Fluorescent Angiotensin AT 1  Receptor Antagonists | Zendy

Giarrusso Marilena A. | Zendy; Taylor Michelle K. | Zendy; Ziogas James | Zendy; Brody Kate M. | Zendy; Macdougall Phoebe E. | Zendy; Schiesser  Carl H. | Zendy

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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.

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