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J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors.
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.
Design, synthesis, and discovery of a novel CCR1 antagonist.
This work has identified xanthene-9-carboxamide 1a, the first murine CCR1 receptor antagonist, which may be a useful tool for clarifying the role of C CR1 receptors in murine models of disease.
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
A potent M(3) antagonist, 14a (K(i) = 0.31 nM), with novel structural features was identified, which showed high selectivity for M( 3) receptors over the other muscarinic receptor subtypes.
Structure-activity relationships of 2-(benzothiazolylthio)acetamide class of CCR3 selective antagonist.
Derivatization of 1a including incorporation of substituent(s) into each benzene ring of the benzothiazole and piperidine side chain resulted in the identification of potent and selective compounds exhibiting nano-molar binding affinity and greater than 800-fold selectivity for the CCR3 receptor over the C CR1 receptor.
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing…
- H. Hirose, I. Aoki, K. Noguchi
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 May 2001
It is demonstrated that compound A has high selectivity for M(3) receptors over M(2) receptors, displays a potent, oral M( 3) antagonistic activity without inhibition of central muscarinic receptors because of low brain penetration, and may have fewer cardiac or CNS side effects than nonselective compounds.
Dicationic dithiocarbamate carbapenems with anti-MRSA activity.
Identification of a potent and nonpeptidyl ccr3 antagonist.
It is suggested that Compound X may be a useful tool for elucidating the pathophysiological roles of CCR3 in a variety of allergic disorders.
Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity.
- Yousuke Yamada, Hajime Takashima, R. Hubbard
- Chemistry, BiologyJournal of medicinal chemistry
- 19 November 2020
A structure-guided design led to a 2-(1S-hydroxyethyl)-imidazole derivative exhibiting low nanomolar inhibition of LpxC and a minimum inhibitory concentration (MIC) of 4 μg/mL against Pseudomonas aeruginosa, which is little affected by the presence of albumin.