1788-55-2Relevant academic research and scientific papers
Design, synthesis, and aldose reductase inhibitory effect of some novel carboxylic acid derivatives bearing 2-substituted-6-aryloxo-pyridazinone moiety
?z?elik, Azime Berna,Akda?, Mevlüt,Beydemir, ?ükrü,Demir, Yeliz
, (2022/03/01)
The polyol pathway is a two-step metabolic pathway in which glucose is reduced to sorbitol and then converted to fructose. The first and rate limiting enzyme of this pathway, aldose reductase (ALR2), is a drug target for treating diabetic complications and inflammation. Given the common features of the known inhibitors, we designed a series of pyridazinone bearing benzoic acid derivatives and then we carried the carboylic acid group onto pyridazinone and synthesized them. We evaluated the compounds against ALR2. Our results showed that all the compounds showed submicromolar or low micromolar inhibitory activity against ALR2. Compound 1 and 3 were found more active than the reference compound (epalrestat) with IC50 values of 0.278 μM (Ki=0.042±0.006 μM, competitive) and 0.188 μM (Ki=0.024±0.001 μM, competitive) respectively. Moreover, non carboxylic acid derivative 16c and the ester counterparts of 1, 3, and 12 (1c, 3c, and 12c) showed submicromolar activity against ALR2. According the results, we are able to establish some SARs in order to use in our further studies.
Histone deacetylase inhibitor taking pyridazinone as mother nucleus structure, and preparation method and applications thereof
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, (2019/02/10)
The invention discloses a histone deacetylase inhibitor taking pyridazinone as a mother nucleus structure, and a preparation method and applications thereof. The structure of the inhibitor is shown asa formula I; and the compound shown as the formula I has good histone deacetylase inhibitory activity and anti-tumor cell proliferation effects, and can be used for treating cancers. The structure ofthe inhibitor is shown as the formula I.
Pyridazinone derivatives
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Page/Page column 24, (2011/11/12)
Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment
PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Page/Page column 119, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
