Publications by authors named "Gregory Adrian Gunawan"

Article Synopsis
  • Mycobacterial bioenergetics is a promising target for new anti-tuberculosis drugs due to its importance in energy generation and bacteria survival.
  • The study involved modifying naphthoquinoneimidazoles by adding a trialkylphosphonium cation to enhance their antimycobacterial activity through changes in the structure.
  • The most effective compound showed a strong selectivity index and bactericidal action by causing rapid depolarization of bacterial membranes, leading to decreased ATP levels and maintaining excellent antibacterial properties.
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Peptide-derived cyclophanes inhabit a unique niche in the chemical space of macrocyclic peptides with several examples of pharmaceutical importance. Although both synthetic and biocatalytic methods are available for constructing these macrocycles, versatile (bio)catalysts able to incorporate a variety of amino acids that compose the macrocycle would be useful for the creation of diverse peptide cyclophanes. In this report, we synergized the use of bioinformatic tools to map the biosynthetic landscape of radical SAM enzymes (3-CyFEs) that catalyze three-residue cyclophane formation in the biosynthesis of a new family of RiPP natural products, the triceptides.

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Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility. Potent activity could be achieved without the carboxamide linker but not in the absence of the indole ring.

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