Synthesis and anti-histamine release activity of phenyl tetrazole compounds / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1112-1117, 2009.
Article
in Chinese
| WPRIM
| ID: wpr-344048
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Tetrazoles
/
Molecular Structure
/
Chemistry
/
Rats, Sprague-Dawley
/
P-Methoxy-N-methylphenethylamine
/
Anti-Asthmatic Agents
/
Histamine Release
/
Mast Cells
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Type:
Article
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