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European Journal of Medicinal Chemistry
Volume 216, 2021, 113293

Antimicrobial drugs bearing guanidine moieties: A review

Seong-HeunKim1, Dorothy Semenya1, Daniele Castagnolo

School of Cancer and Pharmaceutical Sciences, King’s College London, 150 Stamford Street, SE1 9NH, London, United Kingdom.


Compounds incorporating guanidine moieties constitute a versatile class of biologically interesting molecules with a wide array of applications. As such, guanidines have been exploited as privileged structural motifs in designing novel drugs for the treatment of various infectious and non-infectious diseases. In designing anti-infective agents, this moiety carries great appeal by virtue of attributes such as hydrogen-bonding capability and protonatability at physiological pH in the context of interaction with biological targets. This review provides an overview of recent advances in hit-to-lead development studies of antimicrobial guanidine-containing compounds with the aim to highlight their structural diversity and the pharmacological relevance of the moiety to drug activity, insofar as possible. In so doing, emphasis is put on chemical and microbiological properties of such compounds in relation to antibacterial, antifungal and antimalarial activities.

Keywords: Guanidine, Bacteria, Fungal infections, Malaria, Antimicrobials, Tuberculosis.

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