- New procedure for the total synthesis of cilostamide
-
An efficient route to synthesise a wide range of N,N-R,R-4-(2-oxo-1,2- dihydroquinolin-6-yloxy)butanamide, specially Cilostamide (R = methyl and R = cyclohexyl), one of the most selective inhibitors of phosphodiesterase3 (PDE3) enzyme, from 5-methoxy-2-ni
- Seyedi, Seyed Mohammad,Sadeghian, Hamid,Arghiani, Zahra
-
experimental part
p. 183 - 186
(2009/04/06)
-
- Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide
-
Evaluation of a series of lactam heterocyclic analogues of cilostamide as inhibitors of cyclic AMP phosphodiesterase derived from both human platelets and rat heart in comparison with their corresponding methoxy-substituted heterocycles has revealed that the N-cyclohexyl-N-methyl-4-oxybutyramide side chain of 2 is an important lipophilic and/or steric pharmacophore. Attachment of this side chain to the parent heterocycle of the potent cyclic AMP phosphodiesterase inhibitor anagrelide afforded the hybrid structure RS-82856, shown to be more potent than either of its progenitors as an inhibitor of cyclic AMP phosphodiesterase or of ADP-induced platelet aggregation. The available in vitro data suggest that 1 possesses potentially useful antithrombotic and cardiotonic properties.
- Jones,Venuti,Alvarez,Bruno,Berks,Prince
-
p. 295 - 303
(2007/10/02)
-
- Substituted carbostyrils as inhibitors of cyclic AMP phosphodiesterase
-
A series of 6-substituted carbostyrils has been synthesized and tested as inhibitors of two vascular smooth muscle phosphodiesterases, one of them selective for cyclic AMP and the other calmodulin dependent and selective for cyclic GMP. The inhibitory act
- Lugnier,Bruch,Stoclet,et al.
-
p. 121 - 125
(2007/10/02)
-
- Studies on 2-oxoquinoline derivatives as blood platelet aggregation inhibitors. III. N-cyclohexyl-N-(2-hydroxyethyl)-4-(1,2-dihydro-2-oxo-6-quinolyloxy) butyramide and related compounds
-
A series of N,N-disubstituted-ω-(1,2-dihydro-2-oxoquinolyloxy)alkanecarboxamides was synthesized and tested for inhibitory activity towards collagen- and ADP-induced aggregation of rabbit blood platelet in vitro. These compounds were prepared by the react
- Nishi,Tabusa,Tanaka,Ueda,Shimizu,Kanbe,Kimura,Nakagawa
-
p. 852 - 860
(2007/10/02)
-
- NOVEL CARBOSTYRIL DERIVATIVES
-
Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula wherein R1 is hydrogen, C1-4 alkyl, C2-4 alkenyl, phenyl-C1-4 alkyl-; R2 is hydrogen, a halogen atom, hydroxy, phenyl-C1-4 alkoxy; R3 is hydrogen, hydroxy, C1-4 alkyl; R4 is C3-8 cycloalkyl, substituted or unsubstituted phenyl, C3-8 cycloalkyl-C1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R5 is hydrogen, C1-8 alkyl, C2-4 alkenyl, phenyl, C3-8 cycloalkyl, phenyl-C1-4 alkyl, C3-8 cycloalkyl-C1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond
- -
-
-