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Updated: Aug 20, 2026

Dry Powder and Nebulized Aerosol Inhalation of Pharmaceuticals Delivered to Mice Using a Nose-only Exposure System
Published on: April 6, 2017
[Design, synthesis and antiasthmatic activities of NO-donating seratrodast derivatives]
Zhi-guo Zhang1, Yi-hua Zhang, Hui Ji
1Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China.
Aim:
To search for novel antiasthmatic agents.
Methods:
Coupling seratrodast (SD), an antiasthmatic drug, with several different types of NO donors including oxatriazoles, N-hydroxyguanidines and furoxans; evaluating the antiasthmatic effects of coupled compounds by determining their inhibitory activity of guinea pig asthma induced by acetylcholine and histamine; and assessing NO releasing ability.
Results:
Nine novel target compounds (I1-9) were synthesized, and their structures were established by IR, NMR, MS and elemental analysis. Preliminary pharmacological test showed that most of the compounds showed high antiasthmatic activities (the latent period of induced asthma was prolonged from 10 s (SD) to 26-62 s), among which 3 compounds (I4, I6, I7) were more potent than SD (P < 0.05, P < 0.01) and released more NO than others. The maximum concentrations (Cmax) of NO-release in vitro were 0.1878, 0.1393 and 0.2473 mg x L(-1), respectively.
Conclusion:
NO donating-SD derivatives are worthy to be futher investigated.
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