Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-asthmatics

…, SH Jung, JH Kim, JM Lee, BC Suh, MX Xiang…

Index: Kim, Euikyung; Chun, Hyung-Ok; Jung, Sung-Hak; Kim, Jong Hoon; Lee, Jae-Mok; Suh, Byung-Chul; Xiang, Myung Xik; Rhee, Chung K. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2355 - 2358

Full Text: HTML

Citation Number: 19

Abstract

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 ...

Related Articles:

Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl) imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP- …

[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]

Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: prevention of reactive intermediate formation and covalent binding

[Bioorganic and Medicinal Chemistry Letters, , vol. 12, # 16 p. 2149 - 2152]

Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor

[Bioorganic and medicinal chemistry letters, , vol. 12, # 11 p. 1457 - 1461]

More Articles...