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Synthesis and antiarrhythmic properties of N-acylamino derivatives of 1,6,7-substituted 1,2,3,4-tetrahydroisoquinoline-4-spirocyclopentanes and their analogs

“…This investigation continues our previous search for compounds possessing antiarrhythmic activity among the derivatives of 4-spiro-substituted 1,2,3,4-tetrahydroisoquinolines (THIQs) [1,2]. A series of 1,6,7-substituted 4-spirocyclopentane-tetrahydroisoquinolines (IV -XIII) containing acyl groups at the nitrogen atom of the heterocycle has been synthesized and tested for antiarrhythmic properties.…”

“…The antiarrhythmic activity of the synthesized compounds (VIII -XIII and XVIII -XX) was studied on a group of 170 narcotized male and female mongrel rats weighing 180 -220 g with model arrhythmia caused by intravenous injections of aconitine (30 mg/kg) or calcium chloride (200 mg/kg, 10% aqueous solution) [1]. The test substances (2.5 and 5 mg/kg) and the reference drugs isotopin (2.5 mg/kg) and novocainamide (40 mg/kg) were introduced into the femoral vein by single injections 2 -3 min before introducing the arrhythmogenic agents.…”

Enantioselective Total Synthesis of (+)-Monocerin, a Dihydroisocoumarin Derivative with Potent Antimalarial Properties

“…The crude residue was purified by column chromatography on silica gel (60% EtOAc in hexane) to give MOM protected lactone 10a (300 mg, 95%) as a yellow amorphous solid. 2,152.9,137.5,131.1,104.2,97.4,95.1,83.7,76.6,60.8,56.1,55.2,40.4,21.2;LRMS (ESI) 4,152.8,132.14,129.8,104.4,98.0,95.2,86.4,75.4,60.8,56.0,55.2,39.3,21.4;LRMS (ESI) 5,153.1,138.0,129.9,103.8,86.0,71.5,60.8,56.1,40.2,25.3,17.7,LRMS (ESI) 3,152.7,137.5,131.7,104.6,97.9,85.2,73.7,60.7,56.0,43.1,25.4,21.2,17.8, 2, 137.9, 129.3, 103.5, 93.9, 84.6, 74.0, 71.4, 67.0, 60.8, 58.9, 56.1, 37.4; LRMS (ESI) 379.4 [M+Na] + .…”

“…1,2 These natural products exhibit a wide range of biological properties including antifungal, insecticidal, antiparasitic, and plant pathogenic activity. 3,4,5 Monocerin (1, Figure 1), which was first isolated by Aldridge and Turner from Exserohilum monoceras (Drechsler), is a dihydroisocoumarin natural product which protects wheat against the powdery mildew, Erysiphe graminis. 6 Aldridge and Turner also demonstrated monocerin's antifungal properties.…”

Been There, Done That, Bought the T-Shirt: Beşiktaş Fans and the Commodification of Football in Turkey

“…32 This framework can help open up aspects of how such "new kinds of experience" are often reported by Ç arşı fans, as intimated by Alen Markaryan, who notes: "I use the pure power and potential of the terraces to do something for the good of humanity, the Child Care Foundation, the Red Crescent, and making oppressed people's voices heard around the whole world; and I am successfully supporting my team." 33 The talk is of harnessing the power of a group of people in the football stadium, not for any commercial ends but for the basic "good of humanity." Regardless of its integration with commercial and consumption networks, those within Ç arşı focus on the educational and transformative power of the group.…”