DOAJ Open Access 2024

Incorporation of an Isohexide Subunit into the Endochin-like Quinolone Scaffold

Julia Senkina Spencer Knapp

Abstrak

In order to improve the drug-likeness qualities, the antimalarial endochin-like quinolone (ELQ) scaffold has been modified by replacing the 4-(trifluoromethoxy)phenyl portion with an isoidide unit that is further adjustable by varying the distal O-substituents. As expected, the water solubilities of the new analogs are greatly improved, and the melting points are lower. However, the antimalarial potency of the new analogs is reduced to EC<sub>50</sub> > 1 millimolar, a result ascribable to the hydrophilic nature of the new substitution.

Topik & Kata Kunci

Organic chemistry

Penulis (2)

Julia Senkina

Spencer Knapp

Format Sitasi

APA MLA BibTeX

Senkina, J., Knapp, S. (2024). Incorporation of an Isohexide Subunit into the Endochin-like Quinolone Scaffold. https://doi.org/10.3390/molecules29153615

Akses Cepat

PDF tidak tersedia langsung

Cek di sumber asli →

Lihat di Sumber doi.org/10.3390/molecules29153615

Informasi Jurnal

Tahun Terbit: 2024
Sumber Database: DOAJ
DOI: 10.3390/molecules29153615
Akses: Open Access ✓