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Antimicrobial drugs bearing guanidine moieties: A review

Research output: Contribution to journalReview articlepeer-review

Original languageEnglish
Article number113293
Published15 Apr 2021

Bibliographical note

Funding Information: We gratefully acknowledge the South African National Research Foundation-SARChI for financial support to DS. Publisher Copyright: © 2021 Elsevier Masson SAS Copyright: Copyright 2021 Elsevier B.V., All rights reserved.

King's Authors


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.

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