当前位置:
X-MOL 学术
›
ChemMedChem
›
论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and in vitro Metabolic Stability of Sterically Shielded Antimycobacterial Phenylalanine Amides
ChemMedChem ( IF 3.4 ) Pub Date : 2024-02-08 , DOI: 10.1002/cmdc.202300593 Markus Lang 1 , Uday S. Ganapathy 2 , Lea Mann 1 , Rüdiger W. Seidel 1 , Richard Goddard 3 , Frank Erdmann 1 , Thomas Dick 2 , Adrian Richter 4
ChemMedChem ( IF 3.4 ) Pub Date : 2024-02-08 , DOI: 10.1002/cmdc.202300593 Markus Lang 1 , Uday S. Ganapathy 2 , Lea Mann 1 , Rüdiger W. Seidel 1 , Richard Goddard 3 , Frank Erdmann 1 , Thomas Dick 2 , Adrian Richter 4
Affiliation
Nα-aroyl-N-aryl-phenylalanine amides (AAPs) are active against numerous mycobacteria including Mycobacterium tuberculosis and Mycobacterium abscessus. As peptides, they are rapidly degraded in human and murine microsomal suspensions. Adding small substituents to the residues adjacent to the amide bonds, in particular at the anilide bond, results in increased stability.
中文翻译:
空间屏蔽抗分枝杆菌苯丙氨酸酰胺的合成及体外代谢稳定性
N α-芳酰基-N-芳基-苯丙氨酸酰胺 (AAP) 对多种分枝杆菌具有活性,包括结核分枝杆菌和脓肿分枝杆菌。作为肽,它们在人和鼠微粒体悬浮液中迅速降解。在酰胺键附近的残基上添加小的取代基,特别是在苯胺键处,可以提高稳定性。
更新日期:2024-02-08
中文翻译:
空间屏蔽抗分枝杆菌苯丙氨酸酰胺的合成及体外代谢稳定性
N α-芳酰基-N-芳基-苯丙氨酸酰胺 (AAP) 对多种分枝杆菌具有活性,包括结核分枝杆菌和脓肿分枝杆菌。作为肽,它们在人和鼠微粒体悬浮液中迅速降解。在酰胺键附近的残基上添加小的取代基,特别是在苯胺键处,可以提高稳定性。