New Advances in Chemical Research, April 2021.The transformation of simple hydrocarbons into more complex has revolutionised modern synthetic chemistry. This type of reactivity has quickly become one of the cornerstones of modern catalysis .1118-61-2, Name is 3-Aminocrotononitrile, SMILES is CC(N)=CC#N, belongs to naphthyridine compound. In a document, author is de los Rios, Cristobal, introduce the new discover, Recommanded Product: 3-Aminocrotononitrile.
Tacrine was the first drug approved for the treatment of Alzheimer’s disease (AD) in 1993, which was withdrawn in 2013 due to its hepatotoxicity. However, new, non-hepatotoxic tacrine derivatives have been constantly searched for. In this context, since 1997, we have prepared a number of diversely functionalized tacrines by changing the benzene ring present in tacrine to five- or six-membered aromatic ring cores that could present anticholinesterasic activity and additional pharmacological properties. The new compounds were designed as juxtaposed structures between tacrine and the well-known Ca2+ antagonists 1,4-dihydropyridines, with the goal of obtaining multi-target directed ligands for AD. In this account, we present our results on the PyridoTacrine (PyrTac) family of tacrine analogues, resulting from the substitution of the benzene ring by a pyridine. We highlight their pharmacological profile and review similar analogues in the literature. A first set of PyrTac showed inhibitory activity of cholines-terases (ChE) and a blocking profile of voltage-gated Ca2+ channels (VGCC). A second family with improved ChE inhibition lost VGCC blocking activity. However, the lead compound of this family (5f) presented an activating profile of the phosphatase 2A (PP2A) and showed interesting outcomes in experimental in vivo models of AD and stroke. We have identified the PyrTac ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b] [1,8]naphthyridine-3-carboxylate (5f), which presents additional pharmacological properties beyond the mere cholinergic improvement. These new properties warrant attention to 5f and its further development as a new potential therapeutic agent for AD therapy. (C) 2019 Elsevier Masson SAS. All rights reserved.
The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.Welcome to check out more blogs about 1118-61-2, in my other articles. Recommanded Product: 3-Aminocrotononitrile.
Reference:
1,8-Naphthyridine – Wikipedia,
,1,8-Naphthyridine | C8H6N2 – PubChem