4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity |
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Authors: | Felicia Phei Lin Lim Anton V Dolzhenko |
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Institution: | 1. School of Pharmacy, Curtin Health Innovation Research Institute, Curtin University, GPO Box U1987, Perth, Western Australia 6845, Australia;2. School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan 47500, Malaysia |
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Abstract: | The trichloromethyl moiety was successfully employed as a leaving group in nucleophilic substitutions with various amines for the synthesis of 4-amino-substituted pyrazolo1,5-a]1,3,5]triazin-2-amines. The key precursor for this reaction, 4-trichloromethylpyrazolo1,5-a]1,3,5]triazin-2-amine, was prepared via the solvent-dependent condensation of 5-guanidino-3-phenylpyrazole with trichloroacetonitrile. In a broad biological activity screening, some of the prepared compounds were identified as CGRP receptor antagonists. |
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Keywords: | IAWSPJGLRHNCEI-UHFFFAOYSA-N PYSGDQZZNYXTRQ-UHFFFAOYSA-N WZJVTFCFIFIHJS-UHFFFAOYSA-N WICDHIIRVNIUEM-UHFFFAOYSA-N MBDXKRDXVFXNOK-UHFFFAOYSA-N JBZOYQRTLOLVDT-UHFFFAOYSA-N BRHIQUCSJXGEAT-UHFFFAOYSA-N LAQRBTFZIOULDX-UHFFFAOYSA-N QXHHPHVDYQYETA-UHFFFAOYSA-N HQPAJLMIOWMEJA-UHFFFAOYSA-N GMBRLOYDXGNEHQ-UHFFFAOYSA-N ACDVHCPSJBNJKU-UHFFFAOYSA-N UQVXRMFPSYXETN-UHFFFAOYSA-N BEMZPDJICQKHEP-UHFFFAOYSA-N YFQLFZIXJKOOIF-UHFFFAOYSA-N WSIJUPUWACMKBX-UHFFFAOYSA-N HGLDBRRLRQAXAV-UHFFFAOYSA-N ARUIXIORASZCAF-UHFFFAOYSA-N NBIIAHSTPYATPV-UHFFFAOYSA-N |
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