10 -（2 - 苯并恶唑甲酰基）- 5,10 - 二氮杂无环 - 5,6,7,8 - 四氢叶酸：一种潜在的甘氨酰胺核糖核苷酸转甲酰酶和氨基咪唑甲酰胺核糖核苷酸转甲酰酶抑制剂。
10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.
作者信息
Marsilje Thomas H, Hedrick Michael P, Desharnais Joel, Capps Kevin, Tavassoli Ali, Zhang Yan, Wilson Ian A, Benkovic Stephen J, Boger Dale L
机构信息
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
出版信息
Bioorg Med Chem. 2003 Oct 1;11(20):4503-9. doi: 10.1016/s0968-0896(03)00457-7.
The design and synthesis of 10-(2-benzoxazolcarbonyl)-DDACTHF (1) as an inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Ketone 1 and the corresponding alcohol 13 were evaluated for inhibition of GAR Tfase and AICAR Tfase and the former was found to be a potent inhibitor of recombinant human (rh) GAR Tfase (Ki=600 nM).
报道了10-(2-苯并恶唑甲酰基)-DDACTHF(1)作为甘氨酰胺核糖核苷酸转甲酰酶(GAR Tfase)和氨基咪唑甲酰胺转甲酰酶(AICAR Tfase)抑制剂的设计与合成。对酮1和相应的醇13进行了GAR Tfase和AICAR Tfase抑制活性评价，发现前者是重组人(rh)GAR Tfase的有效抑制剂(Ki=600 nM)。
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