Role of the Hydrogen Bonding Heteroatom-Lys53 Interaction between the p38α Mitogen-Activated Protein (MAP) Kinase and Pyridinyl-Substituted 5-Membered Heterocyclic Ring Inhibitors

被引：24

作者：

Abu Thaher, Bassam ^{[2
]}

Koch, Pierre ^{[1
]}

Schattel, Verena ^{[1
]}

Laufer, Stefan ^{[1
]}

机构：

[1] Univ Tubingen, Inst Pharm, Dept Pharmaceut & Med Chem, D-72076 Tubingen, Germany

[2] Islam Univ Gaza, Dept Chem, Fac Sci, Gaza, Israel

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 08期

关键词：

STRUCTURAL BASIS; P38; INHIBITORS; IMIDAZOLES; MOLECULES;

D O I：

10.1021/jm801467h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the framework of Investigating the role of heteroatoms in pyridinyl-substituted 5-membered (hetero)cycles as potential p38 alpha MAP kinase inhibitor scaffolds, cyclopentene, pyrrole, furan, and imidazole analogues were synthesized and tested with respect to their ability to inhibit p38a MAP kinase. The vicinal pyridine/4-fluorophenyl pharmacophore was conserved, such as in the prototypical imidazole inhibitor SB203580. The strength of the HB interaction was calculated and compared to the biological data.

引用

页码：2613 / 2617

页数：5

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