Abstract:
:A series of new 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as A(2B)-AdoR antagonists have been synthesized and evaluated for their binding affinities for the A(2B), A(1), A(2A), and A(3)-AdoRs. 8-(1-((3-phenyl-1,2,4-oxadiazol-5-yl)methyl)-1H-pyrazol-4-yl)-1,3-dipropyl-1H-purine-2,6(3H,7H)-dione (4) displayed high affinity (K(i)=1 nM) and selectivity for the A(2B)-AdoR versus A(1), A(2A), and A(3)-AdoRs (A(1)/A(2B), A(2A)/A(2B), and A(3)/A(2B) selectivity ratios of 370, 1100, and 480, respectively). The synthesis and SAR of this novel class of compounds are presented herein.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Elzein E,Kalla R,Li X,Perry T,Parkhill E,Palle V,Varkhedkar V,Gimbel A,Zeng D,Lustig D,Leung K,Zablocki Jdoi
10.1016/j.bmcl.2005.10.002subject
Has Abstractpub_date
2006-01-15 00:00:00pages
302-6issue
2eissn
0960-894Xissn
1464-3405pii
S0960-894X(05)01268-0journal_volume
16pub_type
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