Search Results - "Combs, D W"
-
1
γ-Aminobutyrate-A Receptor Modulation by 3-Aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines
Published in Journal of medicinal chemistry (01-07-1999)“…A series of 3-aryl-1-(arylsulfonyl)-1,4,5,6-tetrahydropyridazine allosteric modulators of the GABAA receptor was synthesized, and biological activity was…”
Get full text
Journal Article -
2
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents
Published in Journal of medicinal chemistry (01-01-1990)“…A series of 6-benzoxazinylpyridazin-3-ones was prepared and evaluated for inhibition of cardiac phosphodiesterase (PDE) fraction III in vitro and for positive…”
Get full text
Journal Article -
3
Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue
Published in Biochemical pharmacology (15-07-1991)“…Canine cardiac muscle contains a type IV cyclic AMP (cAMP) phosphodiesterase (PDE) that is composed of two subtypes. One subtype is sensitive to rolipram…”
Get more information
Journal Article -
4
Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6- tetrahydropyridazines
Published in Journal of medicinal chemistry (01-12-1995)Get full text
Journal Article -
5
Nonsteroidal progesterone receptor ligands with unprecedented receptor selectivity
Published in The Journal of steroid biochemistry and molecular biology (01-12-2000)“…We have characterized a series of nonsteroidal progesterone receptor ligands, the tetrahydropyridazines. Compounds in this series, exemplified by RWJ 26819,…”
Get full text
Journal Article -
6
Determination of Hg and other trace elements in soil using neutron activation analysis
Published in Journal of radioanalytical and nuclear chemistry (01-04-1994)Get full text
Conference Proceeding Journal Article -
7
Synthesis and cardiotonic activity of a series of substituted 4-alkyl-2(1H)-quinazolinones
Published in Journal of medicinal chemistry (01-08-1987)“…The synthesis, cardiac fraction III cyclic nucleotide phosphodiesterase (PDE-III) inhibition, and positive inotropic activity of a series of…”
Get full text
Journal Article -
8
Parallel synthesis of 2-alkoxy and 2-acyloxyphenylpropyl amides and amines using dihydrocoumarins as versatile synthons. Application of a novel resin quench-capture method
Published in Tetrahedron letters (12-02-1999)“…A solution phase synthesis for the preparation of libraries of 2-substituted phenylpropyl amines and amides was accomplished using dihydrocoumarins as a useful…”
Get full text
Journal Article -
9
Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors
Published in Journal of medicinal chemistry (01-12-1995)“…A novel series of nonsteroidal heterocycles was discovered which display cell-type selective, high-affinity (nanomolar) binding to the progesterone receptors…”
Get full text
Journal Article -
10
Induction of a novel conformation in the progesterone receptor by ZK299 involves a defined region of the carboxyl-terminal tail
Published in Molecular endocrinology (Baltimore, Md.) (01-10-1996)“…Progesterone receptor antagonists are a promising class of therapeutic drugs indicated for the treatment of a variety of reproductive conditions. Understanding…”
Get full text
Journal Article -
11
Design, synthesis and bronchodilatory activity of a series of quinazoline-3-oxides
Published in Drug design and delivery (01-10-1990)“…A synthetic program of rational drug design was undertaken to develop a series of quinazoline-3-oxides as pulmonary-selective inhibitors of ovalbumin-induced,…”
Get more information
Journal Article -
12
Heteroatom analogs of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones
Published in Journal of medicinal chemistry (01-01-1992)“…A series of close analogues of the potent, long-acting cardiotonic bemoradan (2a) was synthesized and examined in both in vitro and in vivo test systems…”
Get full text
Journal Article -
13
2,6-Dihydroxy-4H-pyridazino[3,4,5-de]quinazoline: A new ring system
Published in Journal of heterocyclic chemistry (01-11-1989)“…The synthesis and spectral properties of 2,6‐dihydroxy‐4H‐pyridazino[3,4,5‐de]quinazoline 1 are described. This compound represents the first member of a new…”
Get full text
Journal Article -
14
Benzoxazinones as PPARγ Agonists. 2. SAR of the Amide Substituent and In Vivo Results in a Type 2 Diabetes Model
Published in Journal of medicinal chemistry (01-01-2004)“…A series of benzoxazinones has been synthesized and tested for PPARγ agonist activity. Synthetic approaches were developed to provide either racemic or chiral…”
Get full text
Journal Article -
15
Nonsteroidal progesterone receptor ligands. I: 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines
Published in Journal of medicinal chemistry (1995)Get full text
Journal Article -
16
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase
Published in Bioorganic & medicinal chemistry letters (01-03-2005)“…[Display omitted] A series of inhibitors of mammalian 15-lipoxygenase based on tryptamine and homotryptamine scaffolds is described. Compounds with aryl…”
Get full text
Journal Article -
17
Induction of a novel conformation in the progesterone receptor by ZK299 involves a defined region of the carboxyl-terminal tail
Published in Molecular endocrinology (Baltimore, Md.) (01-10-1996)“…Abstract Progesterone receptor antagonists are a promising class of therapeutic drugs indicated for the treatment of a variety of reproductive conditions…”
Get full text
Journal Article -
18
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists
Published in Bioorganic & medicinal chemistry letters (07-06-2004)“…Spirobenzazepines as V 1a selective as well as V 1a/V 2 dual vasopressin receptor antagonists have been described. A novel series of spirobenzazepines was…”
Get full text
Journal Article -
19
Benzoxazinones as PPARγ agonists. part 1: SAR of three aromatic regions
Published in Bioorganic & medicinal chemistry letters (21-07-2003)“…A series of benzoxazinones was synthesized as PPARγ agonists. The compounds were obtained in seven steps, and SAR was developed by variations to the core shown…”
Get full text
Journal Article -
20
Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1
Published in Bioorganic & medicinal chemistry letters (05-01-2004)“…Inhibition of the sodium hydrogen exchanger isoform-1 (NHE-1) has been shown to limit damage to the myocardium under ischemic conditions in animals. While most…”
Get full text
Journal Article