Synthesis and anti-histamine release activity of phenyl tetrazole compounds.
- Author:
Zhi-Yu LI
1
;
Ping-Bo LU
;
Hui JI
;
Qing SHAO
;
Qi-Dong YOU
;
Xiao LIU
Author Information
1. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Anti-Asthmatic Agents;
chemical synthesis;
chemistry;
pharmacology;
Histamine Release;
drug effects;
Mast Cells;
drug effects;
metabolism;
Molecular Structure;
Rats;
Rats, Sprague-Dawley;
Structure-Activity Relationship;
Tetrazoles;
chemical synthesis;
chemistry;
pharmacology;
p-Methoxy-N-methylphenethylamine;
pharmacology
- From:
Acta Pharmaceutica Sinica
2009;44(10):1112-1117
- CountryChina
- Language:Chinese
-
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.
