NAD(P)H:quinone oxidoreductase 1 inducer activity of some novel aminoquinazoline derivatives was written by Ghorab, Mostafa M.;Alsaid, Mansour S.;Higgins, Maureen;Dinkova-Kostova, Albena T.;Shahat, Abdelaaty A.;Elghazawy, Nehal H.;Arafa, Reem K.. And the article was included in Drug Design, Development and Therapy in 2016.Quality Control of 1-Ethyl-1H-pyrazol-5-amine This article mentions the following:
This work presents the design and synthesis of novel quinazoline derivatives I [R = heptyl, morpholinoethyl, 3-(2-oxopyrrolidin-1-yl)propyl, etc.] and evaluation of their NQO1 inducer activity in murine cells. Mol. docking of I was performed to assess their ability to inhibit Keap1-Nrf2 protein-protein interaction through occupying the Keap1-Nrf2-binding domain, which leads to Nrf2 accumulation and enhanced gene expression of NQO1. Docking results showed that all compounds can potentially interact with Keap1. Compound I [R = 1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl], the most potent inducer, showed the largest number of interactions with key amino acids in the binding pocket (Arg483, Tyr525, and Phe478) compared to the native ligand or any other compound in this series. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Quality Control of 1-Ethyl-1H-pyrazol-5-amine).
1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Quality Control of 1-Ethyl-1H-pyrazol-5-amine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics