SCHEDULED MAINTENANCE
Introduction to the antibiotic and antiviral compounds themed collection
Guest editors Michael J. Sofia and Xuechen Li introduce the themed collection on antibiotic and antiviral compounds.
Total synthesis of bioactive tetracyclic norditerpene dilactones
Tetracyclic norditerpene dilactones are an important class of terpenoids that have been isolated from both terrestrial and marine sources, typically from Podocarpus plants and from filamentous fungi.
A review of the latest research on Mpro targeting SARS-COV inhibitors
Since the outbreak of COVID-19, the pandemic caused by SARS-CoV-2 infection is still spreading at an alarming rate and has caused huge loss of life and economic damage worldwide.
Design, synthesis and biological evaluation of a halogenated phenazine-erythromycin conjugate prodrug for antibacterial applications
We report the synthesis and initial biological assessment of a halogenated phenazine–erythromycin conjugate prodrug 5 aimed to treat bacterial infections.
Solid-phase synthesis of coralmycin A/epi-coralmycin A and desmethoxycoralmycin A
A bidirectional solid-phase strategy is described for the total synthesis of coralmycin A and a desmethoxy analogue that possessed potent antibacterial activity.
Semisynthesis and biological evaluation of a focused library of unguinol derivatives as next-generation antibiotics
Semisynthetic unguinol derivatives showed potent activity against a panel of methicillin-resistant Staphylococcus aureus strains and are promising candidates for further development.
Multi-drug loaded eugenol-based nanoemulsions for enhanced anti-mycobacterial activity
Reformulation of 1st line anti-TB drugs using a eugenol based nanoemulsion system to enhance its drug potency as an anti-mycobacterium agent and to improve its sustainable release.
Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives
In this study, a new series of tetrahydrobenzothiophene derivatives have been designed.
The identification of highly efficacious functionalised tetrahydrocyclopenta[c]pyrroles as inhibitors of HBV viral replication through modulation of HBV capsid assembly
Pharmacokinetic optimisation of the clinical candidate HBV capsid inhibitor AB-506 resulted in dramatic improvements in oral exposure and half-life providing compound 17 which demonstrated low dose QD efficacy in a mouse model of HBV replication.
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism
S2727 (Dacomitinib) was virtually screened out from a compound library via targeting the PC 190723 binding site of FtsZ and its inhibition effect on the functions of FtsZ was demonstrated by biological assays.
Potency and metabolic stability: a molecular hybrid case in the design of novel PF74-like small molecules targeting HIV-1 capsid protein
To achieve balanced potency and metabolic stability profiles, a molecular hybridization approach was used to design a novel PF74-like chemotype 4. Synthesis, SAR and molecular modeling of chemotype 4 are reported.
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from Mycobacterium tuberculosis to overcome kanamycin resistance
Haloperidol analogues were developed as inhibitors of the Mycobacterium tuberculosis resistance enzyme Eis to serve as kanamycin adjuvants.
SF5- and SCF3-substituted tetrahydroquinoline compounds as potent bactericidal agents against multidrug-resistant persister Gram-positive bacteria
Bacteria persister cells are immune to most antibiotics and hence compounds that are active against persister bacteria are needed.
Research Article
N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa
Simultaneous inhibition of metallo-β-lactamases (MBLs) and virulence factors such as LasB from Pseudomonas aeruginosa offers a new approach to combat antibiotic-resistant pathogens.
Influence of ring size in conformationally restricted ring I analogs of paromomycin on antiribosomal and antibacterial activity
Aminoglycosides with conformationally locked side chains and small hydrophobic patches show increased anti-bacterial activity and ribosomal selectivity. Fine tuning of side chain orientation indicates that the gt conformation is ideal for binding.
A niclosamide–tobramycin hybrid adjuvant potentiates cefiderocol against P. aeruginosa
A niclosamide-tobramycin hybrid was shown to synergize with cefiderocol, a recently approved siderophore cephalosporin, against multidrug-resistant Pseudomonas aeruginosa.
Introduction of a cyano group at the 2-position of an (R,S)-3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) derivative of thymine elicits selective anti-HBV activity
The substantial impact of acyclic nucleoside phosphonates (ANPs) on human medicine encourages the synthesis of new ANP analogues with a potentially differentiated antiviral spectrum.
Assessment of the rules related to gaining activity against Gram-negative bacteria
Evaluation of the applicability of Gram-negative activity rules using 16 amino acid modified compounds against a panel of Escherichia coli and its mutant strains.
About this collection
This special cross-journal collection of RSC Medicinal Chemistry and Organic and Biomolecular Chemistry(OBC) is dedicated to the latest synthetic and medicinal chemistry advances in antibiotic and antiviral compounds. The collection is guest edited by Dr Mike Sofia (Arbutus Biopharma) and Professor Xuechen Li (University of Hong Kong) and covers all aspects of the development of antibacterial and antiviral agents, from the discovery of novel agents to mechanistic studies, delivery approaches, resistance studies or structural studies on target-drug interactions.
New articles will be added to the collection upon publication. Please return to this page frequently to see the collection grow.