Phosphine-Catalyzed Domino Benzannulation: An Efficient Method to Construct Biaryl Skeletons

The first phosphine-catalyzed domino benzannulation reaction to prepare a variety of functionalized biaryls from allenoates and dienic sulfones is developed

Phosphine-Catalyzed Domino Reaction: An Efficient Method for the Synthesis of Bicyclo[3.2.0]heptenes Skeleton

Dienic sulfones and γ-CH₃ allenoates can be converted into bicyclo[3.2.0]heptene derivatives in moderate to good yield using trimethylphosphine as the catalyst under mild conditions

Phosphine-Catalyzed Domino Benzannulation: An Efficient Method to Construct Biaryl Skeletons

The first phosphine-catalyzed domino benzannulation reaction to prepare a variety of functionalized biaryls from allenoates and dienic sulfones is developed

The face images of one subject in the AR database.

<p>The face images of one subject in the AR database.</p

Rates of classification errors of the methods on the ORL database (%).

<p>Rates of classification errors of the methods on the ORL database (%).</p

Asymmetric Formal [4 + 2] Annulation of <i>o</i>‑Quinone Methides with β‑Keto Acylpyrazoles: A General Approach to Optically Active <i>trans</i>-3,4-Dihydrocoumarins

An asymmetric cascade reaction between β-keto acylpyrazoles and <i>o</i>-quinone methides in a formal [4 + 2] fashion to access potentially pharmacological active <i>trans</i>-3,4-dihydrocoumarins has been achieved efficiently by using a quinine-based chiral squaramide as the catalyst. The desired products were obtained in high yields with excellent diastereo- and enantioselectivities (up to 96% yield, >19/1 dr and 96% ee) under mild reaction conditions

Rates of classification errors of the methods on the FERET database (%).

<p>Rates of classification errors of the methods on the FERET database (%).</p

Rates of classification errors of the methods on the AR database (%).

<p>Rates of classification errors of the methods on the AR database (%).</p

Discovery of Novel Acetohydroxyacid Synthase Inhibitors as Active Agents against <i>Mycobacterium tuberculosis</i> by Virtual Screening and Bioassay

Acetohydroxyacid synthase (AHAS) has been regarded as a promising drug target against <i>Mycobacterium tuberculosis</i> (MTB) as it catalyzes the biosynthesis of branched-chain amino acids. In this study, 23 novel AHAS inhibitors were identified through molecular docking followed by similarity search. The determined IC₅₀ values range from 0.385 ± 0.026 μM to >200 μM against bacterium AHAS. Five of the identified compounds show significant in vitro activity against H37Rv strains (MICs in the range of 2.5–80 mg/L) and clinical MTB strains, including MDR and XDR isolates. More impressively, compounds <b>5</b> and <b>7</b> can enhance the killing ability against macrophages infected pathogen remarkably. This study suggests our discovered inhibitors can be further developed as novel anti-MTB therapeutics targeting AHAS