Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
The pharmacology of L-670,596, a potent and selective thromboxane/prostaglandin endoperoxide receptor antagonist.
- A. Ford-hutchinson, Y. Girard, P. Masson
- Biology, ChemistryCanadian Journal of Physiology and Pharmacology
- 1 September 1989
It is concluded that L-670,596 is a potent, selective, orally active thromboxane A2/prostaglandin endoperoxide receptor antagonist.
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.
The good inhibitory profile shown by naphthalenenitrile 9ac is accompanied by an improved resistance to oxidative metabolism, and is orally active in the functional model of antigen-induced bronchoconstriction in allergic squirrel monkeys.
Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
In rats and dogs, 3g presents excellent pharmacokinetics and bioavailabilities and, more particularly in the conscious antigen sensitive squirrel monkey model, compound 3g has been selected for preclinical animal toxicity studies.
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Synthesis of dephostatin, a novel protein tyrosine phosphatase inhibitor
First synthesis of sulfoxides and sulfones in the 3H-phenothiazin-3-one and 5H-benzo[a]phenothiazin-5-one ring systems. Addition reactions with nucleophiles
Synthese des composes du titre par oxydation des sulfoxydes et sulfones de phenothiazinol-3 et benzo [a] phenothiazinol-5
Studies on L‐640,035: a novel antagonist of contractile prostanoids in the lung
It is concluded that L‐640,035 is a novel, relatively selective, and orally active antagonist of the actions of contractile prostanoids on pulmonary smooth muscle.