In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of the first potent and selective αvβ5 integrin inhibitor based on an amide-containing core, published in 2020-12-15, which mentions a compound: 1445085-77-7, mainly applied to tetrahydronaphthyridine ethylpyrrolidinebutanoic acid preparation alphaVbeta5 integrin selective inhibitor; Homology; Integrins; Selective; avb5, Recommanded Product: 1445085-77-7.
Integrins αvβ5 and αvβ3 are closely related, proangiogenic members of the wider RGD-binding integrin family. Due to their high sequence homol., the development of αvβ5-selective compounds has remained elusive to synthetic and medicinal chemists. Herein, we describe a survey of SAR around a series of amide-containing 3-aryl-succinamic acid-based RGD mimetics. This resulted in the discovery of α,α,α-trifluorotolyl I which exhibits 800 x selectivity for αvβ5vs. αvβ3 with a pyrrolidine amide linker that confers selectivity for αvβ5 by positioning a key aryl ring in the SDL of αvβ5 with good complementarity; binding in this mode is disfavored in αvβ3 due to clashes with key residues in the β3-subunit. Compound I exhibits selective inhibition by a cell adhesion assay, high passive permeability and solubility which enables potential use of this inhibitor as an αvβ5-selective in vitro tool compound
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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem