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 ...
[Brackeen, Marcus F.; Cowan, David J.; Stafford, Jeffrey A.; Schoenen, Frank J.; Veal, James M.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 24 p. 4848 - 4854]
