Electric Literature of 10288-72-9, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 10288-72-9, 6-Hydroxy-1,4-benzodioxane, introducing its new discovery.
Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: Discovery of TR-14035, a dual alpha4beta7/alpha4beta1 integrin antagonist
alpha4beta1 and alpha4beta7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions provides a strong rationale to target integrins for drug development. Important advances have been made in identifying potent and selective candidates, peptides and peptidomimetics, for further development. Herein, we report the discovery of a series of novel N-benzoyl-L-biphenylalanine derivatives that are potent inhibitors of alpha4 integrins. The potency of the initial lead compound (1: IC50 alpha4beta7/alpha4beta1 =5/33 muM) was optimized via sequential manipulation of substituents to generate low nM, orally bioavailable dual alpha4beta1/alpha4beta7 antagonists. The SAR also led to the identification of several subnanomolar antagonists (134, 142, and 143). Compound 81 (TR-14035; IC50 alpha4beta7/alpha4beta1 =7/87 nM) has completed Phase I studies in Europe. The synthesis, SAR and biological evaluation of these compounds are described.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 10288-72-9. In my other articles, you can also check out more blogs about 10288-72-9
Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem