Transformation-Guided Genome Mining Provides Access to Brominated Lanthipeptides.

Natural product biosynthesis is nature's tinkering ground for developing new enzymes that can achieve chemical transformations that are outside the purview of traditional chemical catalysis. Herein we describe a genome mining approach that leads to the discovery of a halogenase that regioselectively brominates a tryptophan side chain indole for a macrocyclic peptide substrate, enabling downstream chemical arylation by Suzuki-Miyaura coupling. The halogenase was found to prefer a macrocyclic peptide substrate over a linear peptide.

Nature's defense against emerging neurodegenerative threats: Dynamic simulation, PCA, DCCM identified potential plant-based antiviral lead targeting borna disease virus nucleoprotein.

The rare zoonotic Borna disease virus (BDV) causes fatal neurological disease in various animals, with a high mortality rate exceeding 90% in central Europe. However, unlike most viruses, it establishes persistent infections within the host cell nucleus, hindering treatment. As successful BDV treatments remain elusive, the researchers turned to a computational approach, utilizing molecular docking, ADME/T, post-docking MMGBSA, MD simulation, DCCM, and PCA to identify promising phytochemical drug candidates targeting the BDV Nucleoprotein (PDB ID: 1N93).

Toxic Effects of Lead Exposure on Freshwater Climbing Perch, , and Bioremediation Using Leaf Powder.

The acute and chronic toxicity of lead to was determined in this study using static replacement bioassay testing. During the chronic toxicity studies, an experiment on the bioremediation of lead toxicity using leaf powder was conducted. The 96 h LC values of lead for was 1.

Recent advancements in the quest of benzazoles as anti-Mycobacterium tuberculosis agents.

Tuberculosis (TB) remains a global health challenge, claiming numerous lives each year, despite recent advancements in drug discovery and treatment strategies. Current TB treatment typically involves long-duration chemotherapy regimens that are often accompanied by adverse effects. The introduction of new anti-TB drugs, such as Bedaquiline, Delamanid, and Pretomanid, offers hope for more effective treatment, although challenges persist keeping the quest to find new anti-TB chemotypes an incessant exercise of medicinal chemists.

"On Water" Cationic Ruthenium(II) Catalysed Direct Aryl C(sp)-H Amidation of Biorelevant Heterocyclic Scaffolds.

Ru(II)-Catalyzed "On Water" direct aryl C(sp)-H amidation of 2-arylbenzo[d]-thiazole/oxazole with acyl azide is reported under silver-free condition. Deuterium scrambling experiments suggested reversible C-H activation catalyzed by active cationic ruthenium species. The organic solvents such as DCE, DMF, DMSO, MeCN, dioxane, and PhMe were not conducive for the C-H amidation except for PhCl in which case, however, inferior yield (31 %) was obtained.