Antibacterial Potential of Extracts and Phytoconstituents Isolated from Leaves In Vitro.

(1) Background: Rapidly increasing antibiotic resistance is one of the greatest threats to global health, affecting individuals regardless of age. Medicinal plants are widely used in traditional medicine to prevent and attenuate infectious conditions with minimal adverse effects. However, only a few have been phytochemically investigated for their medicinal properties and subsequent biological activities.

Discovery of a Novel Antimicrobial Agent by the Virtual Screening of a Library of Small Molecules.

A virtual screening approach based upon a combination of docking and pharmacophore methods was utilized on a library of 1.4 million molecules to identify novel antimicrobial agents, which may potentially act via inhibition of the caseinolytic protease. Using this method, compound 6 was found to be bactericidal against three staphylococcal species (minimum inhibitory concentration (MIC)=4-16 μg/mL).

Structure-Based Scaffold Repurposing toward the Discovery of Novel Cholinesterase Inhibitors.

Cholinesterases (ChE) are well-known drug targets for the treatment of Alzheimer's disease (AD). In continuation of work to develop novel cholinesterase inhibitors, we utilized a structure-based scaffold repurposing approach and discovered six novel ChE inhibitors from our recently developed DNA gyrase inhibitor library. Among the identified hits, two compounds (denoted and ) were found to be the most potent inhibitor of acetylcholinesterase (AChE, IC = 6.

Recent advances in DNA gyrase-targeted antimicrobial agents.

Antimicrobial resistance is one of the greatest challenges facing the world today. In the United States alone, it is responsible for the death of more than 20,000 people each year. DNA gyrase, a well-validated drug target, is involved in bacterial DNA replication, repair and decatenation.

Recent update on anti-dengue drug discovery.

Dengue is the most important arthropod-borne viral disease of humans, with more than half of the global population living in at-risk areas. Despite the negative impact on public health, there are no antiviral therapies available, and the only licensed vaccine, Dengvaxia, has been contraindicated in children below nine years of age. In an effort to combat dengue, several small molecules have entered into human clinical trials.

Leptospirosis from water sources.

Leptospirosis outbreaks have been associated with many common water events including water consumption, water sports, environmental disasters, and occupational exposure. The ability of leptospires to survive in moist environments makes them a high-risk agent for infection following contact with any contaminated water source. Water treatment processes reduce the likelihood of leptospirosis or other microbial agents causing infection provided that they do not malfunction and the distribution networks are maintained.