28096-55-1Relevant academic research and scientific papers
Synthesis, molecular docking and ADME prediction of some new benzimidazole carboxamidines derivatives as antimicrobial agents
Erol, Meryem,Celik, Ismail,Temiz-Arpaci, Ozlem,Goker, Hakan,Kaynak-Onurdag, Fatma,Okten, Suzan
, p. 2028 - 2038 (2020)
In this study, 15 new 1H-benzimidazole-5-carboxamidine derivative compounds that could be new antimicrobial agents were synthesized and their antimicrobial activities were determined using the microdilution method. When the activity results were examined,
Small Sequence-Sensitive Compounds for Specific Recognition of the G?C Base Pair in DNA Minor Groove
Farahat, Abdelbasset A.,Guo, Pu,Shoeib, Hadir,Paul, Ananya,Boykin, David W.,Wilson, W. David
, p. 4539 - 4551 (2020/03/25)
A series of small diamidines with thiophene and modified N-alkylbenzimidazole σ-hole module represent specific binding to single G?C base pair (bp) DNA sequence. The variation of N-alkyl or aromatic rings were sensitive to microstructures of the DNA minor
1 H -Benzimidazole-5-carboxamidine derivatives: Design, synthesis, molecular docking, DFT and antimicrobial studies
Erol, Meryem,Celik, Ismail,Temiz-Arpaci, Ozlem,Goker, Hakan,Kaynak-Onurdag, Fatma,Okten, Suzan
, p. 21309 - 21317 (2020/12/31)
In this study, 15 new N-(cyclohexyl)-2-substituted-1H-benzimidazole-5-carboxamidine derivatives that could be new antimicrobial agents were synthesized and their antimicrobial activities were determined using the microdilution method. Some of the derivatives showed significant efficacy against MRSA and VREF with an MIC value of 8 μg mL-1 compared to reference drugs. Molecular docking studies of the compounds against PBP4 and active and allosteric regions of PBP2a were performed and estimated ADME profiles were calculated. The nitrogens of the amidine group of M7, one of the most effective antimicrobial compounds compared to reference drugs, formed two separate hydrogen bonds with ASP275 (1.77 ?) and ASP295 (1.83 ?) in the allosteric region of PBP2a. Geometric optimization parameters, MEP analysis, and HUMO and LUMO quantum parameters of M7 were calculated using DFT/B3LYP theory and the 6-311G(d,p) basis set and the results are displayed.
Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI
Farahat, Abdelbasset A.,Bennett-Vaughn, Cheree,Mineva, Ekaterina M.,Kumar, Arvind,Wenzler, Tanja,Brun, Reto,Liu, Yang,Wilson, W. David,Boykin, David W.
, p. 5907 - 5910 (2016/12/03)
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
BICYCLIC IMIDAZOL DERIVATIVES AGAINST FLAVIVIRIDAE
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Page/Page column 247, (2008/06/13)
Disclosed are compounds, compositions and methods for treatingFlaviviridae family virus infections.
Imidazopyridinone derivatives and their use as phosphodiesterase inhibitors
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, (2008/06/13)
A compound (Ia): wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc.
Synthesis of some new 2-substituted-phenyl-1H-benzimidazole-5-carbonitriles and their potent activity against Candida species
G?ker, Hakan,Ku?, Canan,Boykin, David W.,Yildiz, Sulhiye,Altanlar, Nurten
, p. 2589 - 2596 (2007/10/03)
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
Cycloalkyl or benzyl-6-substituted-quinoxalinediones
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, (2008/06/13)
Heterocyclic dihydroxyquinoxaline compounds having the formula STR1 wherein R 1 is C 1-12 -alkyl, which may optionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C 3-8 -cycloalkyl, aryl, aralkyl; and wherein R 6 is, hydrogen, halogen, CN, CF 3, NO 2, or OR'', wherein R'' is C 1-4 -alkyl and R 5, R 7 and R 8 is hydrogen, provided R 6 is not CF 3, OCH 3, NO 2, C 1 or Br when R 1 is CH 3 ; orR 6 and R 7 independently are NO 2, halogen, CN, CF 3, or OR'', wherein R'' is C 1-4 -alkyl, and R 5 and R 8 are each hydrogen; orR 5 and R 6 together form a further fused aromatic ring, which may be substituted with halogen, NO 2, CN, CF 3 or OR'', wherein R'' is C 1-4 -alkyl, and R 7 and R 8 independently are hydrogen, halogen, CN, CF 3, NO 2 or OR'', wherein R'' is C 1-4 -alkyl; orR 7 and R 8 together form a further fused aromatic ring, which may be substituted with halogen, NO 2, CN, CF 3 or OR'', wherein R'' is C 1-4 -alkyl, and R 5 and R 6 independently are hydrogen, halogen, CN, CF 3, NO 2 or OR'', wherein R'' is C 1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.
