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Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.33 no.6, 2010년, pp.821 - 830   SCIE 피인용횟수: 1
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Synthesis and Antimicrobial and Nitric Oxide Synthase Inhibitory Activities of Novel Isothiourea Derivatives

Kazimierczuk, Zygmunt    (Department of Experimental Pharmacology, Polish Academy of Sciences   ); Chalimoniuk, Malgorzata    (Department of Cellular Signaling, Mossakowski Medical Research Center, Polish Academy of Sciences   ); Laudy, Agnieszka Ewa    (Department of Pharmaceutical Microbiology, Medical University of Warsaw   ); Moo-Puc, Rosa    (Unidad Interinstitucional de Investigacion Clinica y Epidemiologica, Facultad de Medicina, UADY/Instituto Mexicano del Seguro Social   ); Cedillo-Rivera, Roberto    (Unidad Interinstitucional de Investigacion Clinica y Epidemiologica, Facultad de Medicina, UADY/Instituto Mexicano del Seguro Social   ); Starosciak, Bohdan Jerzy    (Department of Pharmaceutical Microbiology, Medical University of Warsaw   ); Chrapusta, Stanislaw J.    (Department of Experimental Pharmacology, Polish Academy of Sciences  );
  • 초록

    The reaction of substituted benzylhalides, or of halomethyl derivatives of thiophene or furane, with thiourea or its derivatives yielded the respective isothioureas as hydrohalide salts. The products (a total of 17, including 16 novel compounds) were tested for activity against five Gram-positive and nine Gram-negative bacterial strains, six yeast species and two protozoan species. The most active against Gram-positive bacteria were S-(2,4-dinitrobenzyl)isothiourea hydrochloride (MIC range for four out of five strains tested: $12.5-25\;{\mu}g$ /mL) and S-(2,3,4,5,6-pentabromobenzyl)isothiourea hydrobromide (MIC range: $12.5-50\;{\mu}g$ /mL). The lowest MICs of novel isothioureas for yeast and Gram-negative bacteria ranged between 50 and $100\;{\mu}g$ /mL. Nine novel isothioureas showed appreciable genotoxicity in the Bacillus subtilis 'rec-assay' test, the most potent being S-2-(5-nitrofuran-2-ylmethyl)isothiourea and S-(2-nitrobenzyl) isothiourea. At $10\;{\mu}M$ concentration, S-(3,4-dichlorobenzyl)isothiourea hydrochloride and S-(2,3,4,5,6-pentabromobenzyl)isothiourea hydrobromide inhibited $Ca^{2+}$ /calmodulin-dependent (non-inducible) nitric oxide synthase activity in normal rat brain homogenates stronger (p


  • 주제어

    Isothiourea derivative .   Synthesis .   Antibacterial activity .   Antifungal activity .   Anti-protozoal activity .   Nitric oxide synthase.  

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  • 이 논문을 인용한 문헌 (1)

    1. Cho, Seung-Sik ; Hong, Joon-Hee ; Chae, Jung-Il ; Shim, Jung-Hyun ; Na, Chong-Sam ; Yoo, Jin-Cheol 2014. "Biological Evaluation of Nargenicin and Its Derivatives as Antimicrobial Anti-inflammatory Agents" 韓國有機農業學會誌 = Korean journal of organic agriculture, 22(3): 469~481     

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