Month: September 2024

Ring opening [3+2] cyclization of azaoxyallyl cations with benzo[d]isoxazoles: Efficient access to 2-hydroxyaryl-oxazolines was written by He, Yicheng;Pi, Chao;Wu, Yangjie;Cui, Xiuling. And the article was included in Chinese Chemical Letters in 2020.Recommanded Product: 4-Bromobenzo[d]isoxazole This article mentions the following:

A selective ring-opening [3+2]cyclization reaction of benzo[d]isoxazoles with 2-bromo-propanamides was developed. The azaoxyallyl cation intermediates were employed as C∼O 3-atom synthon to build oxa-heterocycles via the selectivity of suitable cyclization partners. This transformation provided rapid access to highly functionalized 2-hydroxyaryl-oxazolines under mild conditions and excellent regioselectivity. In the experiment, the researchers used many compounds, for example, 4-Bromobenzo[d]isoxazole (cas: 1126848-34-7Recommanded Product: 4-Bromobenzo[d]isoxazole).

4-Bromobenzo[d]isoxazole (cas: 1126848-34-7) belongs to benzisoxazole derivatives. Benzisoxazole is an aromatic organic compound containing a benzene-fused isoxazole ring structure. Its aromaticity makes it relatively stable. These include antidepressants, anti-inflammatory agents, antimalarial drugs, antipsychotics, antiviral agents, steroids, and anesthetics.Recommanded Product: 4-Bromobenzo[d]isoxazole

Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Novel N-benzylpiperidine derivatives of 5-arylisoxazole-3-carboxamides as anti-Alzheimer’s agents was written by Saeedi, Mina;Felegari, Peyman;Iraji, Aida;Hariri, Roshanak;Rastegari, Arezoo;Mirfazli, S. Sara;Edraki, Najmeh;Firuzi, Omidreza;Mahdavi, Mohammad;Akbarzadeh, Tahmineh. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2021.Name: 5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid This article mentions the following:

The complex pathophysiol. of Alzheimer’s disease (AD) has prompted researchers to develop multitarget-directed mols. to find an effective therapy against the disease. In this context, a novel series of N-(1-benzylpiperidin-4-yl)-5-arylisoxazole-3-carboxamide derivatives were designed, synthesized, and evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). In vitro biol. evaluation demonstrated that compound I was the best AChE (IC₅₀ = 16.07μM) and BuChE inhibitor (IC₅₀ = 15.16μM). A kinetic study of I was also conducted, which presented a mixed-type inhibition for both enzymes. Mol. docking studies revealed that compound I fitted well into the active sites of AChE and BuChE, forming stable and strong interactions with key residues Glu199, Trp84, Asp72, Tyr121, and Phe288 in AChE and His438, Trp82, Ala328, Tyr332, Phe329, Thr120, and Pro285 in BuChE. Besides, the inhibition of BACE1 by I and the biometal chelation activity of I were measured. The neuroprotective assessment revealed that I exhibited 23.2% protection at 50μM toward amyloid-beta-induced PC12 neuronal cells. Overall, this study exhibited that compound I was a promising compound targeting multiple factors associated with AD. In the experiment, the researchers used many compounds, for example, 5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid (cas: 334017-34-4Name: 5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid).

5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid (cas: 334017-34-4) belongs to benzisoxazole derivatives. The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. Functionalized benzisoxazoles and benzisoxazoyls have a variety of uses, including pharmaceutical drugs such as some antipsychotics and the anticonvulsant zonisamide.Name: 5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid

Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics