Eric E. Allen

A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization

The structural optimization for binding affinity and attempted modification of agonist function of a nonpeptide ligand of the human C5a receptor is described.

Quinazolinones 1: design and synthesis of potent quinazolinone- containing AT1-selective angiotensin-II receptor antagonists

Abstract We present the design, syntheses, and in vitro biological data of a series of substituted quinazolinone containing, AT1 selective, Angiotensin II (AII) receptor antagonists. Substituents at the 6-position of the quinazolin-4(3H)-ones 3 have pronounced effects on the vitro potency related to both their electronic and lipophilic character.

Quinazolinones 2: QSAR and in vivo characterization of AT1 selective AII antagonists

Abstract The structure activity relatoionship, linear regression analysis and in vivo evaluation of a series of substituted 2-butyl-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]quinazolin-4(1H)-ones as antagonists of the AT1 receptor for angiotensin II is presented. L-159,093 (2-butyl-6-(N-isopropyl-N-methyl-carbamoyl)amino-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]quin azolin-4(1H)-one (IC50=0.1nM rabbit aorta) is shown to be a potent orally active AII antagonist in rats and rhesus.

New potent angiotensin II receptor antagonists containing phenylthiophenes and phenylfurans in place of the biphenyl moiety.

Abstract The biphenyl fragment of the potent angiotensin II receptor antagonist L-158,809 was replaced by a phenylthiophene and a phenylfuran moiety. Replacement of the tetrazole-bearing phenyl by a thiophene resulted in a small loss in binding affinity (