143617-90-7Relevant articles and documents
Structure-Activity Relationships of Benzamides and Isoindolines Designed as SARS-CoV Protease Inhibitors Effective against SARS-CoV-2
Welker, Armin,Kersten, Christian,Müller, Christin,Madhugiri, Ramakanth,Zimmer, Collin,Müller, Patrick,Zimmermann, Robert,Hammerschmidt, Stefan,Maus, Hannah,Ziebuhr, John,Sotriffer, Christoph,Schirmeister, Tanja
supporting information, p. 340 - 354 (2020/10/19)
Inhibition of coronavirus (CoV)-encoded papain-like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure-activity relationships (SAR) of the noncovalent active-site directed inhibitor (R)-5-amino-2-methyl-N-(1-(naphthalen-1-yl)ethyl) benzamide (2 b), which is known to bind into the S3 and S4 pockets of the SARS-CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS-CoV-2 replication in cell culture suggesting that, due to the high structural similarities of the target proteases, inhibitors identified against SARS-CoV PLpro are valuable starting points for the development of new pan-coronaviral inhibitors.
Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer
Scott, David A.,Aquila, Brian M.,Bebernitz, Geraldine A.,Cook, Donald J.,Dakin, Les A.,Deegan, Tracy L.,Hattersley, Maureen M.,Ioannidis, Stephanos,Lyne, Paul D.,Omer, Charles A.,Ye, Minwei,Zheng, XiaoLan
scheme or table, p. 4794 - 4797 (2009/05/30)
The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides are reported, along with the pharmacokinetic properties and in vivo activity of selected examples.
Analogs of Ac-CCK-7 Incorporating Dipeptide Mimics in Place of Met28-Gly29
Tilley, Jefferson W.,Danho, Waleed,Shiuey, Shian-Jun,Kulesha, Irina,Swistok, Joseph,et al.
, p. 3774 - 3783 (2007/10/02)
A series of analogs of Ac-CCK-7 28-Gly29-Trp-Met-Asp-Phe-NH2, (1)> were prepared in which The Met28-Gly29 dipeptide was replaced by ω-aminoalkanoic acids.Compounds were assessed in binding assay