31075-58-8Relevant academic research and scientific papers
Design, Synthesis, Cytotoxicity, and Molecular Docking Studies of New Benzimidazole Hybrids as Possible Anticancer Agents
Mishra, Shashank Shekher,Sharma, C. S.
, p. 21 - 29 (2021/08/12)
In the course of efforts to develop new anticancer agents, benzimidazole-based morpholine, thiomorpholine, and piperazine hybrid compounds were designed and synthesized. The structures of the synthesized compounds were confirmed by Proton nuclear magnetic resonance, Carbon-13 NMR, and mass spectroscopy. The title compounds were screened for cytotoxicity against breast and lung cancer cell lines. Compound 6c was found most active against lung cancer cell line with IC50 value of 2.11 μM and compound 10c was found most active against breast cancer cell line with IC50 of 2.23 μM. The molecular docking analysis was also carried out to explore binding pattern of compound with the target protein. All synthesized compounds showed excellent binding affinity toward target protein. Therefore, these findings will be helpful in future drug design of more potent anticancer agents.
Copper-catalysed C-H functionalisation gives access to 2-aminobenzimidazoles
Clark, Peter R.,Williams, Glynn D.,Tomkinson, Nicholas C. O.
, p. 7943 - 7955 (2019/09/06)
This paper describes the development, optimisation and exemplification of a copper-catalysed C-H functionalisation to form pharmaceutically relevant 2-aminobenzimidazoles from aryl-guanidines. High throughput screening was used as a tool to identify a catalytically active copper source, DoE was used for reaction optimisation and a range of aryl-guanidines were prepared and exposed to the optimum conditions to afford a range of 2-aminobenzimidazoles in moderate to good yields. The methodology has been applied to the synthesis of Emedastine, a marketed anti-histamine pharmaceutical compound, with the key cyclisation step performed on a gram-scale.
Eco-friendly strategy: design and synthesis of biologically potent benzimidazole-amine hybrids via visible-light generated oxidative C-H arylamylation of analenic amidines
Siddiqui,Ibad, Farah,Ibad, Afshan,Abdul Waseem, Malik,Watal, Geeta
, p. 5 - 10 (2015/12/23)
An operationally simple visible light mediated intramolecular cyclization of benzimidazole to 2-amino benzimidazole hybrid. The disclosed procedure is rapid and the convenient synthesis of benzimidazole-amine hybrids from easily available substituted cycl
Arylation of amines and monoarylation of symmetrical diamines in the presence of brine solution with diheteroaryl halides
Verma, Sanjeev K.,Ghorpade, Ramarao,Kaushik
supporting information, p. 2645 - 2655 (2014/08/18)
A simple, scalable, ligand-free, and metal-free protocol for arylation of amines and monoarylation of symmetrical diamines with diheteroaryl halides in the presence of brine solution has been developed. The protocol has broad structural applicability for chemoselective monoarylation of a wide variety of symmetrical, cyclic, and acyclic aliphatic diamines. The protocol is also applicable for selective arylation of aliphatic amine in the presence of aromatic amine.
A DBU-diheteroaryl halide adduct as the fastest current N-diheteroarylating agent
Verma, Sanjeev K.,Acharya,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
, p. 18783 - 18786 (2013/10/22)
An unexpected diazabicyclo[5.4.0]undec-7-ene (DBU) catalysed rate enhancement of N-arylation of amines with diheteroaryl halides is reported. DBU is found to activate the Ar-Cl bond of a diheteroaryl halide, forming a green coloured adduct under neat conditions. The activated green coloured adduct was used for the arylation of amines under neat conditions and was found to be the fastest diheteroarylating agent reported to date. The Royal Society of Chemistry 2013.
Chemospecific and ligand free CuI catalysed heterogeneous N-arylation of amines with diheteroaryl halides at room temperature
Verma, Sanjeev K.,Acharya,Kaushik
supporting information; experimental part, p. 1324 - 1327 (2011/04/16)
A ligand free, copper-catalyzed N-arylation reaction of amines with diheteroaryl halides in heterogeneous medium at room temperature has been developed. The protocol is very effective for low boiling amines and useful for amines available in aqueous solution. The reaction gives chemospecific arylation of amines with diheteroaryl halides in the mixture monoheteroaryl halides, diheteroaryl halides and carbocyclic aryl halides. The reaction is also chemospecific with respect to arylation of aliphatic amines. Monoarylated piperazines were also synthesized at room temperature following this protocol. The Royal Society of Chemistry 2011.
CuI-catalyzed amination of arylhalides with guanidines or amidines: A facile synthesis of 1-H-2-substituted benzimidazoles
Deng, Xiaohu,McAllister, Heather,Mani, Neelakandha S.
supporting information; scheme or table, p. 5742 - 5745 (2009/12/06)
(Figure Presented) CuI/L5 (N,N′-dimethylethylenediamine) proves to be an efficient catalyst system for the amination of arylhalides with guanidines. The same catalyst system is then successfully applied to the one-step synthesis of 1-H-2-aminobenzimidazol
QUINOLONES USEFUL AS INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS
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Page/Page column 89, (2008/12/06)
The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
2,2'-DIALKOXY, 2,2'-DIHYDROXY, AND 2,2'-DIAMINO DERIVATIVES OF 1,1'-AZOBENZIMIDAZOLE. THE FIRST SYNTHESIS OF HETEROCYCLIC TETRAZENES BY MEANS OF A NUCLEOPHILIC SUBSTITUTION REACTION
Kuz'menko, V. V.,Nanavyan, I. M.,Pozharskii, A. F.
, p. 154 - 157 (2007/10/02)
2,2'-Dimethanesulfonyl-1,1'-azobenzimidazole is prepared by the oxidation of 1-amino-2-methanesulfonylbenzimidazole with lead tetraacetate.The reaction of this tetrazene with alkali in DMSO, with sodium alkoxides in the corresponding alcohol or ammonia, or with primary or secondary amines leads to the formation of 2,2'-dihydroxy, 2,2'-dialkoxy, or 2,2'-diamino derivatives of 1,1'-azobenzimidazole.
