- Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI
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A series of novel benzimidazole diamidines were prepared from the corresponding dicyano analogues either by applying Pinner methodology (5a–c, 10 and 13a) or by making amidoximes intermediates that were reduced to the corresponding amidines (15a–c). The n
- Farahat, Abdelbasset A.,Bennett-Vaughn, Cheree,Mineva, Ekaterina M.,Kumar, Arvind,Wenzler, Tanja,Brun, Reto,Liu, Yang,Wilson, W. David,Boykin, David W.
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p. 5907 - 5910
(2016/12/03)
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- Syntheses of dual-radioisotope-labeled CP-I, a GABAA receptor partial agonist
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CP-I is a potent subtype-selective GABAA receptor partial agonist. Owing to its significant metabolic cleavage at C8 observed in preliminary biotransformation studies with non-radiolabeled CP-I, the syntheses of CP-I labeled at the right or left hand side with 14C or labeled with 3H at the right hand side were required. The two compounds labeled with 14C at the left or right hand side were synthesized in 2 and 5 radio-synthetic steps using [14C]2-chloroacetyl chloride and [ 14C]NaCN as starting radiolabeled materials, respectively. CP-I was labeled with tritium at the right hand side by a tritium de-halogenation method. Batches of radiolabeled CP-I were mixed to give dual-radioisotope-labeled CP-I. An efficient approach to [14C]fluoropyridinyl imidazole was developed, and a short synthesis of iodo-substituted fluoropyridinyl imidazole was also achieved. The details of these syntheses are discussed. Copyright
- Zhang, Yinsheng,Greenfield, Laura,Hong, Yang
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p. 411 - 417
(2012/07/13)
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- BASIC AMINE COMPOUND AND USE THEREOF
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Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A 1 and A 2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH 2 , C(=O), NR 11 , or CHR 35 and D represents a group represented by the following formula (6): where Q represents a single bond, NR 12 , or a group represented by the formula (13): and Y represents a group represented by the following formula (7) : where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents -NR 25 R 26 ; and R 1 to R 26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.
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Page/Page column 23
(2010/11/24)
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- Benzimidazole and pyridylimidazole derivatives
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This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
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- Synthesis of some new 2-substituted-phenyl-1H-benzimidazole-5-carbonitriles and their potent activity against Candida species
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New 2-substituted-phenyl-1H-benzimidazole-5-carboxylic acids (35, 38), ethyl-5-carboxylate (36), -5-carboxamides (37, 39),-5-carboxaldehyde (42), -5-chloro (40), -5-trifluoromethyl (41), and -5-carbonitriles (44-53, 55-67), -6-carbonitrile (54) were prepa
- G?ker, Hakan,Ku?, Canan,Boykin, David W.,Yildiz, Sulhiye,Altanlar, Nurten
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p. 2589 - 2596
(2007/10/03)
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- Synthesis and antimicrobial activity of some new 2-phenyl-N-substituted carboxamido-1H-benzimidazole derivatives
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Some 1H-benzimidazole-carboxamide derivatives were prepared and their antimicrobial activities against Staphyloccus aureus, Escherichia coli and Candida albicans evaluated. Compounds 18, 22, and 25 exhibited the best activity against Candida albicans.
- Goeker, Hakan,Tuncbilek, Meral,Suezen, Sibel,Kus, Canan,Altanlar, Nurten
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p. 148 - 152
(2007/10/03)
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