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Bioorg Med Chem Lett. 2003 Jul 21;13(14):2355-8.

Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.

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Pharmacology and Analytical Chemistry Research, 319 Hyundai I Valley, 223-12 Sandaewon-dong, Choongwon-gu, Sungnam-si, 462-120, Kyonggi-do, Republic of Korea.


A new series of catechol hydrazines was synthesized and their structure-activity relationship (SAR) was analyzed for developing an effective phosphodiesterase 4 (PDE4) inhibitor as an anti-asthmatic drug candidate. Among the (E)-Analogues tested using in vitro assays, 5CC showed a strong PDE4 inhibitory activity and a significantly improved rolipram binding profile compared with rolipram, a prototype PDE4 inhibitor. Moreover, from in-vivo asthma model, we observed that (E)-Analogue 5CC had a good efficacy against guinea-pig respiratory tract inflammation and bronchoconstriction, along with a remarkably reduced emetic side effect, compared with rolipram. Conclusively, (E)-Analogue 5CC seems to be a promising candidate for the development of anti-asthmatic PDE4 inhibitors.

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