with $2.32 {\mu}M$ of $IC_{50}$ value. RT-PCR analysis suggested that the prepared thioureas inhibited NO production through the suppression of iNOS mRNA expression.

• Bulletin of the Korean Chemical Society
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• v.22 no.11
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• pp.1270-1272
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• 2001

• Bulletin of the Korean Chemical Society
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• v.28 no.12
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• pp.2552-2554
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• 2007

• Bulletin of the Korean Chemical Society
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• v.21 no.9
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• pp.919-922
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• 2000

The cyclization reaction of N-(2-hydroxyethyl)-N'-phenylthioureas 2 containingambident nucleophile was ex-amined in the combination of a variety ofbases and p-toluenesulfonyl chloride (TsCl).N-(2-Hydroxyeth-yl) thioureas 2 were readily obtained in high yields from the reaction of the corresponding 1,2-aminoalcohols with phenyl isothiocyanate, avoiding the need for O-protection.The use of a one-pot reaction (NaOH/TsCl) was found to be most effective in producing the requisite 2-phenylaminothiazolines (S-cyclization) 3 in the case ofthioureas 2a-2e derived from N-unsubstituted aminoalcohols,while in the thioureas 2f and 2g prepared from N-substituted aminoalcohols the combination of Et3N and TsCl led to the S-cyclization products.

• Bulletin of the Korean Chemical Society
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• v.24 no.7
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• pp.1038-1040
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• 2003

• Bulletin of the Korean Chemical Society
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• v.15 no.7
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• pp.602-604
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• 1994

• Bulletin of the Korean Chemical Society
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• v.22 no.7
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• pp.761-764
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• 2001

• Archives of Pharmacal Research
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• v.16 no.3
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• pp.186-190
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• 1993

Two series of substituted sulforrythiazolidin-4-ones and sulforrylthiazolines have been synthesized and examined for their antidiabetic and biological aticity.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.173.2-173.2
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• 2003

Vanilloid receptor I (VR1) is a nonselective cation ion channel placed in the plasma membrane of peripheral sensory neurons that is potential target for analgesia A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG. Their structure-activity relationship in reveals that not only the two oxygens and amide hydrogen of sulfonamido group but also the optimal size of methyl in methanesulfonamido group play an integral role for the antagonistic activity on vanilloid receptor.

• YAKHAK HOEJI
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• v.30 no.5
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• pp.214-219
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• 1986

A gas chromatographic procedure is described for the quantitative analysis of ephedrine hydrochloride, pseudoephediiiie hydrochloride and norephedrine hydrochloride in pharmaceutical preparations. The procedure was based upon the determination of thioureas formed from amines and phenylisothiocyanate. The recoveries of ephedrine, pseudoephedrine and norephedrine from pharmaceutical preparations were 100.7(S.E. 0.9), 99.5(0.8), 99.1(0.8) and 99.1%(O.9), respectively. The high accuracy and precision of this assay were inherent in the flame photometric detectors normally used in gas chromatography.