Chen, Allie Y. et al. published their research in Journal of Medicinal Chemistry in 2017 | CAS: 55661-33-1

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Category: thiazole

Dipicolinic Acid Derivatives as Inhibitors of New Delhi Metallo-β-lactamase-1 was written by Chen, Allie Y.;Thomas, Pei W.;Stewart, Alesha C.;Bergstrom, Alexander;Cheng, Zishuo;Miller, Callie;Bethel, Christopher R.;Marshall, Steven H.;Credille, Cy V.;Riley, Christopher L.;Page, Richard C.;Bonomo, Robert A.;Crowder, Michael W.;Tierney, David L.;Fast, Walter;Cohen, Seth M.. And the article was included in Journal of Medicinal Chemistry in 2017.Category: thiazole This article mentions the following:

The efficacy of β-lactam antibiotics is threatened by the emergence and global spread of metallo-β-lactamase (MBL) mediated resistance, specifically New Delhi metallo-β-lactamase-1 (NDM-1). By utilization of fragment-based drug discovery (FBDD), a new class of inhibitors for NDM-1 and two related β-lactamases, IMP-1 and VIM-2, was identified. On the basis of 2,6-dipicolinic acid (DPA), several libraries were synthesized for structure-activity relationship (SAR) anal. Inhibitor I (IC50 = 80 nM) was identified to be highly selective for MBLs when compared to other Zn(II) metalloenzymes. While DPA displayed a propensity to chelate metal ions from NDM-1, I formed a stable NDM-1:Zn(II):inhibitor ternary complex, as demonstrated by 1H NMR, ESR (EPR) spectroscopy, equilibrium dialysis, intrinsic tryptophan fluorescence emission, and UV-vis spectroscopy. When coadministered with I (at concentrations nontoxic to mammalian cells), the min. inhibitory concentrations (MICs) of imipenem against clin. isolates of Escherichia coli and Klebsiella pneumoniae harboring NDM-1 were reduced to susceptible levels. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Category: thiazole).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica