Category: 871125-81-4

Doebelin, Christelle published the artcileIdentification of potent RORβ modulators: Scaffold variation, Name: (3-Bromo-5-isopropoxyphenyl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(19), 3210-3215, database is CAplus and MEDLINE.

The authors sought to develop RORβ-selective probe mols. to investigate the function of the receptor in vitro and in vivo and its role in the pathophysiol. of disease. To accomplish this, the authors modified a potent dual RORβ/RORγ inverse agonist from the primary literature with the goal of improving selectivity for RORβ vs. RORγ. Truncation of the Western portion of the mol. ablated activity at RORγ and led to a potent series of RORβ modulators. Continued exploration of this series investigated alternate replacement cores for the aminothiazole ring. Numerous suitable replacements were found during the course of the authors’ SAR investigations and are reported herein.

Bioorganic & Medicinal Chemistry Letters published new progress about 871125-81-4. 871125-81-4 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (3-Bromo-5-isopropoxyphenyl)boronic acid, and the molecular formula is C9H12BBrO3, Name: (3-Bromo-5-isopropoxyphenyl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Correy, Galen J. published the artcileOvercoming insecticide resistance through computational inhibitor design, Application of (3-Bromo-5-isopropoxyphenyl)boronic acid, the publication is Proceedings of the National Academy of Sciences of the United States of America (2019), 116(42), 21012-21021, database is CAplus and MEDLINE.

Insecticides allow control of agricultural pests and disease vectors and are vital for global food security and health. The evolution of resistance to insecticides, such as organophosphates (OPs), is a serious and growing concern. OP resistance often involves sequestration or hydrolysis of OPs by carboxylesterases. Inhibiting carboxylesterases could, therefore, restore the effectiveness of OPs for which resistance has evolved. Here, we use covalent virtual screening to produce nano-/picomolar boronic acid inhibitors of the carboxylesterase αE7 from the agricultural pest Lucilia cuprina as well as a common Gly137Asp αE7 mutant that confers OP resistance. These inhibitors, with high selectivity against human acetylcholinesterase and low to no toxicity in human cells and in mice, act synergistically with the OPs diazinon and malathion to reduce the amount of OP required to kill L. cuprina by up to 16-fold and abolish resistance. The compounds exhibit broad utility in significantly potentiating another OP, chlorpyrifos, against the common pest, the peach-potato aphid (Myzus persicae). These compounds represent a solution to OP resistance as well as to environmental concerns regarding overuse of OPs, allowing significant reduction of use without compromising efficacy.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 871125-81-4. 871125-81-4 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (3-Bromo-5-isopropoxyphenyl)boronic acid, and the molecular formula is C9H12BBrO3, Application of (3-Bromo-5-isopropoxyphenyl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary