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A series of novel 7-amino-5-oxo-2-substituted-aryl/heteroaryl-5,8-dihydro[1,2,4]triazolo[1,5-a]-pyridine-6-carbonitriles (4a-4t) was synthesized, characterized and evaluated for their binding affinity and selectivity towards hA , hA , hA and hA adenosine receptors (ARs). Compound 4a with a phenyl ring at 2-position of the triazolo moiety of the scaffold showed high affinity and selectivity for hA AR (K hA = 0.076 μM, hA = 25.6 μM and hA > 100 μM). Introduction of various electron donating and withdrawing groups at different positions of the phenyl ring resulted in drastic reduction in affinity and selectivity towards all the ARs, except compound 4b with a phenol group at 2-position. Interestingly, the replacement of the phenyl ring with a smaller heterocyclic thiophene ring (π excessive system) resulted in further improvement of affinity for hA AR of compound 4t (K hA = 0.051 μM, hA = 9.01 μM and hA > 13.9 μM) while retaining the significant selectivity against all other AR subtypes similar to compound 4a. The encouraging results for compounds 4a and 4t indicate that substitution at 2-position of the scaffold with π-excessive systems other than thiophene may lead to even more potent and selective hA AR antagonists. This article is protected by copyright. All rights reserved.
This article was published in the following journal.
Name: Chemical biology & drug design
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Organic chemicals where aryl or alkyl groups are joined by two nitrogen atoms through a double bond (R-N=N-R'; R and R' may be either aryl or alkyl). They may be used as DYES.
A group of transfer RNAs which are specific for carrying each one of the 20 amino acids to the ribosome in preparation for protein synthesis.
An enzyme that catalyzes the synthesis of pyroglutamate from a gamma-glutamyl-amino acid, also releasing the free amino acid. The enzyme acts on derivatives of glutamate, 2-aminobutyrate, alanine and glycine. The enzyme has been proposed to have a role in a gamma-glutamyl cycle for amino acid transport into cells in the intestines. EC 220.127.116.11.
An enzyme which catalyzes the hydrolysis of an aryl-dialkyl phosphate to form dialkyl phosphate and an aryl alcohol. It can hydrolyze a broad spectrum of organophosphate substrates and a number of aromatic carboxylic acid esters. It may also mediate an enzymatic protection of LOW DENSITY LIPOPROTEINS against oxidative modification and the consequent series of events leading to ATHEROMA formation. The enzyme was previously regarded to be identical with Arylesterase (EC 18.104.22.168).
Aryl hydrocarbon receptor nuclear translocator is a basic HELIX-LOOP-HELIX MOTIF containing protein that forms a complex with DIOXIN RECEPTOR. The complex binds xenobiotic regulatory elements and activates transcription of a variety of genes including UDP GLUCURONOSYLTRANSFERASE. AhR nuclear translocator is also a subunit of HYPOXIA-INDUCIBLE FACTOR 1.