Characterization and computational studies of 2-(benzamido) thiazol-5-yl benzoate
- Odame, Felix, Hosten, Eric C, Betz, Richard, Lobb, Kevin A, Tshentu, Zenixole R
- Authors: Odame, Felix , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447003 , vital:74576 , xlink:href="https://doi.org/10.1134/S0022476619010190"
- Description: Thiazoles have shown a broad range of biological activities and are found in many potent biologically active molecules such as Sulfathiazol (antimicrobial drug), Ritonavir (antiretroviral drug), Abafungin (antifungal drug), and Tiazofurin (antineoplastic drug) [1]. They have exhibited some degree of plant growth regulatory and antifungal activities [2], whilst some thiazoles have shown anti-infective [3] as well as antibacterial activities [4]. The regio-controlled synthesis of 2,5-disubstituted and 2,4,5-trisubstituted thiazoles from ethyl-2-bromo-5-chloro-4-thiazolecarboxylates using sequential palladium-catalyzed coupling reactions has been reported [5]. An efficient general method for the preparation of 2,4-di- and trisubsituted thiazoles is via P–TsOH. H2O-Catalyzed cyclization of trisubstituted propargylic alcohols with thioamides has been accomplished with moderate to excellent product yields under mild and standard conditions [6]. In the presence of triethylamine, (Z)-(2-acetoxyl-1-alkenyl) phenyl-λ3 iodanes reacts with thioureas or thioamides in methanol to afford 2,4- disubstituted thiazoles in good yields. The reaction is thought to proceed by the generation of highly reactive α-λ3 iodanyl ketones through ester exchange of the β-acetoxy group with liberation of methyl acetate, followed by nucleophilic substitutions with thioureas or thioamides [7].
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- Authors: Odame, Felix , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447003 , vital:74576 , xlink:href="https://doi.org/10.1134/S0022476619010190"
- Description: Thiazoles have shown a broad range of biological activities and are found in many potent biologically active molecules such as Sulfathiazol (antimicrobial drug), Ritonavir (antiretroviral drug), Abafungin (antifungal drug), and Tiazofurin (antineoplastic drug) [1]. They have exhibited some degree of plant growth regulatory and antifungal activities [2], whilst some thiazoles have shown anti-infective [3] as well as antibacterial activities [4]. The regio-controlled synthesis of 2,5-disubstituted and 2,4,5-trisubstituted thiazoles from ethyl-2-bromo-5-chloro-4-thiazolecarboxylates using sequential palladium-catalyzed coupling reactions has been reported [5]. An efficient general method for the preparation of 2,4-di- and trisubsituted thiazoles is via P–TsOH. H2O-Catalyzed cyclization of trisubstituted propargylic alcohols with thioamides has been accomplished with moderate to excellent product yields under mild and standard conditions [6]. In the presence of triethylamine, (Z)-(2-acetoxyl-1-alkenyl) phenyl-λ3 iodanes reacts with thioureas or thioamides in methanol to afford 2,4- disubstituted thiazoles in good yields. The reaction is thought to proceed by the generation of highly reactive α-λ3 iodanyl ketones through ester exchange of the β-acetoxy group with liberation of methyl acetate, followed by nucleophilic substitutions with thioureas or thioamides [7].
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Characterization and computational studies of a co-crystal of 2-aminobenzimidazole and 2-[(benzoylcarbamothioyl) amino] propanoic acid
- Odame, Felix, Hosten, Eric C, Betz, Richard, Lobb, Kevin A, Tshentu, Zenixole R
- Authors: Odame, Felix , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447030 , vital:74578 , xlink:href="https://doi.org/10.1134/S0022476618050268"
- Description: A novel co-crystal of 2-aminobenzimidazole and 2-[(benzoylcarbamothioyl)amino] propanoic acid is synthesized and characterized by spectroscopy, elemental analysis, GC-MS, and single crystal XRD. A computation of the structures involved in the formation of the co-crystal are carried out and their contribution to reactivity is explained.
- Full Text:
- Authors: Odame, Felix , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447030 , vital:74578 , xlink:href="https://doi.org/10.1134/S0022476618050268"
- Description: A novel co-crystal of 2-aminobenzimidazole and 2-[(benzoylcarbamothioyl)amino] propanoic acid is synthesized and characterized by spectroscopy, elemental analysis, GC-MS, and single crystal XRD. A computation of the structures involved in the formation of the co-crystal are carried out and their contribution to reactivity is explained.
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Synthesis, characterization and DPPH scavenging activity of some benzimidazole derivatives
- Odame, Felix, Krause, Jason, Hosten, Eric C, Betz, Richard, Lobb, Kevin A, Tshentu, Zenixole R, Frost, Carminita L
- Authors: Odame, Felix , Krause, Jason , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R , Frost, Carminita L
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447209 , vital:74592 , xlink:href="https://dx.doi.org/10.4314/bcse.v32i2.8 "
- Description: A base-catalyzed conversion of aldehydes to benzimidazoles has been achieved. The compounds have been characterized by IR, NMR, micoranalysis, and GC-MS. The reaction for the formation of benzimidazoles has been monitored with 1 H NMR and IR. The crystal structures of two derivatives, 2-(2- chlorophenyl)-1H-benzimidazole and 2-(1H-benzimidazol-2-yl)-4-nitrophenol, are presented. A study of the DPPH scavenging activity of these compounds showed that 2-(1H-benzimidazol-2-yl)phenol (2), 2-p-tolyl-1Hbenzimidazole (3) and 2-(4-methoxyphenyl)-1H-benzimidazole (7) gave IC50 values 1974, 773 and 800 µM.
- Full Text:
- Authors: Odame, Felix , Krause, Jason , Hosten, Eric C , Betz, Richard , Lobb, Kevin A , Tshentu, Zenixole R , Frost, Carminita L
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447209 , vital:74592 , xlink:href="https://dx.doi.org/10.4314/bcse.v32i2.8 "
- Description: A base-catalyzed conversion of aldehydes to benzimidazoles has been achieved. The compounds have been characterized by IR, NMR, micoranalysis, and GC-MS. The reaction for the formation of benzimidazoles has been monitored with 1 H NMR and IR. The crystal structures of two derivatives, 2-(2- chlorophenyl)-1H-benzimidazole and 2-(1H-benzimidazol-2-yl)-4-nitrophenol, are presented. A study of the DPPH scavenging activity of these compounds showed that 2-(1H-benzimidazol-2-yl)phenol (2), 2-p-tolyl-1Hbenzimidazole (3) and 2-(4-methoxyphenyl)-1H-benzimidazole (7) gave IC50 values 1974, 773 and 800 µM.
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