Synthesis and anti-histamine release activity of phenyl tetrazole compounds / 药学学报
Acta Pharmaceutica Sinica
; (12): 1112-1117, 2009.
Article
em Zh
| WPRIM
| ID: wpr-344048
Biblioteca responsável:
WPRO
ABSTRACT
Ongoing effort to find novel antiasthmatic drugs led to the design and synthesis of a series of compounds bearing phenyl tetrazole group based on the SAR study. The important intermediate 3-(1H-tetrazol-5-yl) benzenamine was synthesized from m-nitroaniline via cyclization and hydrogenation. Followed by amidation, eight new target compounds were obtained. The structures of these compounds were confirmed with 1H NMR, ESI-MS and elemental analysis. Their non-specific and specific anti-histamine effects in the mast cell were determined. Compound NP03 could inhibit non-specific histamine release induced by compound 48/80 in mast cell of SD rats.
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Índice:
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Assunto principal:
Farmacologia
/
Relação Estrutura-Atividade
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Tetrazóis
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Estrutura Molecular
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Química
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Ratos Sprague-Dawley
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P-Metoxi-N-metilfenetilamina
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Antiasmáticos
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Liberação de Histamina
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Mastócitos
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2009
Tipo de documento:
Article