DataSheet1_Design, synthesis and antifungal activity of novel 1,4-benzoxazin-3-one derivatives containing an acylhydrazone moiety.doc

A series of 1,4-benzoxazin-3-one derivatives containing an acylhydrazone moiety were designed, synthesized and evaluated for their in vitro antifungal activities against Gibberella zeae, Pellicularia sasakii, Phytophthora infestans, Capsicum wilt, and Phytophthora capsica. The structures of target compounds were characterized by 1H NMR, 13H NMR, 19F NMR and HRMS. The preliminary antifungal evaluation of all target compounds showed that some target compounds possessed moderate to good activities against G. zeae, P. sasakii, P. infestans and C. wilt. Among them, compounds 5L and 5o exhibited noticeable inhibition effects against G. zeae with the EC50 values (effective concentration for 50% activity) of 20.06 and 23.17 μg/ml, respectively, which were even nearly double effective than that of hymexazol (40.51 μg/ml). Meanwhile, compound 5q displayed a notable inhibitory effect toward P. sasakii, with the EC50 value of 26.66 μg/ml, which was better than that of hymexazol (32.77 μg/ml). In addition, compound 5r yielded the EC50 value of 15.37 μg/ml against P. infestans, which was less than those of hymexazol (18.35 μg/ml) and carbendazim (34.41 μg/ml). Eventually, compound 5p showed higher inhibitory effect against C. wilt, with EC50 value of 26.76 μg/ml, which was better than that of hymexazol (>50 μg/ml).</p

<i>N</i>‑Heterocyclic Carbene-Catalyzed Regio- and Enantioselective C7-Alkylation of 4‑Aminoindoles with α‑Bromoenals

The first carbene-catalyzed regio- and enantioselective indole C7-alkylation reaction between 4-aminoindoles and α-bromoenals is disclosed. The corresponding indole products could be obtained in moderate to good yields with good to excellent enantioselectivities. The evaluation of antibacterial activity against Psa revealed that nine of the C7-functionalized indoles exhibited superior inhibitory activities compared to the positive controls TC and BT. Our approach provides an efficient strategy to introduce a chiral chain into the C7 position of indole compounds, with potential applications evaluated in pesticide development

Synthesis and Antiviral Activity of Novel <i>α</i>-Aminophosphorus Containing Benzofuran Moiety

<div><p>GRAPHICAL ABSTRACT</p><p></p></div

Design, Synthesis, and Antiviral Activity of α-Aminophosphonates Bearing a Benzothiophene Moiety

<div><p></p><p>A series of α-aminophosphonates containing a benzothiophene moiety was designed and synthesized. All synthesized compounds were confirmed by ¹H NMR, ¹³C NMR, ³¹P NMR, infrared spectroscopy, and elemental analysis. <i>The half-leaf method was used to determine the in vivo efficacy of</i> α-aminophosphonates bearing a benzothiophene moiety <i>against the tobacco mosaic virus (TMV). Bioassay results showed that all compounds exhibited certain anti-TMV activity at 500 μg/mL concentration. Compound <b>2f</b> exhibited a curative effect of up to 48.1%</i> against TMV, which was almost similar to that obtained from the standard ningnanmycin (51.9%).</p> <p>[Supplementary materials are available for this article. Go to the publisher's online edition of <i>Phosphorus, Sulfer, and Silicon and the Related Elements</i> for the following free supplemental files: Additional text, figures, and tables.]</p> </div