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• 2. Evidence of CO2 molecule acting as an electron acceptor on a nanoporous metal–organic-framework MIL-53 or Cr3+(OH)(O2C–C6H4–CO2)?
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• Solvents and Organic Chemicals Organic Compounds Organic nitrogen compounds Organonitrogen compounds Amines Primary amines

Research Briefing on 2-(1,2-oxazol-5-yl)ethan-1-amine (CAS: 1083216-31-2) in Chemical Biology and Pharmaceutical Applications

2-(1,2-oxazol-5-yl)ethan-1-amine (CAS: 1083216-31-2) is a heterocyclic amine derivative that has garnered significant attention in recent years due to its potential applications in chemical biology and pharmaceutical research. This compound, characterized by its oxazole ring and primary amine functional group, serves as a versatile building block for the synthesis of bioactive molecules. Recent studies have explored its utility in drug discovery, particularly in the development of small-molecule modulators targeting protein-protein interactions and enzymatic activity.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the use of 2-(1,2-oxazol-5-yl)ethan-1-amine as a key intermediate in the synthesis of novel kinase inhibitors. The researchers highlighted its role in enhancing binding affinity through hydrogen bonding interactions with conserved residues in the ATP-binding pocket of target kinases. Molecular docking simulations and in vitro assays confirmed the compound's potential as a scaffold for optimizing selectivity profiles against closely related kinase isoforms.

In neuropharmacology, a team from MIT reported in ACS Chemical Neuroscience (2024) that derivatives of 2-(1,2-oxazol-5-yl)ethan-1-amine showed promising activity as allosteric modulators of GABA_A receptors. The oxazole moiety was found to contribute significantly to the compounds' blood-brain barrier permeability, while the amine functionality allowed for structural diversification to fine-tune receptor subtype specificity. These findings open new avenues for developing non-sedative anxiolytics with reduced side-effect profiles.

The compound's utility extends to chemical biology applications as well. A recent Nature Chemical Biology publication (2024) described its incorporation into activity-based probes for profiling cysteine proteases. The 2-(1,2-oxazol-5-yl)ethan-1-amine scaffold served as an effective warhead carrier, enabling selective labeling of cathepsin family members in live-cell imaging experiments. This approach provides valuable tools for studying protease function in disease contexts, particularly in cancer metastasis and neurodegenerative disorders.

From a synthetic chemistry perspective, advances in the preparation of 2-(1,2-oxazol-5-yl)ethan-1-amine have been reported. A 2023 Organic Process Research & Development article detailed a scalable, continuous-flow synthesis route that improves yield (78%) and purity (>99%) compared to traditional batch methods. This technological advancement addresses previous challenges in large-scale production, facilitating broader investigation of the compound's pharmaceutical potential.

Ongoing clinical investigations have begun exploring 2-(1,2-oxazol-5-yl)ethan-1-amine derivatives as potential therapeutics. A phase I trial (NCT05678942) is currently evaluating a lead compound for solid tumors, with preliminary data showing favorable pharmacokinetics and manageable toxicity. Meanwhile, computational studies continue to predict new target interactions, suggesting potential applications in infectious diseases and metabolic disorders that warrant experimental validation.

As research progresses, the unique physicochemical properties of 2-(1,2-oxazol-5-yl)ethan-1-amine - including its balanced lipophilicity (cLogP ~1.2), moderate basicity (pK_a ~8.5), and conformational flexibility - position it as a privileged structure in medicinal chemistry. Future directions likely include exploration of its stereochemistry effects, prodrug strategies, and combination with emerging modalities like targeted protein degradation or covalent inhibitor design.

• 37704-51-1(5,5'-propane-1,3-diylbis(1,2-oxazole))
• 122018-86-4(5-Isoxazolepropanamine)
• 1122-01-6(Isoxazole, 5-(1,1-dimethylethyl)-)
• 858489-78-8(Isoxazole, 5-hexyl-)
• 543713-55-9(2-(3-methyl-1,2-oxazol-5-yl)ethan-1-amine)
• 933721-75-6(1-(Isoxazol-5-yl)ethanamine)
• 928340-11-8(Isoxazole, 5-octyl-)
• 217449-09-7(Isoxazole, 5-pentadecyl-)
• 30842-93-4(Isoxazole, 5-propyl-)
• 30842-91-2(5-Ethylisoxazole)