93864-26-7Relevant academic research and scientific papers
Synthesis of Kappa Opioid Antagonists Based on Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence
Scarry, Sarah M.,Lovell, Kimberly M.,Frankowski, Kevin J.,Bohn, Laura M.,Aubé, Jeffrey
, p. 10538 - 10550 (2016/11/17)
The quinoxaline and quinoxalinone family of nitrogen heterocycles is present in molecules of therapeutic relevance for diverse applications ranging from infectious diseases to neuroscience targets. Here, we describe a general synthetic sequence to afford pyrrolo[1,2-α]quinoxalinones from commercially available starting materials and their use in preparing potential kappa opioid receptor antagonists. The biological data obtained from the latter set of compounds is briefly presented and discussed.
KAPPA OPIOID RECEPTOR EFFECTORS AND USES THEREOF
-
Paragraph 00051, (2013/03/28)
The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.
Optically active antifungal azoles: Synthesis and antifungal activity of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-{2-[4-aryl-piperazin-1-yl]-ethyl} -tetrazol-2-yl/1-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol
Upadhayaya, Ram Shankar,Sinha, Neelima,Jain, Sanjay,Kishore, Nawal,Chandra, Ramesh,Arora, Sudershan K.
, p. 2225 - 2238 (2007/10/03)
A series of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-{2-[4-aryl-piperazin-1-yl]- ethyl}-tetrazol-2-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol (11a-n) and (2R,3S)-2-(2,4-difluorophenyl)-3-(5-{2-[4-aryl-piperazin-1-yl]-ethyl} -tetrazole-1-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol (12a-n) has been synthesized. The antifungal activity of compounds was evaluated by in vitro agar diffusion and broth dilution assay. Compounds 11d and its positional isomer 12d having 3-trifluoromethyl substitution on the phenyl ring of piperazine demonstrated significant antifungal activity against variety of fungal cultures (Candida spp. C. neoformans and Aspergillus spp.). The compound 12d showed MIC value of 0.12μg/mL for C. albicans, C. albicans V-01-191A-261 (resistant strain); 0.25μg/mL for C. tropicalis, C. parapsilosis ATCC 22019 and C. krusei and MIC value of 0.5μg/mL for C. glabrata, C. krusei ATCC 6258, which is comparable to itraconazole and better than fluconazole. Further, compound 11d showed significant activity (MIC; 0.25-0.5μg/mL) against Candida spp. and strong anticryptococcal activity (MIC; 0.25μg/mL) against C. neoformans.
POTENTIAL NEUROLEPTICS OF THE ORTHOPRAMIDE SERIES; SYNTHESIS OF N-(3-(TERT.AMINO)PROPYL)-5-SULFAMOYL-2-METHOXYBENZAMIDES
Valenta, Vladimir,Vlkova, Marie,Holubek, Jiri,Svatek, Emil,Metysova, Jirina,Protiva, Miroslav
, p. 797 - 808 (2007/10/02)
Heating ethyl 5-sulfamoyl-2-methoxybenzoate with a series of twelve 3-(tert.amino)propylamines (IIIa-IIIl) afforded the title compounds IIa-IIl which were transformed to salts and subjected to pharmacological screening as potential neuroleptics of the sulpiride series.Only compounds IId (hydrogen oxalate, VUFB-15 453) and IIg (methanesulfonate, VUFB-15 397) showed indications of the desired psychotropic activity.
