2002 triazole derivatives

triazole derivativesR 0280

10 - 1191-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: Novel Synthesis via Cy-clization of N-Acyl-S-methylisothioureas with Alkylhydrazines andTheir Potent Corticotropin-Releasing Factor-1 (CRF1) ReceptorAntagonist Activities. — A series of the functionalized title triazoles(VII) is synthesized using a novel cyclization of N,N-dialkyl-N’-benzoyl-S-methylisothioureas (V) with alkylhydrazines. Compounds of this series arefound to possess good binding affinity for the CRF1 receptor (best affinity: com-pound (VIIb)). — (CHEN, CHEN; DAGNINO JR., RAYMOND; HUANG,CHARLES Q.; MCCARTHY, JAMES R.; GRIGORIADIS, DIMITRI E.;Bioorg. Med. Chem. Lett. 11 (2001) 24, 3165-3168; Neurocrine Biosci., Inc.,San Diego, CA 92121, USA; EN)

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