title: Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5.
abstract: HTS and the following synthesis of a series of the compounds led us to the discovery of hydroxamic acid analogs as potent dual inhibitors of phosphodiesterase (PDE)-1 and 5. These compounds have highly related structure and deviation of the structure usually resulted in reduced potency. This result can be used to design other molecules that may be utilized for the therapy of cardiovascular symptoms that relates to cGMP level.
authors: Research Division, Sumitomo Pharmaceuticals Co., Ltd, 3-1-98 Kasugadenaka, Konohana-ku, Osaka 554-0022, Japan.
authors: Akihito
authors: A
authors: Dan
authors: Takaaki
authors: T
authors: Shiyama
authors: Kazuto
authors: K
authors: Yamazaki
authors: Naoto
authors: N
authors: Kusunose
authors: Katsuya
authors: K
authors: Fujita
authors: Hideshi
authors: H
authors: Sato
authors: Kazutaka
authors: K
authors: Matsui
authors: Masafumi
authors: M
authors: Kitano
mesh_terms: D006152:Cyclic GMP / Q000378:metabolism; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D006877:Hydroxamic Acids; D010726:Phosphodiesterase Inhibitors; D010727:Phosphoric Diester Hydrolases; D006152:Cyclic GMP