709-19-3Relevant articles and documents
Synthesis and biological evaluation of 2-methyl-1H-benzimidazole-5-carbohydrazides derivatives as modifiers of redox homeostasis of Trypanosoma cruzi
Melchor-Doncel de la Torre, Silvia,Vázquez, Citlali,González-Chávez, Zabdi,Yépez-Mulia, Lilián,Nieto-Meneses, Rocío,Jasso-Chávez, Ricardo,Saavedra, Emma,Hernández-Luis, Francisco
, p. 3403 - 3407 (2017)
Twelve novel benzimidazole derivatives were synthesized and their in vitro activities against epimastigotes of Trypanosoma cruzi were evaluated. Two derivatives (6 and 7), which have 4-hydroxy-3-methoxyphenyl moiety in their structures, proved to be the m
Homology modelling, molecular dynamics simulation and docking evaluation of β-tubulin of Schistosoma mansoni
El-Shehabi, Fouad,Mansour, Basem,Bayoumi, Waleed A.,El Bialy, Serry A.,Elmorsy, Mohammad A.,Eisa, Hassan M.,Taman, Amira
, (2021/09/16)
Schistosomiasis is one of the neglected diseases causing considerable morbidity and mortality throughout the world. Microtubules with its main component, tubulin play a vital role in helminthes including schistosomes. Benzimidazoles represent potential drug candidates by binding β-tubulin. The study aimed to generate a homology model for the β-tubulin of S. mansoni using the crystal structure of O vis aries (Sheep) β-tubulin (PDB ID: 3N2G D) as a template, then different β-tubulin models were generated and two previously reported benzimidazole derivatives (NBTP-F and NBTP-OH) were docked to the generated models, the binding results indicated that both S. mansoni, S. haematobium were susceptible to the two NBTP derivatives. Additionally, three mutated versions of S. mansoni β-tubulin wild-type were generated and the mutation (F185Y) seems to slightly enhance the ligand binding. Dynamics simulation experiments showed S. haematobium β-tubulin is highly susceptible to the tested compounds; similar to S. mansoni, moreover, mutated models of S. mansoni β-tubulin altered its NBTPs susceptibility. Moreover, additional seven new benzimidazole derivatives were synthesized and tested by molecular docking on the generated model binding site of S. mansoni β-tubulin and were found to have good interaction inside the pocket.
BICYCLIC HETEROARYL DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
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Paragraph 0297, (2020/10/21)
The present disclosure provides certain bicyclic heteroaryl compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I). Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS
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Page/Page column 39, (2018/03/06)
The present invention relates to C-3 novel triterpenone with C-17 reverse amide compounds of Formula (I); and pharmaceutically acceptable salts thereof, wherein ring Formula (II), R1, R2, R3, R4, R5, R6, R7, 'n' and 'm' are as defined in Formula (I). The invention also relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Selective exploitation of acetoacetate carbonyl groups using imidazolium based ionic liquids: synthesis of 3-oxo-amides and substituted benzimidazoles
Chakraborty, Ankita,Majumdar, Swapan,Maiti, Dilip K.
, p. 3298 - 3302 (2016/07/11)
An unprecedented Br?nsted base ionic liquid tuned selective aminolysis of ester carbonyl of acetoacetates is demonstrated to achieve acetoacetamide derivatives. Other imidazolium ionic liquid performs an efficient cyclization catalysis involving acetoacetate-carbonyl groups and o-phenylenediamine at elevated temperature to produce benzimidazoles via C–C bond cleavage of intermediate 1,5-benzodiazepinones under solvent-free conditions.
Silica–ferric chloride (SiO2–FeCl3) catalyzed selective synthesis of 2-substituted benzimidazole through Csp2Csp3bond cleavage of β-ketoester/amide
Majumdar, Swapan,Chakraborty, Ankita,Bhattacharjee, Subrata,Debnath, Sudipto,Maiti, Dilip K.
supporting information, p. 4595 - 4598 (2016/09/23)
Silica–ferric chloride (SiO2–FeCl3) supported reagent was successfully utilized as recyclable catalyst for the general and highly efficient synthesis of 2-substituted benzimidazole by the condensation of 1,2-diamino benzene and β-ketoester/amide followed by original Csp2Csp3bond cleavage. Evidences in favor of C[sbnd]C (α–β) bond cleavage of β-ketoesters/amides are established.
Trimethylsilyl chloride catalyzed synthesis of substituted benzimidazoles using two phase system under microwave conditions, and their antimicrobial studies
Karuvalam, Ranjith P.,Haridas, Karickal R.,Shetty, Suchetha N.
, p. 1122 - 1125,4 (2020/08/24)
A convenient method using TMSCl (20 mol%) and microwave-induced technique for the synthesis of various benzimidazole is described. This has reduced the reaction time drastically as well as improved the yield when compared to conventional heating. The synthesized compounds were evaluated for their in vitro antibacterial and antifungal activities against four strains each. Preliminary results indicated that, compounds 3e, 3f, 3g, 3k, 3m, 3n and 3o demonstrated very good antimicrobial activity, comparable to the first line standard drugs. The most effective compounds have exhibited activity at MIC of 6.25 μg/mL.
Synthesis and antibacterial activity of novel 4″-O-benzimidazolyl clarithromycin derivatives
Cong, Chao,Wang, Haiyang,Hu, Yue,Liu, Chen,Ma, Siti,Li, Xin,Cao, Jichao,Ma, Shutao
supporting information; experimental part, p. 3105 - 3111 (2011/07/08)
Novel 4″-O-benzimidazolyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These benzimidazolyl derivatives exhibited excellent activity against erythromycin-susceptible strains better than the references, and some of them showed greatly improved activity against erythromycin-resistant strains. Compounds 16 and 17, which have the terminal 2-(4-methylphenyl)benzimidazolyl and 2-(2-methoxyphenyl)benzimidazolyl groups on the C-4″ bishydrazide side chains, were the most active against erythromycin-resistant Staphylococcus pneumoniae expressing the erm gene and the mef gene. In addition, compound 17 exhibited the highest activity against erythromycin-susceptible S. pneumoniae ATCC49619 and Staphylococcus aureus ATCC25923 as well. It is worth noting that the 4″-O-(2-aryl)benzimidazolyl derivatives show higher activity against erythromycin-susceptible and erythromycin-resistant strains than the 4″-O-(2-alkyl)benzimidazolyl derivatives.
Tetra butyl ammonium chloride catalyzed synthesis of substituted benzimidazoles under microwave conditions
Ranjith, P. Karuvalam,Siji,Divia,Karickal, R. Haridas
experimental part, p. 589 - 593 (2011/01/12)
TBACl (10 mol %) was found to be a useful catalyst for the synthesis of substituted benzimidazoles. The method was proved to be simple, convenient and the product was isolated with good yield.
New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity
Galal, Shadia A.,Hegab, Khaled H.,Kassab, Ahmed S.,Rodriguez, Mireya L.,Kerwin, Sean M.,El-Khamry, Abdel-Mo'men A.,El Diwani, Hoda I.
experimental part, p. 1500 - 1508 (2009/07/11)
Metal complexes of 2-methyl-1H-benzimidazole-5-carboxylic acid hydrazide (4a; L1) and its Schiff base 2-methyl-N-(propan-2-ylidene)-1H-benzimidazole-5-carbohydrazide (5a; L2) with transition metal ions e.g., copper, silver, nickel, i
