Abstract：
:During the course of our efforts toward the discovery of human histamine H4 antagonists from a series of 2-aminiopyrimidines, it was noted that a 6-trifluoromethyl group dramatically reduced affinity of the series toward the histamine H4 receptor. This observation was further investigated by synthesizing a series of ligands that varied in pKa of the pyrimidine derived H4 ligands by over five orders of magnitude and the effect on histamine H4 affinity. This trend was then extended to the discovery of C-linked piperidinyl-2-amino pyridines as histamine H4 receptor antagonists.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Savall BM,Meduna SP,Venable J,Wei J,Smith RC,Hack MD,Thurmond RL,McGovern P,Edwards JPdoi
10.1016/j.bmcl.2014.10.013subject
Has Abstractpub_date
2014-12-01 00:00:00pages
5489-92issue
23eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)01058-0journal_volume
24pub_type
杂志文章abstract：:Betulinic acid has been modified at C-3, C-20, and C-28 positions and the toxicity of the derivatives has been evaluated against cultured human melanoma (MEL-2) and human epidermoid carcinoma of the mouth (KB) cell lines. This preliminary investigation demonstrates that simple modifications of the parent structure of ...
journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
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