Design and synthesis of urea and thiourea derivatives and their inhibitory activities on lipopolysaccharide-induced NO production

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 12, 2007, Pages 3317-3321

  Kim, Yoon Jung ^a   Ryu, Jae Ha ^a   Cheon, Ye Jin ^a   Lim, Hyo Jin ^a   Jeon, Raok ^a  

^a Sookmyung Women's University   (South Korea)

Author keywords

Carbazole; Inhibitor; Nitric oxide; Nitric oxide synthase; Thiourea; Urea

Indexed keywords

INDUCIBLE NITRIC OXIDE SYNTHASE; LIPOPOLYSACCHARIDE; MESSENGER RNA; NITRIC OXIDE; THIOUREA DERIVATIVE; UREA DERIVATIVE;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; MACROPHAGE ACTIVATION; MOUSE; NONHUMAN; PROTEIN EXPRESSION;

GENE EXPRESSION REGULATION, ENZYMOLOGIC; LIPOPOLYSACCHARIDES; MACROPHAGE ACTIVATION; MACROPHAGES; MODELS, CHEMICAL; NITRIC OXIDE; NITRIC OXIDE SYNTHASE TYPE II; RNA, MESSENGER; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA; UREA;

EID: 34249279170     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.005     Document Type: Article

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24. 6 cells/60-mm dish) were stimulated for 6 h with LPS (1 μg/mL) in the presence or absence of test compounds. After washing twice with phosphate-buffered saline, total RNA was isolated from cell pellet, using an RNA isolation reagent (Trizol, Invitrogen, Carlsbad, CA). Two micrograms of RNA was reverse transcribed into cDNA using reverse transcriptase and random hexamer. The PCR samples, contained in the reaction mixture, were comprised of mixture buffer, dNTP, Taq DNA polymerase (Promega, Madison, WI), and primers (sense and antisense). The sense and antisense primers for iNOS were 5′-ATGTCCGAAGCAAACATCAC-3′ and 5′-TAATGTCCAGGAAGTAGGTG-3′, respectively. The sense and antisense primers for β-actin were 5′-TGTGATGGTGGGAATGGGTCAG-3′ and 5′-TTTGATGTCACGCACGATTTCC-3′, respectively. The PCR amplification was performed under following conditions; 25 cycles of denaturation at 94 °C for 30 s, annealing at 55 °C for 30 s, and extension at 72 °C for 30 s, using thermal cycler (Gene Amp PCR system 2400, Applied Biosystems, Foster City, CA). The amplified PCR products were separated on a 2% agarose gel.
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