Triazole-substituted phenylboronic acids as tunable lead inhibitors of KPC-2 antibiotic resistance was written by Zhou, Jingyuan;Stapleton, Paul;Xavier-Junior, Francisco Humberto;Schatzlein, Andreas;Haider, Shozeb;Healy, Jess;Wells, Geoffrey. And the article was included in European Journal of Medicinal Chemistry in 2022.Related Products of 4298-52-6 This article mentions the following:
Inhibition of β-lactamases is a promising strategy to overcome antimicrobial resistance to commonly used β-lactam antibiotics. Boronic acid derivatives have proven to be effective inhibitors of β-lactamases due to their direct interaction with the catalytic site of these enzymes. We synthesized a series of phenylboronic acid derivatives and evaluated their structure-activity relationships as Klebsiella pneumoniae carbapenemase (KPC-2) inhibitors. We identified potent KPC-2 inhibitors 2e & 6c (Ki = 0.032 μM and 0.038 μM, resp.) that enhance the activity of cefotaxime in KPC-2 expressing Escherichia coli. The measured acid dissociation constants (pKa) of selected triazole-containing phenylboronic acids was broad (5.98-10.0), suggesting that this is an addnl. property of the compounds that could be tuned to optimize the target interaction and/or the physicochem. properties of the compounds These findings will help to guide the future development of boronic acid compounds as inhibitors of KPC-2 and other target proteins. In the experiment, the researchers used many compounds, for example, 2-Ethynylthiophene (cas: 4298-52-6Related Products of 4298-52-6).
2-Ethynylthiophene (cas: 4298-52-6) belongs to benzothiophene derivatives. Benzothiophene is relatively a stable molecule. The electrophilic substitution of benzothiophene systems is much less regioselective than that of indoles. It is also used in the manufacturing of dyes such as thioindigo.Related Products of 4298-52-6
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem