59832-12-1Relevant articles and documents
Synthesis of Benzo[4,5]imidazo[2,1-b]thiazole by Copper(II)-Catalyzed Thioamination of Nitroalkene with 1H-Benzo[d]imidazole-2-thiol
Jana, Sourav,Chakraborty, Amrita,Shirinian, Valerii Z.,Hajra, Alakananda
supporting information, p. 2402 - 2408 (2018/05/08)
A Copper(II)-catalyzed thioamination of β-nitroalkene with 1H-benzo[d]imidazole-2-thiol has been developed for the synthesis of benzo[4,5]imidazo[2,1-b]thiazole derivatives. A variety of N-fused benzoimidazothiazole derivatives are obtained in high yields through successive C?N and C?S bond formations. This protocol is also applicable to β-substituted β-nitroalkenes to afford 2,3-disubstituted benzoimidazothiazoles. (Figure presented.).
Development of a rationally designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administration
Rothman, Richard B.,Blough, Bruce E.,Woolverton, William L.,Anderson, Karen G.,Negus, S. Stevens,Mello, Nancy K.,Roth, Bryan L.,Baumann, Michael H.
, p. 1361 - 1369 (2007/10/03)
Convergent lines of evidence support a dual deficit model of stimulant withdrawal, where reductions in synaptic dopamine (DA) and 5-hydroxytryptamine (serotonin) (5-HT) contribute to dysphoria, drug craving, and relapse. Thus, we predicted that a nonamphetamine compound with substrate activity at DA and 5-HT transporters (i.e., a dual DA/5-HT releaser) would be an effective medication for treating stimulant addictions. Ideally, this type of medication would alleviate withdrawal symptoms, suppress cocaine self-administration, and lack side effects commonly associated with central nervous system stimulants. In the present work, more than 350 compounds were screened in vitro for activity as substrate-type releasing agents at DA, 5-HT, and norepinephrine transporters. These efforts identified PAL-287 (1-napthyl-2-aminopropane) as a nonamphetamine compound with potent substrate activity at biogenic amine transporters. In vivo microdialysis in rats demonstrated that PAL-287 (1-3 mg/kg i.v.) increased extracellular DA and 5-HT in frontal cortex, but effects on 5-HT were somewhat greater. PAL-287 induced substantially less locomotor stimulation than (+)-amphetamine, a drug that increases only extracellular DA. Administration of high-dose (+)-methamphetamine or (±)-3,4-methylenedioxymethamphetamine to rats produced long-lasting depletion of cortical 5-HT, whereas PAL-287 (18 mg/kg i.p. × 3) did not. PAL-287 displayed little or no reinforcing properties in rhesus monkeys trained to self-administer cocaine, yet PAL-287 produced a dose-dependent decrease in responding for cocaine when infused at a dose of 1.0 mg/kg/h. Collectively, the findings reported here demonstrate that nonamphetamine monoamine releasing agents such as PAL-287 might be promising candidate medications for the treatment of stimulant dependence.
Cycloaddition of Isocyanides with 1-Aryl-2-nitro-1-propenes, Methyl 2-Nitro-3-arylpropenoates, and Methyl 2-Nitro-2,4-pentadienoates. Synthesis of 1-Hydroxyindoles and 1-Hydroxypyrroles
Foucaud, Andre,Razorilalana-Rabearivony, Claudia,Loukakou, Emile,Person, Herve
, p. 3639 - 3644 (2007/10/02)
The cycloadditions of isocyanides with various aryl nitroalkenes have been investigated.When the aryl groups were XC6H4, naphthyl, and 2-pyridinyl, the reactions gave the 1-hydroxyindoles, 1-hydroxybenzoindoles, and 1-hydroxy-7-azaindole.When the ar
