97936-36-2Relevant academic research and scientific papers
NEUROPROTECTIVE PDI MODULATING SMALL MOLECULES AND METHODS OF USE THEREOF
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Paragraph 0181; 0183; 0185, (2020/06/19)
The present disclosure provides, inter alia, compounds and compositions having the formula (I) as defined herein. Methods of using and making such compounds and compositions are also provided. The present disclosure further provides screening methods, including detectable probes as well as diagnostic methods and methods for monitoring the progress of a disease, such as a neurodegenerative disease.
NOVEL COMPOUND HAVING 4-PYRIDYLALKYLTHIO GROUP AS SUBSTITUENT
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Page/Page column 63, (2008/06/13)
A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a pharmaceutical. Compound represented by the following general formula [I] or salts thereof are useful as therapeutic agents for diseases in which angiogenesis or augmentation of vascular permeability is involved. In the formula, ring "A" is a benzene ring or an aromatic five- or six-memberd heterocycle which can be fused with a cycloalkane ring, "B" is alkylene, R1 and R2, the same or different, are H, OH, substituted or unsubstituted alkoxy and the like, X and Y, the same or different, are group(s) selected from H, halogen, OH, substituted or unsubstituted alkoxy and the like respectively, p is 0, 1 or 2, and q is 0 or 1.
Synthesis and evaluation of new ethyl 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridine-2-alkanoate derivatives as potential herbicides
Gil,Zabalza,Navarro,Manu,Gonzalez,Merino,Canal,Royuela,Aparicio-Tejo
, p. 148 - 156 (2007/10/03)
Several ethyl 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridine-2-alkanoate derivatives were synthesized as herbicides. Only 5-methyl derivatives inhibited both hypocotyl and root growth in the lettuce (Lactuca sativa L.) seedling test at 100 mg litre-1. Only ethyl propionate and valerate derivatives showed significant inhibition at 0.1 mg litre-1, whereas ethyl acetate or butyrate derivatives were inactive. Contrary to unoxidized derivatives, the inhibitory effect of 1-oxide and 1,1-dioxide derivatives was strongly dependent on concentration; ethyl 2,3-dihydro-5-methyl-3-oxoisothiazolo[5,4-b]pyridine-2-propionate 1,1-dioxide inhibited 100% of germination at 100 mg litre-1 and 45% of lettuce seedling growth at 0.1 mg litre-1. Quantitative structure-inhibition of growth relationship analysis carried out by adaptive least-squares (ALS) method gave a good correlation with small and hydrophobic 5-substituents as well as with odd carbon-chain ethyl alkanoates in position 2. Active compounds did not show auxin-like activity from 0.1 to 100 mg litre-1.
Synthesis and diuretic activity of pyrido[2,3-d]pyrimidones and related compounds
Monge,Martinez-Merino,Cenarruzabeitia,et al.
, p. 61 - 66 (2007/10/02)
The synthesis of a series of pyrido[2,3-d]pyrimidine-4-one derivatives (7) and the results of a study of their potassium-sparing diuretic activity are described. Compounds 7 were prepared from 2-chloro-3-pyridinecarbonyl chloride, 1,2-dihydro-2-thioxo-3-pyridinecarbonyl chloride, 2-methylthio-3-pyridinecarbonyl chloride or 2-(p-chlorophenyl)thio-3-pyridinecarbonylchloride and different amines through the respective amides (4). Compounds 4 and 7 were assayed for diuretic and potassium-sparing activities. Although some of the compounds showed significant diuretic activity, a significant increase of the Na+/K+ index was only observed with 5-oxo-5H(1,3)thiazolo[3,2-a]pyrido[3,2-e]pyrimidine.
