Antimicrobial drugs bearing guanidine moieties: A review

TY - JOUR

T1 - Antimicrobial drugs bearing guanidine moieties

T2 - A review

AU - Kim, Seong Heun

AU - Semenya, Dorothy

AU - Castagnolo, Daniele

N1 - 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.

PY - 2021/4/15

Y1 - 2021/4/15

N2 - 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.

AB - 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.

KW - Antimicrobials

KW - Bacteria

KW - Fungal infections

KW - Guanidine

KW - Malaria

KW - Tuberculosis

UR - http://www.scopus.com/inward/record.url?scp=85101531526&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2021.113293

DO - 10.1016/j.ejmech.2021.113293

M3 - Review article

AN - SCOPUS:85101531526

SN - 0223-5234

VL - 216

JO - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

JF - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

M1 - 113293

ER -