New phosphorous-containing lead structures against drought stress in crops interacting with RCAR/(PYR/PYL) receptor proteins were identified starting from in-depth SAR studies of related sulfonamide lead structures and protein docking studies. A converging 6-step synthesis via phosphinic chlorides and phosphono chloridates as key intermediates afforded envisaged tetrahydroquinolinyl phosphinamidates and phosphonamidates. Whilst tetrahydroquinolinyl phosphonamidates 13a,b exhibited low to moderate target affinities, the corresponding tetrahydroquinolinyl phosphinamidates 12a,b revealed confirmed strong affinities for RCAR/ (PYR/PYL) receptor proteins in Arabidopsis thaliana on the same level as essential plant hormone abscisic acid (ABA) combined with promising efficacy against drought stress in vivo (broad-acre crops wheat and canola).

从有关磺酰胺前导结构的深入SAR研究和蛋白质对接研究开始，鉴定了与RCAR /（PYR / PYL）受体蛋白相互作用的农作物抗干旱胁迫的新含磷前导结构。通过次膦酰氯和膦酰氯作为关键中间体的聚合的6步合成提供了设想的四氢喹啉基次膦酸酯和次膦酸酯。虽然四氢喹啉基膦酰胺基膦酸酯13a，b表现出低至中等的靶亲和力，但相应的四氢喹啉基膦酰胺基膦酸酯12a，b揭示了已证实的拟南芥中RCAR /（PYR / PYL）受体蛋白的亲和力与必需植物激素脱落酸（ABA）相同，并具有对抗体内干旱胁迫的有效功效（大面积作物小麦和油菜籽）。