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Fluorescent Angiotensin AT 1 Receptor Antagonists
Author(s) -
Giarrusso Marilena A.,
Taylor Michelle K.,
Ziogas James,
Brody Kate M.,
Macdougall Phoebe E.,
Schiesser Carl H.
Publication year - 2012
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.201200064
Subject(s) - chemistry , chinese hamster ovary cell , acenaphthene , naphthalene , coumarin , fluorescence , anthracene , angiotensin ii , chinese hamster , stereochemistry , angiotensin receptor , receptor , pharmacology , combinatorial chemistry , in vitro , biochemistry , organic chemistry , medicine , physics , quantum mechanics
Fluorescent selective angiotensin AT 1 receptor antagonists (sartans) that contain naphthalene ( 6 , 7 , 10 , and 11 ), anthracene ( 12 and 14 ), acenaphthene ( 13 and 15 ), and coumarin ( 8 and 9 ) substituents have been prepared and their preliminary pharmacology evaluated in Chinese hamster ovary (CHO) cell based assays. Compounds 6 – 15 proved to be effective sartans with p K B estimates in the range of 6.7–10.5; their potential as cellular imaging agents is also discussed.