- Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity
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NMDA receptors mediate glutamatergic neurotransmission and are therapeutic targets due to their involvement in a variety of psychiatric and neurological disorders. Here, we describe the design and synthesis of a series of (R)-3-(5-furanyl)carboxamido-2-am
- Zhao, Fabao,Atxabal, Unai,Mariottini, Sofia,Yi, Feng,Lotti, James S.,Rouzbeh, Nirvan,Liu, Na,Bunch, Lennart,Hansen, Kasper B.,Clausen, Rasmus P.
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p. 734 - 746
(2022/01/03)
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- Synthesis and SAR of 5-aryl-furan-2-carboxamide derivatives as potent urotensin-II receptor antagonists
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The synthesis and biological evaluation as potential urotensin-II receptor antagonists of a series of 5-arylfuran-2-carboxamide derivatives 1, bearing a 4-(3-chloro-4-(piperidin-4-yloxy)benzyl)piperazin-1-yl group, are described. The results of a systemat
- Lim, Chae Jo,Kim, Nam Hui,Park, Hye Jin,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
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p. 577 - 580
(2019/01/05)
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- Hydroxamic Acids as Potent Inhibitors of FeII and MnII E. coli Methionine Aminopeptidase: Biological Activities and X-ray Structures of Oxazole Hydroxamate-EcMetAP-Mn Complexes
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New series of acids and hydroxamic acids linked to five-membered heterocycles including furan, oxazole, 1,2,4- or 1,3,4-oxadiazole, and imidazole were synthesized and tested as inhibitors against the FeII, CoII, and MnII f
- Huguet, Florian,Melet, Armelle,Alves de Sousa, Rodolphe,Lieutaud, Aurelie,Chevalier, Jacqueline,Maigre, Laure,Deschamps, Patrick,Tomas, Alain,Leulliot, Nicolas,Pages, Jean-Marie,Artaud, Isabelle
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experimental part
p. 1020 - 1030
(2012/07/31)
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- Synthesis of heterocycles from arylation products of unsaturated compounds: XVIII. 5-Arylfuran-2-carboxylic acids and their application in the synthesis of 1,2,4-thiadiazole, 1,3,4-oxadiazole, and [1,2,4]triazolo[3,4-b][1,3,4] thiadiazole derivatives
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Arylation of furan-2-carboxylic acid or its methyl ester with arenediazonium chlorides in the presence of copper(II) chloride gave the corresponding 5-arylfuran-2-carboxylic acids or methyl 5-arylfuran-2- carboxylates. 5-Arylfuran-2-carbonyl chlorides rea
- Gorak,Obushak,Matiichuk,Lytvyn
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experimental part
p. 541 - 550
(2009/08/17)
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- Synthesis and antimicrobial activities of some new triazolothiadiazoles bearing 4-methylthiobenzyl moiety
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A series of substituted triazolothiadiazoles (6a-j and 7a-j) have been synthesized by condensing 4-amino-3-[4-methylthiobenzyl]-4H-1,2,4-triazole-5-thiol (5) with substituted aryl furoic acids/aromatic acids in the presence of POCl3. The triazole (5) was obtained by the fusion of 4-methylthiophenyl acetic acid (4) with thiocarbohydrazide. The structures of newly synthesized compounds are characterized by elemental analysis, IR, 1H NMR and mass spectroscopic studies and were screened for their antimicrobial activities. The preliminary results revealed that some of the compounds exhibited promising antimicrobial activities.
- Prasad, D. Jagadeesh,Ashok, Mithun,Karegoudar, Prakash,Poojary, Boja,Holla, B. Shivarama,Kumari, Nalilu Sucheta
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experimental part
p. 551 - 557
(2009/09/08)
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- Synthesis of some thiadiazolotriazinone derivatives as possible antimicrobial agents
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A series of 7-substituted-3-t-butyl 4(H)-1,3,4-thiadiazolo(2,3-c)-1,2,4- triazine-4-one (3) have been synthesized by condensing 4-amino-6-t-butyl-3- mercapto-1,2,4-triazin-5(4H)-one (1) with substituted Arylfuroic acids (2) using POCl3 as a cyclizing agen
- Prasad, D. Jagadeesh,Karthikeyan,Karegoudar, Prakash B.,Poojary, Boja,Holla, B. Shivarama,Kumari, N. Suchetha
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p. 1083 - 1091
(2008/02/01)
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- Metalloform-selective inhibition: Synthesis and structure-activity analysis of Mn(II)-form-selective inhibitors of Escherichia coli methionine aminopeptidase
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Methionine aminopeptidase (MetAP) is a promising target for development of novel antibacterial, antifungal and anticancer agents. However, its physiologically relevant metal ion remains to be defined, and its inhibitors need to inhibit the in vivo metallo
- Huang, Qing-Qing,Huang, Min,Nan, Fa-Jun,Ye, Qi-Zhuang
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p. 5386 - 5391
(2007/10/03)
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