Trypsin inhibitors for the treatment of pancreatitis. Issue 17 (1st September 2016)

• Record Type: Journal Article
• Authors: Brandl, Trixi; Simic, Oliver; Skaanderup, Philip R.; Namoto, Kenji; Berst, Frederic; Ehrhardt, Claus; Schiering, Nikolaus; Mueller, Irene; Woelcke, Julian
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 17(2016)
• Page Start: 4340
• Page End: 4344
• Publication Date: 2016-09-01
• Subjects: YBZBHUMSHGXQNF-FIBWVYCGSA-N -- AYVQDWAWTUYBGU-RVUATISTSA-N -- PZBPHXPZLFDRAP-REWPJTCUSA-N; Trypsin inhibitor -- Pancreatitis -- hERG inhibition -- X-ray crystal structure; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.07.029
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Proline-based trypsin inhibitors occupying the S1–S2–S1′ region were identified by an HTS screening campaign. It was discovered that truncation of the P1′ moiety and appropriate extension into the S4 region led to highly potent trypsin inhibitors with excellent selectivity against related serine proteases and a favorable hERG profile.