Total Synthesis of the Four Stereoisomers of Cyclo(l-Trp-l-Arg) Raises Uncertainty of the Structures of the Natural Products and Invalidates Their Promising Antimicrobial Activities

Article Biochemistry & Molecular Biology

Valorisation of the diterpene podocarpic acid-Antibiotic and antibiotic enhancing activities of polyamine conjugates

Steven A. Li et al.

Summary: A series of podocarpic acid-polyamine conjugates were synthesized for antimicrobial research, leading to the discovery of two derivatives with potent growth inhibitory effects on Staphylococcus aureus and Cryptococcus neoformans. Some analogues also showed antibiotic adjuvant properties in the presence of sub-therapeutic amounts of doxycycline or erythromycin. However, cytotoxicity and hemolytic properties were observed for certain compounds, highlighting the importance of structural requirements and lipophilicity for antimicrobial activity.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Medicinal

Spermine Derivatives of Indole-3-carboxylic Acid, Indole-3-acetic Acid and Indole-3-acrylic Acid as Gram-Negative Antibiotic Adjuvants

Melissa M. Cadelis et al.

Summary: The discovery of new antibiotic adjuvants is crucial for combating antimicrobial resistance. Some newly discovered compounds show good antibiotic adjuvant activities with lower cytotoxic and haemolytic properties, indicating their potential for further development as treatment options.

CHEMMEDCHEM (2021)

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Review Chemistry, Multidisciplinary

Towards the sustainable discovery and development of new antibiotics

Marcus Miethke et al.

Summary: There is a growing demand for novel antimicrobials to treat infections caused by multidrug-resistant bacterial pathogens, but there is currently a lack of investment in this field. New agents with innovative chemistry and modes of action are urgently needed to combat the public health threat posed by antimicrobial resistance. The consortium proposes short-term and long-term solutions to overcome urgent limitations in research and funding, aiming to bridge the gap between academic, industrial, and political stakeholders to improve the ability to discover and develop new antibiotics.

NATURE REVIEWS CHEMISTRY (2021)

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Review Infectious Diseases