Leupyrrins are highly potent antifungal agents. A structure-activity-relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified leupylogs that incorporate a stable and readily available aromatic side chain. For their synthesis a concise strategy is described that enables a short and versatile access.
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http://dx.doi.org/10.1002/chem.202002622 | DOI Listing |
Nanomicro Lett
January 2025
CAS Key Laboratory of Organic Solids, Institute of Chemistry, Beijing National Laboratory for Molecular Sciences, Chinese Academy of Sciences, Beijing, 100049, People's Republic of China.
Finding ways to produce dense and smooth perovskite films with negligible defects is vital for achieving high-efficiency perovskite solar cells (PSCs). Herein, we aim to enhance the quality of the perovskite films through the utilization of a multifunctional additive in the perovskite anti-solvent, a strategy referred to as anti-solvent additive engineering. Specifically, we introduce ortho-substituted-4'-(4,4″-di-tert-butyl-1,1':3',1″-terphenyl)-graphdiyne (o-TB-GDY) as an AAE additive, characterized by its sp/sp-cohybridized and highly π-conjugated structure, into the anti-solvent.
View Article and Find Full Text PDFMol Divers
January 2025
Department of Chemistry, National Institute of Technology Calicut, Kozhikode, 673601, Kerala, India.
Quinoline is a highly privileged scaffold with significant pharmacological potential. Introducing a carbonyl group into the quinoline ring generates a quinolone ring, which exhibits promising biological properties. Incorporating a carboxamide linkage at different positions within the quinoline and quinolone frameworks has proven an effective strategy for enhancing pharmacological properties, particularly anticancer potency.
View Article and Find Full Text PDFThe gut microbiome is a complex system that directly interacts with and influences many systems in the body. This delicate balance of microbiota plays an important role in health and disease and is highly influenced by lifestyle factors and the surrounding environment. As further research emerges, understanding the full potential of the gut microbiome and the impact of using nutraceuticals to positively influence its function may open the door to greater therapeutic outcomes in the treatment and prevention of disease.
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2025
Department of Molecular Biology and Microbiology, Case Western Reserve University School of Medicine, Cleveland, Ohio, USA.
Foremost in the design of new β-lactamase inhibitors (BLIs) are the boronic acid transition state inhibitors (BATSIs). Two highly potent BATSIs being developed are S02030 and MB076 strategically designed to be active against cephalosporinases and carbapenemases, especially KPC. When combined with cefepime, S02030 and MB076 demonstrated potent antimicrobial activity against laboratory and clinical strains of expressing a variety of class A and class C β-lactamases, including and .
View Article and Find Full Text PDFJ Infect Dis
January 2025
Gilead Sciences, Inc., 333 Lakeside Dr., Foster City, CA, 94404 USA.
Background: Lenacapavir is a highly potent first-in-class inhibitor of HIV-1 capsid approved for the treatment of heavily treatment-experienced (HTE) people with HIV-1 (PWH) harboring multidrug resistant (MDR) virus, in combination with an optimized background regimen (OBR). Resistance analyses conducted after 2 years of lenacapavir treatment in the phase 2/3 CAPELLA study are described.
Methods: CAPELLA enrolled viremic HTE PWH with resistance to 2 or more drugs per class in at least 3 of the 4 main drug classes.
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