申请人:——
公开号:US20020032325A1
公开(公告)日:2002-03-14
Synthesis, nitric oxide synthase inhibition, and antiproliferative activity of eight structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles, specifically
4-amino-3-mercapto-triazoles;
3-R-8-aryl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazepines;
3-R-8-aryl-5,6-dihydro-1,2,4-triazolo[4,5-b]-1,3,4-thiadiazepines;
4-amino-3-(R′-mercaptyl)-5-R-(4H)-1.2.4-triazoles;
4-(R′-imino)-3-mercapto-5-(R)-4H-1.2.4-triazoles;
3-(R)-6-(R′)-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazines;
1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles; and
4-(R′-imino)-3-alkylthio-5-R-1,2,4-triazoles
are described. These variants of 4-amino-3-mercapto-1,2,4-triazoles are effective as inhibitors of nitric oxide synthase and malignant cellular proliferation.
功能化 4-氨基-3-巯基-1,2,4-三唑的八种结构变体的合成、一氧化氮合酶抑制作用和抗增殖活性,特别是
4-氨基-3-巯基三唑;
3-R-8-aryl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazepines;
3-R-8-aryl-5,6-dihydro-1,2,4-triazolo[4,5-b]-1,3,4-thiadiazepines;
4-amino-3-(R′-mercaptyl)-5-R-(4H)-1.2.4-triazoles;
4-(R′-imino)-3-mercapto-5-(R)-4H-1.2.4-triazoles;
3-(R)-6-(R′)-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazines;
1,2,4-三唑并-lsqb;3,4-b]-1,3,4-噻二唑;以及
4-(R′-imino)-3-alkylthio-5-R-1,2,4-triazoles
进行了描述。这些 4-氨基-3-巯基-1,2,4-三唑的变体可有效抑制一氧化氮合酶和恶性细胞增殖。