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Updated: Jun 17, 2026

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Published on: May 31, 2021
[Synthesis and anti-histamine release activity of phenyl tetrazole compounds]
Zhi-Yu Li1, Ping-Bo Lu, Hui Ji
1Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
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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