Hatley, RJD; Barrett, TN; Slack, RJ; Watson, ME; Baillache, DJ; Gruszka, A; Washio, Y; Rowedder, JE; Pogany, P; Pal, S; Macdonald, SJF in [Hatley, Richard J. D.; Barrett, Tim N.; Slack, Robert J.; Watson, Morag E.; Baillache, Daniel J.; Gruszka, Anna; Washio, Yoshiaki; Rowedder, James E.; Pogany, Peter; Pal, Sandeep; Macdonald, Simon J. F.] GlaxoSmithKline GSK, Med Res Ctr, Gunnels Wood Rd, Stevenage SG1 2NY, Herts, England published The Design of Potent, Selective and Drug-Like RGD alpha v beta 1 Small-Molecule Inhibitors Derived from non-RGD alpha 4 beta 1 Antagonists in 2019, Cited 39. COA of Formula: C7H4F2O2. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.
Up to 45 % of deaths in developed nations can be attributed to chronic fibroproliferative diseases, highlighting the need for effective therapies. The RGD (Arg-Gly-Asp) integrin alpha v beta 1 was recently investigated for its role in fibrotic disease, and thus warrants therapeutic targeting. Herein we describe the identification of non-RGD hit small-molecule alpha v beta 1 inhibitors. We show that alpha v beta 1 activity is embedded in a range of published alpha 4 beta 1 (VLA-4) ligands; we also demonstrate how a non-RGD integrin inhibitor (of alpha 4 beta 1 in this case) was converted into a potent non-zwitterionic RGD integrin inhibitor (of alpha v beta 1 in this case). We designed urea ligands with excellent selectivity over alpha 4 beta 1 and the other alpha v integrins (alpha v beta 3, alpha v beta 5, alpha v beta 6, alpha v beta 8). In silico docking models and density functional theory (DFT) calculations aided the discovery of the lead urea series.
COA of Formula: C7H4F2O2. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com