1515-27-1Relevant articles and documents
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists
Xu, Rong,Sim, Meng-Kwoon,Go, Mei-Lin
, p. 3220 - 3231 (1998)
A number of O-alkynyloximes of tropinone and N-methyl-4-piperidinone have been synthesized and evaluated for muscarinic activity. The affinities of these oximes were tested in homogenates of cerebral cortex, heart, and submandibulary glands from rats using [3H]pirenzepine and [3H]-N- methylscopolamine as radioligands. The oximes bind to the cortical muscarinic receptors with pK(i) values varying from 3 to 7. Higher binding affinities were observed for the O-alkynyl tropinone oximes than the corresponding piperidinone analogues. Binding to the muscarinic sites in the heart and submandibulary glands was also observed but with lower affinities. Good M1 subtype selectivity (10-fold or greater) was observed with some oximes (26a, 28a, 32a) at the cortical sites. These oximes also attenuated scopolamine- induced impairment of the water mask task in mice. Functional assays for M3 activity on the rat aorta showed that all oximes possessed M3 agonist action but M2 agonist activity was not observed at the endothelium-denuded rabbit aorta. Analysis of the quantitative structure-activity relationship (QSAR) indicated that the Connolly surface area is an important determinant of activity, accounting for 70% of the variation in cortical binding affinity among the oximes.
Bactericidal composition containing isotianil and osthole
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Paragraph 0022; 0029; 0035, (2021/08/11)
The invention discloses a bactericidal composition containing isotianil and osthole, and belongs to the technical field of pesticide preparation. The bactericidal composition comprises, by weight, 1-50% of isotianil, 0.1-10% of osthole, 5-10% of a bacteri
PYRAZOLE DERIVATIVES AS MODULATORS OF THE WNT/B-CATENIN SIGNALING PATHWAY
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Paragraph 0213, (2020/07/31)
Pyrazole compounds (I) for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a pyrazole compounds, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2- yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors
Han, Sun-Young,Choi, Jie Won,Yang, Jeon,Chae, Chong Hack,Lee, Jongkook,Jung, Heejung,Lee, Kwangho,Ha, Jae Du,Kim, Hyoung Rae,Cho, Sung Yun
scheme or table, p. 2837 - 2842 (2012/05/20)
A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H- quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity.
NOVEL NITROSO COMPOUNDS AS NITROXYL DONORS AND METHODS OF USE THEREOF
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Page/Page column 40, (2009/12/04)
The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase
Moormann, Alan E.,Metz, Sue,Toth, Mihaly V.,Moore, William M.,Jerome, Gina,Kornmeier, Christine,Manning, Pamela,Hansen Jr., Donald W.,Pitzele, Barnett S.,Webber
, p. 2651 - 2653 (2007/10/03)
The potency and selectivity of a series of 5-hetero-2-iminohexahydroazepines were examined as inhibitors of the three human NOS isoforms. The effect of ring substitution of the 5-carbon for a heteroatom is presented. Potencies (IC50's) for these inhibitors are in the low micromolar range for hi-NOS with some examples exhibiting a 500× selectivity versus hec-NOS.
Synthesis of various geometric and enantiomeric oxime O-(α and β methylcholinyl) ethers as potential anticholinergic agents
Huerta,Isaacson,Brown,Delgado
, p. 1120 - 1124 (2007/10/04)
Various enantiomeric and geometric oxime O (α and β methylcholinyl) ethers were synthesized as potential anticholinergic agents. The synthesis, separation, resolution, and structural characterization of these compounds are reported. The first step of the synthetic pathway involved an oxime formation, with subsequent O alkylation of the respective oxime with 2 chloro N,N dimethylpropylamine hydrochloride. The separation of the α and β structural isomers utilized vacuum fractional distillation and/or column chromatography, and the resolution of the enantiomers was accomplished via the formation of tartrate diastereoisomers. A preliminary pharmacological evaluation for anticholinergic activity was conducted using a rat ileum assay. Structure activity relationships, including some stereochemical properties and antimuscarinic activity, are discussed.
