It is herein described the synthesis of a series of thirty novel 1,2,3-triazole-1,4 disubstituted compounds inspired on the known SRPKs inhibitor N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide (SRPIN340) and biological evaluation of them against human glioblastoma multiforme cell line U87MG. Starting with 1-fluoro-2 nitro-4-(trifluoromethyl)benzene (1), the substances were prepared via a five-step synthetic route. The crucial step corresponded to the copper-catalyzed cycloaddition reaction between trifluoromethyl phenyl azides and different alkynes. In general, the compounds were obtained with good yields and they were characterized utilizing spectroscopic (IR and NMR) and spectrometric (HRMS) techniques. The evaluation of the synthesized compounds at three different treatment time (24 h, 48 h, and 72 h) and concentrations (50, 100, and 150 µmol L-1) revealed that five derivatives were capable of reducing cell viability by 50% after 72 h of treatment at the highest concentration. On the contrary, three derivatives significantly increased cell viability being this effect more pronounced after 48 h of treatment. In this regard, it stands out the compound 2-((1-(2-morpholino-5-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)isoindoline-1,3-dione (7) which increased cell viability in approximately 300% after 48 h of treatment at 100 µmol L-1. The substances that increased cell viaiblity present as common structural features the presence of a saturated nitrogen-containing six-membered ring and carbonylated fragments.

The demand for new insecticides is increasing due to the appearance of insect populations that are resistant to currently used products. New insecticides should be efficient in controlling pests and present low toxicity to non-target organisms. Ascia monuste (Lepidoptera: Pieridae) is a destructive pest of cole vegetables, and the fire ant Solenopsis saevissima (Hymenoptera: Formicidae) is an important predator of these caterpillars in brassica crops. Tetragonisca angustula (Hymenoptera: Apidae) is very important in pollinating many plants and providing honey. Therefore, this study evaluated the toxicity of synthetic amides to A. monuste and its selectivity in favor of S. saevissima and T. angustula. The amides (2E,4E)-N-propylhexa-2,4-dienamide (3) and (2E, 4E)-N-butylhexa-2,4-dienamide (4) caused high (96 and 93%, respectively) and fast (48 h) mortality of A. monuste. The amides 3 and 4 were not harmful to the predator (mortality of 5.7% for amide 3 and 7.14% for amide 4) and were slightly harmful to the pollinator (mortality of 38.57% for amide 3 and 28.12% for amide 4). The amides 3 and 4 are promising, as insecticides, due to the high and rapid mortality of A. monuste with low and moderate toxicity to S. saevissima and T. angustula, respectively.