4943-83-3Relevant articles and documents
Effects Of 2-Methyl-3-propynylquinazolin-4-(3H)-one On Vascular Reactivity in Isolated Porcine Tail Arteries
Ojeikere, Odafenkhoa,Usifoh, Cyril,Ebeigbe, Anthony
, p. 321 - 329 (2003)
The vascular effects of 2-methyl-3-propynylquinazolin-4-(3H)-one (QUIN) have been studied on isolated porcine tail arteries. QUIN had no effect on resting tension but relaxed, dose-dependently, arteries precontracted with noradrenaline or high-K+/su
Synthesis of Novel Isoindolo[2,1-a]quinazolinedione Derivatives Containing a 1,2,3-Triazole Ring System
Esmaeili-Marandi, Fatemeh,Saeedi, Mina,Yavari, Issa,Mahdavi, Mohammad,Shafiee, Abbas
, p. 37 - 40 (2016)
A synthesis of isoindolo[2,1-a]quinazolinedione derivatives, coupled with a 1,2,3-triazole ring system, via the reaction of isatoic anhydride, HC=CCH2NH2, and 2-formylbenzoic acid is described, which led to the formation of the isoin
Quinazolinone [2, 3 - a] carboline derivative as well as preparation method and application thereof
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Paragraph 0054-0057; 0141-0144, (2021/10/11)
The main content of the invention is to provide a new quinazolinone [2, 3 - a] carboline compound as well as a preparation method and application thereof, and has the quinazolinone of the general formula (I) and [2, 3 - a] carboline compounds. A quinazolo
Glycosyl triazoles as novel insect β-N-acetylhexosaminidase OfHex1 inhibitors: Design, synthesis, molecular docking and MD simulations
Dong, Lili,Shen, Shengqiang,Chen, Wei,Lu, Huizhe,Xu, Dongdong,Jin, Shuhui,Yang, Qing,Zhang, Jianjun
, p. 2315 - 2322 (2018/12/11)
The insect enzyme GH20 β-N-acetyl-D-hexosaminidase OfHex1 represents an important chitinolytic enzyme found in the agricultural pest Ostrinia furnacalis (Guenée) and inhibition of this enzyme has been considered a promising strategy for the development of eco-friendly pesticides. In this article, based on the structure of the catalytic domains of OfHex1, a series of novel glycosyl triazoles were designed and synthesized via Cu-catalyzed azide-alkyne [3+2] cycloaddition reaction. To investigate the potency and selectivity of these glycosyl triazoles, the inhibition activities towards OfHex1 and HsHexB (human β-N-acetylhexosaminidase B) were studied. Particularly compound 17c (OfHex1, Ki = 28.68 μM; HsHexB, Ki > 100 μM) exhibited a suitable activity and selectivity against OfHex1. Furthermore, the possible inhibitory mechanisms of 17c with OfHex1 were studied using molecular docking and MD simulations. The structure-activity relationship results as well as the formed binding patterns may provide promising insights into the further development of novel OfHex1 inhibitors.