2000
DOI: 10.1021/jm991096e
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1,2,4-Triazolo[4,3-a]quinoxalin-1-one:  A Versatile Tool for the Synthesis of Potent and Selective Adenosine Receptor Antagonists

Abstract: 4-Amino-6-benzylamino-1,2-dihydro-2-phenyl-1,2,4-triazolo[4, 3-a]quinoxalin-1-one (1) has been found to be an A(2A) versus A(1) selective antagonist (Colotta et al. Arch. Pharm. Pharm. Med. Chem. 1999, 332, 39-41). In this paper some novel triazoloquinoxalin-1-ones 4-25 bearing different substituents on the 2-phenyl and/or 4-amino moiety of the parent 4-amino-1, 2-dihydro-2-phenyl-1,2,4-triazolo[4,3-a]quinoxalin-1-one (3) have been synthesized and tested in radioligand binding assays at bovine A(1) and A(2A) a… Show more

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Cited by 69 publications
(125 citation statements)
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“…ARTICLE AR subtype of all of the compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) reported in this work.…”
Section: Journal Of Medicinal Chemistrymentioning
confidence: 98%
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“…ARTICLE AR subtype of all of the compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) reported in this work.…”
Section: Journal Of Medicinal Chemistrymentioning
confidence: 98%
“…The newly 4-substituted phthalazine derivatives 2-20 and the parent 1 (Table 1) Moreover, some selected compounds (12)(13)(14)18, and 19) were tested at the hA 2B subtype by measuring their inhibitory effect on NECA-stimulated cyclic adenosine monophosphate (cAMP) levels in CHO cells stably transfected with the hA 2B AR ( Table 2). To evaluate their hA 3 AR antagonistic effect, the same compounds were tested for their ability to counteract the NECAmediated inhibition of cAMP accumulation in CHO cells stably expressing hA 3 AR ( Table 2).…”
Section: ' Pharmacologymentioning
confidence: 99%
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“…Continuing our studies of this class of AR antagonists, in the present paper we have focused our attention on A 1 selective ligands. Therefore, taking the potent and selective A 1 antagonists 2-phenyl-4-cycloalkylamino derivatives A and B [16] as lead compounds (Figure 1), new 4-cycloalkylamino-2-phenyl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives (1-11) were prepared and tested at bA 1 , bA 2A and hA 3 ARs. Compounds 1-11 were designed to evaluate the influence on A 1 affinity and selectivity of some simple substituents (chloro, nitro or amino groups) at different positions of the benzofused moiety.…”
mentioning
confidence: 99%