New trifluoropropanone sulfides as highly active and selective inhibitors of insect juvenile hormone esterase

Synthesis of novel β-dialkylamino-α,β-unsaturated trifluoromethylketones containing cyclobutene fragment and their reactions with organolithium and Grignard reagents

“…Found: C,59.90;H,5.85;F,21.84;N,5.47. C 13 H 18 F 3 NO requires: C,59.76;H,6.94;F,21.81;N,5.36%. 8,48.2,45.7,46.4,37.6,30.4,29.3,14.5,13.7.…”

“…IR (mineral oil) 3001, , 1150 4.3. General procedure for preparation 1,2-addition products (5)(6)(7)(8) and 1,4-addition products (9-16) (a) From organolithiums. To the stirred solution or suspension of organolithium (0.007 mol) in THF (7 mL) at À70 C the solution of one of enaminoketones 2, 3 (0.006 mol) in THF (2 mL) was added dropwise.…”

“…Such ketones have been used as the starting compounds in a variety of heterocyclic synthesis 1- 3 and have also been viewed as a target objects because of their possible biological activity. 4,5 Of particular value are b-dialkylaminoa,b-unsaturated trifluoromethylketones since they are not only precursors for heterocyclizations, but, as it was shown recently, are also useful compounds in cross-coupling processes with organolithium and Grignard reagents. This very effective approach was studied only on the examples of the simplest acyclic trifluoroenaminoketones.…”

Purification and characterization of neuropathy target esterase (NTE) from rat brain

“…The inhibitor was prepared in our laboratory according to the procedure of Szekacs et al (1989). Aliquots of 1 ml ultrafiltrated sample from previous step containing approximately 116 nmol/min/mg protein NTE activity in 50 mM Tris-HCl, 1 mM EDTA, 1 mM EGTA, 0.01% polyoxyethylene W1, 500 mM NaCl, 250 mM sucrose buffer pH 8.2 were applied to a 20% (w/v) slurry of prewashed gel in a ratio of 1:1 and incubated with a gentle agitation for 20 h at 4°C.…”

Σύνθεση Και Μελέτη Νέων Βιοδραστικών Λιπιδίων

“…Τριφθορομεθυλοκετόνες Πεπτιδικές τριφθορομεθυλοκετόνες έχουν δείξει σημαντική ανασταλτική δράση έναντι σερινοπρωτεασών (χυμοθρυψίνη, ελαστάση,236,237 θρομβίνη, 238 καλλικρεΐνη 239 ). Επίσης, έχουν δοκιμαστεί έναντι εστερασών,240 κυστεϊνοπρωτεασών, 241 μεταλλοπρωτεασών.…”