42026-49-3Relevant articles and documents
The monoamine oxidase inhibition properties of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives
Marais, Lereze,Petzer, Anél,Petzer, Jacobus P.,Legoabe, Lesetja J.
, p. 391 - 406 (2020)
Abstract: Quinazolinone compounds are of interest in medicinal chemistry since they display a wide range of biological properties. In the present study, a series of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO). Some of these quinazolinones are structurally related to a series of 3,4-dihydro-2(1H)-quinolinone derivatives, which have previously been reported to act as specific inhibitors of MAO-B. The results document that, among 37 compounds synthesised, seven displayed IC50 values 50 value of 7.43?μM while the most potent MAO-B inhibitor possesses an IC50 value of 0.269?μM. Good-potency MAO inhibition was only observed among C6-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives with N1-substitution yielding comparatively low-potency inhibition. MAO-B-specific inhibitors such as some of the quinazolinone compounds investigated here may act as leads for the design of therapies for neurodegenerative disorders such as Parkinson’s disease. Graphical abstract: [Figure not available: see fulltext.].
The evaluation method of destruction of structure
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, (2007/10/09)
PROBLEM TO BE SOLVED: To provide a critical Weibull stress diagram for enabling the evaluations of brittle fractures including the case of the absence of initial cracks through the use of Charpy impact values generally in use at present and provide an appropriate structure destruction evaluating method based on such evaluations. ?SOLUTION: The structure destruction evaluating method includes: (i) the previous grasp of the relation between critical Weibull stress and Charpy impact values on brittle materials (S4); (ii) the determination, on a structure to be designed, of the relation between generated Weibull stress generated in materials used for the structure, one of the brittle materials, and design parameters of the structure (S1-S3); and (iii) the determination of the relation between Charpy impact values characteristic to the materials used and the design parameters of the structure on the basis of the two relations in such a way that the generated Weibull stress may not exceed the critical Weibull stress (S5 and S6). ?COPYRIGHT: (C)2009,JPOandINPIT ?
