Literature

Abstract

A highly potent AMP deaminase (AMPDA) inhibitor series was discovered by replacing the N3 substitutents of the two lead AMPDA inhibitor series with a conformationally restricted group. The most potent compound, 3-[2-(3-carboxy-4-bromo-5,6,7,8-tetrahydronaphthyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (24b), represents a 10- to 250-fold enhancement in AMPDA inhibitory potency without loss in the enzyme specificity. The potency of the inhibitor 24b (AMPDA K(i) = 0.002 microM) is 10(5)-fold lower than the Km for the substrate AMP. It represents the most potent nonnucleotide AMPDA inhibitor known.

DOI： 10.1021/jm000355t

AMP Deaminase Inhibitors. 5. Design, Synthesis, and SAR of a Highly Potent Inhibitor Series

Journal of Medicinal Chemistry 2001.0

Structure-Based de novo design of non-nucleoside adenosine deaminase inhibitors

Bioorganic & Medicinal Chemistry Letters 2003.0

Adecypenol, a unique adenosine deaminase inhibitor containing homopurine and cyclopentene rings. Taxonomy, production and enzyme inhibition.

The Journal of Antibiotics 1986.0

Development of novel N -3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists

Bioorganic & Medicinal Chemistry 2017.0

cAMP-dependent phosphodiesterase inhibition and SAR studies on novel 6,8-disubstituted 2-phenyl-3-(substituted benzothiazole-2-yl)-4[3H]-quinazolinone

Medicinal Chemistry Research 2009.0

Adenosine deaminase inhibitors. Synthesis of deaza analogs of erythro-9-(2-hydroxy-3-nonyl) adenine