Development of inhibitors based on the molecular structure and mechanism of substrate hydrolysis by metallo-beta-lactamases

Research Project

Project/Area Number	26460147
Research Category	Grant-in-Aid for Scientific Research (C)
Allocation Type	Multi-year Fund
Section	一般
Research Field	Drug development chemistry
Research Institution	Kinjo Gakuin University (2015-2016) Kumamoto University (2014)
Principal Investigator	KUROSAKI Hiromasa 金城学院大学, 薬学部, 教授 (70234599)
Co-Investigator(Kenkyū-buntansha)	藤田美歌子熊本大学, 薬学部附属創薬研究センター, 准教授 (00322256)
Project Period (FY)	2014-04-01 – 2017-03-31
Project Status	Completed (Fiscal Year 2016)
Budget Amount *help	¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000) Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000) Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000) Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords	感染症 / ラクタマーゼ / 抗生物質 / Ｘ線結晶構造解析 / 阻害剤 / ラクタム剤 / X線結晶構造解析
Outline of Final Research Achievements	The emergence and rapid spread of carbapenem-resistant pathogens producing metallo-beta-lactamases such as IMP-1 and NDM-1 are of great concern in the clinical setting worldwide. There are no clinically available inhibitors for metallo-beta-lactamases at present. In order to develop the inhibitors for metallo-beta-lactamases, we synthesized seven novel compounds based on the X-crystal structure of metallo-beta-lactamase (IMP-1).

Report

(4 results)