5650-20-4Relevant articles and documents
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders
Cao, Yang,Zhang, Minjia,Wu, Cindy,Lee, Selina,Wroblewski, Mary Elizabeth,Whipple, Trisha,Nagy, Peter I.,Takács-Novák, Krisztina,Balázs, Attila,Tor?s, Szilárd,Messer Jr., William S.
, p. 4273 - 4286 (2003)
Muscarinic agonists might be useful in the treatment of neurological disorders, including Alzheimer's disease, schizophrenia, chronic pain, and drug abuse. Previous studies identified a series of bis-1,2,5-thiadiazole derivatives of 1,2,5,6-tetrahydropyridine with high activity and selectivity for muscarinic receptors. To develop compounds with improved central nervous system penetration, several new derivatives were synthesized and characterized for muscarinic receptor binding and activity. One ligand (11) exhibited agonist activity at M1, M2, and M4 receptors, a selectivity profile suggesting potential utility in the treatment of schizophrenia.
Formation of macrocyclic ethers by free radical cyclization: Effects of chain length, substituents, and solvents
Philippen, Annie,Degueil-Castaing, Marie,Beckwith, Athelstan L. J.,Maillard, Bernard
, p. 6814 - 6819 (2007/10/03)
Free radical reduction by tributylstannane of w-iodopolyoxaalkyl acrylates derived from tri-, tetra-, penta-, hexa-, and heptaethylene glycols gives mixtures of uncyclized reduction products and macrocyclic ethers formed by endo cyclization. The rate constants for cyclization of the intermediate radicals at 80 °C in benzene were determined under carefully defined conditions to be 15 × 104,13 ×104,5.1 × 104,10 × 104 and 3.6 × 104 s-1, for formation of the 12-, 15-, 18-, 21- and 24-membered rings, respectively. These values indicate that the presence of oxygen atoms in the chains increases the rate by a factor of 10-30 by comparison with the previously reported cyclization of alkenyl species. The rate constants at 80 °C in benzene and the endo/exo ratio for reductive cyclizations of the methacrylate, crotonate, cinnamate, maleate, and fumarate esters of 8-iodo-3,6-dioxaoctanol have been determined. The reduction of the 8-iodo-3,6-dioxaoctyl acrylate in solvents of varying polarity indicated that the cyclization rate has a relatively low solvent dependence.
Hydrophilic Lipids
Heimann, Ulrich,Voegtle, Fritz
, p. 858 - 862 (2007/10/02)
The new triesters of glycerol 1-8 with different oligoethylene glycol carboxylic acids ("hydrophilic lipids") have been synthesized and their complexation with alkali and alkaline earth metal cations has been investigated.
