So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Markert, Christian; Thoma, Gebhard; Srinivas, Honnappa; Bollbuck, Birgit; Luond, Rainer M.; Miltz, Wolfgang; Walchli, Rudolf; Wolf, Romain; Hinrichs, Jurgen; Bergsdorf, Christian; Azzaoui, Kamal; Penno, Carlos A.; Klein, Kai; Wack, Nathalie; Jager, Petra; Hasler, Franziska; Beerli, Christian; Loetscher, Pius; Dawson, Janet; Wieczorek, Grazyna; Numao, Shin; Littlewood-Evans, Amanda; Rohn, Till A. researched the compound: Methyl 3-bromopropanoate( cas:3395-91-3 ).Application of 3395-91-3.They published the article 《Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase》 about this compound( cas:3395-91-3 ) in Journal of Medicinal Chemistry. Keywords: tetrazole derivative LYS 006 preparation LTA4H inhibitor antiinflammatory activity. We’ll tell you more about this compound (cas:3395-91-3).
The cytosolic metalloenzyme leukotriene A4 hydrolase (LTA4H) is the final and rate-limiting enzyme in the biosynthesis of pro-inflammatory leukotriene B4 (LTB4). Preclin. studies have validated this enzyme as an attractive drug target in chronic inflammatory diseases. Despite several attempts, no LTA4H inhibitor has reached the market, yet. Herein, we disclose the discovery and preclin. profile of LYS006 (I), a highly potent and selective LTA4H inhibitor. A focused fragment screen identified hits that could be cocrystd. with LTA4H and inspired a fragment merging. Further optimization led to chiral amino acids and ultimately to LYS006, a picomolar LTA4H inhibitor with exquisite whole blood potency and long-lasting pharmacodynamic effects. Due to its high selectivity and its ability to fully suppress LTB4 generation at low exposures in vivo, LYS006 has the potential for a best-in-class LTA4H inhibitor and is currently investigated in phase II clin. trials in inflammatory acne, hidradenitis suppurativa, ulcerative colitis, and NASH.
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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem