[Synthesis and anti-histamine release activity of phenyl tetrazole compounds].
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.
Li
Zhi-Yu
ZY
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Lu
Ping-Bo
PB
Ji
Hui
H
Shao
Qing
Q
You
Qi-Dong
QD
Liu
Xiao
X
D000818:Animals; D018927:Anti-Asthmatic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism*; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
D018927:Anti-Asthmatic Agents; C573653:N-(3-(5-(1H-tetrazol))pheny)-2-(4-isobutylphenyl)propionamide; D013777:Tetrazoles; D003189:p-Methoxy-N-methylphenethylamine