- Synthesis of highly potent and selective hetaryl ureas as integrin αVβ3-receptor antagonists
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Solid-phase synthesis and SAR of integrin αVβ3-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC50 values towards αVβ3 in the nanomolar range and high selectivity versus related integrins like αIIbβ3. For selected examples efficacy in functional cellular assays is demonstrated.
- Lange, Udo E.W.,Backfisch, Gisela,Delzer, Juergen,Geneste, Herve,Graef, Claudia,Hornberger, Wilfried,Kling, Andreas,Lauterbach, Arnulf,Subkowski, Thomas,Zechel, Christian
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p. 1379 - 1382
(2007/10/03)
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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