1999
DOI: 10.1016/s0960-894x(99)00108-0
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Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

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Cited by 31 publications
(16 citation statements)
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“…The organic layer was washed with brine (10 ml) and dried over MgSO 4 . The solvent was evaporated and the residue was chromatographed on silica gel (CHCl 3 / MeOHϭ100/1) to give 12 (119 mg, 41%): mp 269-270°C; 1…”
Section: -Amino-4-cyano-2-hydroxy-4-thiocarbamoylimidazole (10)mentioning
confidence: 99%
See 1 more Smart Citation
“…The organic layer was washed with brine (10 ml) and dried over MgSO 4 . The solvent was evaporated and the residue was chromatographed on silica gel (CHCl 3 / MeOHϭ100/1) to give 12 (119 mg, 41%): mp 269-270°C; 1…”
Section: -Amino-4-cyano-2-hydroxy-4-thiocarbamoylimidazole (10)mentioning
confidence: 99%
“…8-Hydroxypurine derivatives have been reported to have a wide range of biological activities, such as corticotropin-releasing hormone receptor antagonism, 1,2) anti-rhinovirus activity, 3) xanthine oxidase inhibiting activity 4) and excellent binding affinity to a benzodiazepine receptor. 5) Recently, we found a novel type of lead compound, 9-benzyl-8-hydroxyadenine (1), possessing potent interferon (IFN)-inducing activity and conducted substituent modifications at the 2-, 8and 9-positions of 1 to clarify the structure-activity relationships.…”
mentioning
confidence: 99%
“…Thus, in aqueous alkali compounds 3c-e were alkylated with dimethyl sulfate to form 1-alkyl(aryl)-3-methylimidazol-2-ones 4c-e. The regioselective alkylation of imidazolones is confirmed by a number of literature analogs [13][14][15] and also by 1 H NMR spectral data: the signals of the protons of the NMe group are found in the 3.03-3.23 ppm region. The thioamides 5c-f were formed by the reactions of compounds 3c-f with hydrogen sulfide.…”
mentioning
confidence: 52%
“…126 Based on the previous SAR work, the 2-bromo-4-isopropylphenyl derivatives were selected as lead compounds. Compound 25a had weak CRF binding affinity (Ki=890 nM), in contrast to its N-methyl derivative 25b, which had a high binding affinity (Ki= 5 nM).…”
Section: Purinesmentioning
confidence: 99%