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2005
Pyrimidine derivatives
R 0510
Amino-Substituted Heterocycles as Isosteres of trans-Cinnamides: Design and
of Heterocyclic Biaryl Sulfides as Potent Antagonists of LFA-1/ICAM-1
18- 145 Synthesis
Binding. — The influence of the structure of heterocyclic substituent as well as phenylthio substituent on the biological activity is tested in detail. It is shown that the pyrimidinyl (I) and pyridinyl derivatives (II) possess good LFA-1/CAM-1 antagonistic
activity while five-membered rings are less suitable substituents. Thus, the 2-amino-4-phenylpyridine and 4-amino-6-phenylpyrimidine structures represent suitable
isosteres to trans-cinnamide moiety in the parent p-arylthio-trans-cinnamides. —
(WANG*, G. T.; WANG, S.; GENTLES, R.; SOWIN, T.; LEITZA, S.; REILLY, E. B.;
VON GELDERN, T. W.; Bioorg. Med. Chem. Lett. 15 (2005) 1, 195-201; Abbott
Lab., Global Pharm. R&D, Abbott Park, IL 60064, USA; Eng.) — Mischke
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