Category: 189329-94-0

Ondachi, Pauline W. published the artcileSynthesis, Nicotinic Acetylcholine Receptor Binding, and in Vitro and in Vivo Pharmacological Properties of 2′-Fluoro-(substituted thiophenyl)deschloroepibatidine Analogues, Recommanded Product: 5-Bromothiophene-3-carboxamide, the main research area is nicotinic receptor binding fluoro thiophenyldeschloroepibatidine analog preparation nicotine dependence; in vitro/in vivo studies; nAChR antagonist; nicotine receptors; α4β2- and α3β4-nAChR.

The synthesis, nAChR in vitro and in vivo pharmacol. properties of 2′-fluoro-3′-(substituted thiophenyl)deschloroepibatidine analogs are presented herein. All had subnanomolar affinity at α4β2*-nAChRs. Contrary to lead structure epibatidine, a potent nAChR agonist, all were potent α4β2- and α3β4-AChR antagonists in an in vitro functional assay. In vivo, the compounds were also nAChR antagonists with various degrees of agonist activity. Many of the compounds had no agonist effects in the tail-flick, hot-plate, hypothermia, or spontaneous activity tests, whereas others did not have agonist activity in the tail-flick and hot-plate tests but like varenicline, were agonists in the hypothermia and spontaneous activity tests. Compound 4-(5-(7-azabicyclo[2.2.1]hept-2-yl)-2-fluoropyridin-3-yl)thiophene-2-carboxamide had agonist activity in all four in vivo tests. All the compounds were antagonists of nicotine-induced antinociception in the tail-flick test and most were antagonists of nicotine-induced antinociception in the hot-plate test. Compound 2-[5-(4-chlorothiophen-2-yl)-6-fluoropyridin-3-yl]-7-azabicyclo[2.2.1]heptane which had a Ki = 0.86 nM in the binding assay similar potency at α4β2/α3β4 with selectivity relative to α7 nAChRs, AD50 value of 0.001 μg/kg in the tail-flick test with no agonist activity in the in vitro or in vivo test had one of the more interesting profiles.

ACS Chemical Neuroscience published new progress about Drug dependence (treatment). 189329-94-0 belongs to class amides-buliding-blocks, name is 5-Bromothiophene-3-carboxamide, and the molecular formula is C5H4BrNOS, Recommanded Product: 5-Bromothiophene-3-carboxamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Rottlander, Mario published the artcileMultiple cross-coupling reactions of aryl and benzylic zinc halides with aryl halides and triflates in solid-phase synthesis of polyfunctional aromatics, Formula: C5H4BrNOS, the main research area is aryl zinc halide aryl halide coupling; benzyl zinc halide aryl triflate coupling; cross coupling solid phase aryl halide; benzene solid phase synthesis.

Aryl and benzylic zinc bromides undergo efficient Pd(0)-catalyzed cross-coupling reactions on the solid-phase using either Rink or Wang resin. By performing the cross-couplings with the multi-coupling reagents 4-BrZnCH2C6H4O2CCF3 and 4-BrZnC6H4OSi(CHMe2)3, two successive C-C bond forming reactions are possible on the solid-phase.

Synlett published new progress about Aryl halides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 189329-94-0 belongs to class amides-buliding-blocks, name is 5-Bromothiophene-3-carboxamide, and the molecular formula is C5H4BrNOS, Formula: C5H4BrNOS.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics