Sperandina Lappa

Synthesis and structure-activity relationships of new acetylcholinesterase inhibitors: Morpholinoalkylcarbamoyloxyeseroline derivatives

Abstract Several new potent acetylcholinesterase inhibitors have been synthesised as potential drugs for the treatment of Alzheimers disease. Heptylphysostigmine (MF201) is a drug analogue of physostigmine under clinical evaluation. In order to obtain new physostigmine analogues, the methylcarbomoyloxy group was substituted with ω-morpholinoalkylcarbamoyloxy moieties of different chain lengths (C2–C12). Potent in vitro inhibition is seen when the chain length is composed of eight to twelve methylene groups. The inhibitory activity of the C10 and C11 is 7-fold greater with respect to heptylphysostigmine.

Synthesis of inositol phospholipids with thiophosphoester bonds

Abstract the synthesis of phosphatidylinositol (PI) analogues (±)1- O -(1- O -octadecanoyl-2- O -acetyl- rac -3-thioglycerylphosphoryl)- myo -inositol ( 7 ), (±)1- O -(1,2-di- O -octadecyl- rac -3-thioglycerylphosphoryl)- myo -inositol ( 14a ), (±)1- O -(1,2-di- O -octyl- rac -3-thioglycerylphosphoryl)- myo -inositol ( 14b ) and (±)1- O -(1- O -octadecyl-2- O -methyl- rac -3-thioglycerylphosphoryl)- myo -inositol ( 14c ) designed to show a novel mode of PI-phospholipase C (PI-PLC) inhibition, is described.

Synthesis of some thiophosphate analogues (C-S-P) of phosphatidylinositol

Abstract the synthesis of analogues of phosphatidylinositol (PI), designed to show a novel mode of PI-phospholipase C (PI-PLC) inhibition, is described.

Synthesis of some carbamates of myo-inositol

The syntheses are described of the 1-O-carbamoyl (11), 1-O-carbamoyl-2-O-stearoyl (10), 1-O-(acetylcarbamoyl)-2-O-stearoyl (12), 1-O-(heptylcarbamoyl) (13), 2-O-(heptylcarbamoyl) (14) 1,2-di-O-(heptylcarbamoyl) (15), and 1-O-(octadecylcarbamoyl) (16) derivatives of myo-inositol. None of these compounds had significant activity against phospholipase C.

Synthesis and cytotoxic activity of (±) octadecylphosphodithionyl-1-myo-inositol

Abstract the synthesis of the phosphatidylinositol (PI) analogue (±)-octadecylphosphodithionyl-1- myo -inositol is described. The cytotoxic activity on K562 erythroleukaemic cells and the effect on the activity of PI specific phospholipase C (PI-PLC) from human platelets are reported.

Synthesis of (±)-10H-Phenothiazine-10-propanoyl-1′-myo-inositol

Abstract The synthesis of (±)10H-phenothiazine-10-propanoyl-1′-myo-inositol was accomplished in order to test it as inhibitor of phosphatidylinositol specfic phospholipase C (PI-PLC).