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Article

Benzyl-Modified Quinolone-Aminopyrimidine Hybrids with Potent Anti-MRSA Activity and a High Barrier to Resistance

by
Xinghua Xu
,
Renhua Fan
and
Qiuqin He
*
Department of Chemistry, Fudan University, 2005 Songhu Road, Yangpu District, Shanghai 200438, China
*
Author to whom correspondence should be addressed.
Molecules 2026, 31(10), 1633; https://doi.org/10.3390/molecules31101633
Submission received: 13 April 2026 / Revised: 4 May 2026 / Accepted: 8 May 2026 / Published: 12 May 2026
(This article belongs to the Special Issue Small-Molecule Drug Design and Discovery)
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Abstract

A series of novel quinolone–aminopyrimidine hybrids were designed and synthesized through benzyl-position modification. Among them, A3 and A5 exhibited promising anti-MRSA activity, low cytotoxicity, and a low propensity for resistance development. Notably, A5 showed favorable metabolic stability in both HLMs and RLMs, whereas A3 displayed excessively prolonged half-lives, suggesting a potential risk of in vivo accumulation. Overall, A5 was identified as a promising lead compound for further antibacterial development.
Keywords: quinolone-aminopyrimidine hybrids; MRSA; resistance quinolone-aminopyrimidine hybrids; MRSA; resistance
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MDPI and ACS Style

Xu, X.; Fan, R.; He, Q. Benzyl-Modified Quinolone-Aminopyrimidine Hybrids with Potent Anti-MRSA Activity and a High Barrier to Resistance. Molecules 2026, 31, 1633. https://doi.org/10.3390/molecules31101633

AMA Style

Xu X, Fan R, He Q. Benzyl-Modified Quinolone-Aminopyrimidine Hybrids with Potent Anti-MRSA Activity and a High Barrier to Resistance. Molecules. 2026; 31(10):1633. https://doi.org/10.3390/molecules31101633

Chicago/Turabian Style

Xu, Xinghua, Renhua Fan, and Qiuqin He. 2026. "Benzyl-Modified Quinolone-Aminopyrimidine Hybrids with Potent Anti-MRSA Activity and a High Barrier to Resistance" Molecules 31, no. 10: 1633. https://doi.org/10.3390/molecules31101633

APA Style

Xu, X., Fan, R., & He, Q. (2026). Benzyl-Modified Quinolone-Aminopyrimidine Hybrids with Potent Anti-MRSA Activity and a High Barrier to Resistance. Molecules, 31(10), 1633. https://doi.org/10.3390/molecules31101633

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