• Archives of Pharmacal Research
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• v.17 no.4
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• pp.223-225
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• 1994

The titled compounds have been synthesized by the oxidative cyclization of N-ethyl-N'-aryl-thioureas and screened for their anti-inflammatory and analogesic activities. Some of the compounds exhibit significant activities.

• Bulletin of the Korean Chemical Society
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• v.13 no.5
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• pp.526-528
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• 1992

1-Aminothiohydantoin derivatives were prepared in good yields by the reaction of alkyl or arylisothiocyanates with ethyl hydrazinoacetate hydrochloride in presence of triethylamine. The intermediates, N-amino-N-ethoxycarbonylmethyl-N'-aralkylthioure as, which were formed during the reaction and could be transformed into the appropriate 1-aminothiohydantoins, were isolated and characterized.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.356.2-356.2
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• 2002

The structure of 1-phenyl-2-substituted thiourea derivatives have been studied and optimized for their cytotoxic activity. The three dimensional quantitative structure activity relationship (3D-QSAR) was investigated using comparative molecular field analysis (CoMFA). The result suggested that electrostatic and steric factors of 2-alkylureido-1-phenyl propanol derivatives were correlated well with cytotoxic activity. (omitted)

• Bulletin of the Korean Chemical Society
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• v.31 no.6
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• pp.1469-1473
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• 2010

Influences of alrylamino (R) substituents on the herbicidal activity ($pI_{50}$) of 1-(4-chloro-2-fluoro-5-propargyloxypheny)-3-(R)-thiourea analogues (1 ~ 35) against the barnyard grass (Echinochloa crusgalli) in the pre-emergence step were discussed quantitatively using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) as the three dimensional quantitative structure-activity relationship (3D-QSAR) method. The statistically most satisfactory CoMFA models for the herbicidal activity against the barnyard grass had the better predictability ($r^2{_{cv.}}$) and correlativity ($r^2{_{ncv.}}$) than those of CoMSIA models. The optimized CoMFA model 1($r^2{_{cv.}}$ = 0.531 & $r^2{_{ncv.}}$ = 0.931) with the sensitivity to the perturbation (${d_q}^{2'}{dr^2}_{yy'}$ = 1.081) and the prediction ($q^2$ = 0.475) produced by a progressive scrambling analyses were not dependent on chance correlation. And statistical qualities with the atom based fit alignment (AF) were slightly higher than those of the field fit alignment (FF). According to the optimized CoMFA model 1, the contribution ratio (%) of the steric field (76.9%) on the herbicidal activity of the Thioureas was three-fold higher than that of the electrostatic field (20.1%) and the hydrophobic field (3.0%) had the least influence. A steric favor group is on the vicinity of the nitrogen atom in alrylamino (R) substituent, and a steric disfavor group is on the outer side of alrylamino (R) substituent. Thus, as the size of alrylamino (R) substituent increases, so does the herbicidal activity of the substituent.

• YAKHAK HOEJI
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• v.51 no.4
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• pp.246-252
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• 2007

Several ureas and thioureas were designed and synthesized and their inhibitory activities of NO production in lipopolysaccharide-activated macrophages were evaluated. Among these compounds, indole-containing thiourea 6e was the most potent showing 17.4 ${\mu}M$ of $IC_{50}$ value.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.339.3-340
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• 2002

Capsaicin is hot taste ingredient of chili pepper and was isolated in 1876 and in 1919 its structure is sympathized compound. induces pain and when persistently dosed. the fact will bring insensible condition to other chemical and mechanical thermal stimulation by incapacitating sensory neuron is known. The analgesic effect by desensitization of such capsaicin is differ from the mechanism by analgesic action by opiate receptor of the existing analgesia or by prostaglandin mediation and the efficacy was known as similar with morphine. (omitted)

• Journal of the Korean Chemical Society
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• v.47 no.3
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• pp.237-240
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• 2003

A synthetic method for the title compounds (2a-o) was carried out. The title compounds (2a-o)were prepared by the condensation of various thioureas and maleic anhydride. Anti-inflammatory activities in vivo were evaluated and compared with standard drug diclofenac sodium. Some compounds showed moderate activity. The structures of all the new compounds were established on the basis of $^1H$ NMR and IR spectral data.

• Journal of the Korean Chemical Society
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• v.52 no.1
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• pp.30-35
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• 2008

purpose of the study was to synthesize new series of 5-cyano substituted pyrimidine analogues with different substitutions at N1 and 6 positions and to evaluate them for antibacterial and antifungal activities. The desired compounds were synthesized by tertiary condensation of ethylcyanoacetate, substituted thioureas and suitable aldehyde in presence of potassium carbonate using MORE technique. The antibacterial and antifungal activities were evaluated by cup plate method in the concentration of 25 mg. The zone of inhibition was measured in mm. All the compounds have shown significant antibacterial and antifungal activities. The maximum activity was shown by P1 and P5 against S.aureus and E.coli respectively, while P6 has shown significant activity against all types of microorganisms. The compound P8 has been found to be significantly effective against C. albicans. Norfloxacin and griseofulvin were used as standards to compare the activites of synthesized compounds. It is concluded that analogues containing p-hydroxy, p-methoxy substituted phenyl moiety at 6 position have been found to be more potent against gram-positive microorganisms, while analogues lacking these substituents on phenyl moiety possessed gram-negative activity. The compounds having p-dimethylamino substituent on phenyl moiety at 6 positions have shown moderate activity. Further, only fluorine containing analogue at N1 position was found to possess appreciable antifungal activity. This suggests that electron donating substituent on aryl moiety as well as electron withdrawing substituent at N1 plays important role in determining potency of the compounds.

• The Korean Journal of Pesticide Science
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• v.5 no.2
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• pp.13-17
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• 2001

A synthesis of new 2-phenylimino-1,3-thiazolines 2 for the purpose of development of new agrochemical fuugicide was described. Reaction of chlorine with diketene followed by treatment of benzylamine without isolation of intermediate 8a gave ${\gamma}-chloro-{\beta}-keto$ benzylamide 10a. Thioureas 4 obtained from the reaction of methyl isothiocyanate with aniline derivatives were subjected to 10a in acetone solution to afford the corresponding 2-phenylimino-1,3-thiazoline hydrochloric acid salts 2 through unisolable inltermediates 11 and 12. The plausible reaction mechanism including nucleophilic attack of sulfur assisted neighboring nitrogen lone pair electron on phenyl of thiourea 4 was discussed.

• The Korean Journal of Pesticide Science
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• v.10 no.2
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• pp.149-152
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• 2006

Construction of focused library of 2-benzylimino-1,3-thiazolines 7 through molecular modification of 3-alkyl-2-phenylimino-1,3-thiazolines 1 which showed selective fungicidal activity against rice blast and their fungitoxic activity against 6 kinds of typical plant diseases was described. Fifty four compounds of focused library of 2-benzylimino-1,3-thiazolines 7 were synthesized from the reaction of the corresponding $\gamma$-chloroacetoacetanilides 6 with N-benzyl thioureas 5 by parallel synthetic methodology. As results of fungicidal screening against the typical plant diseases, twenty eight kinds of 7 at 100 ${\mu}g$ $mL^{-1}$ showed the control value over 50% against tomato late blight.