Bridged α-helix mimetic small molecules. Issue 88 (21st October 2019)

• Record Type: Journal Article
• Authors: Lee, Yeongju; Im, Haeri; Das, Sanket; Oh, Misook; Lee, Ji Hoon; Ham, Sihyun; Lim, Hyun-Suk
• Is Part Of: Chemical communications. Volume 55:Issue 88(2019)
• Page Start: 13311
• Page End: 13314
• Publication Date: 2019-10-21
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c9cc03627j
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Herein, we report a strategy for generating conformationally restricted α-helix mimetic small molecules by introducing covalent bridges that limit rotation about the central axis of α-helix mimetics. Abstract : Herein, we report a strategy for generating conformationally restricted α-helix mimetic small molecules by introducing covalent bridges that limit rotation about the central axis of α-helix mimetics. We demonstrate that the bridged α-helix mimetics have enhanced binding affinity and specificity to the target protein due to the restricted conformation as well as extra interaction of the bridge with the protein surface.