3-苄基-1-甲基异硫脲和1-甲基-3-苯基异硫脲作为诱导型一氧化氮合酶潜在抑制剂的合成及生物学评价
Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS.
作者信息
Paesano Nicola, Marzocco Stefania, Vicidomini Caterina, Saturnino Carmela, Autore Giuseppina, De Martino Giovanni, Sbardella Gianluca
机构信息
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy.
出版信息
Bioorg Med Chem Lett. 2005 Feb 1;15(3):539-43. doi: 10.1016/j.bmcl.2004.11.047.
PMID:15664809
Abstract
Novel benzyl- and phenyl-isothioureidic derivatives have been synthesised and evaluated as inhibitors of nitric oxide synthesis, induced in lipopolysaccharide (LPS)-activated J774.A1 macrophage cell line. The most potent iNOS inhibitor resulting was 1-methyl-3-phenyl-S-methyl isothiourea 5l.
摘要
新型苄基和苯基异硫脲衍生物已被合成，并作为脂多糖（LPS）激活的J774.A1巨噬细胞系中诱导的一氧化氮合成抑制剂进行了评估。产生的最有效的诱导型一氧化氮合酶（iNOS）抑制剂是1-甲基-3-苯基-S-甲基异硫脲5l。
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