- Synthesis and biological evaluation of 2-methyl-1H-benzimidazole-5-carbohydrazides derivatives as modifiers of redox homeostasis of Trypanosoma cruzi
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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
- 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
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- Homology modelling, molecular dynamics simulation and docking evaluation of β-tubulin of Schistosoma mansoni
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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.
- El-Shehabi, Fouad,Mansour, Basem,Bayoumi, Waleed A.,El Bialy, Serry A.,Elmorsy, Mohammad A.,Eisa, Hassan M.,Taman, Amira
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- BICYCLIC HETEROARYL DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
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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.
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- C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS
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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.
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- Selective exploitation of acetoacetate carbonyl groups using imidazolium based ionic liquids: synthesis of 3-oxo-amides and substituted benzimidazoles
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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.
- Chakraborty, Ankita,Majumdar, Swapan,Maiti, Dilip K.
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p. 3298 - 3302
(2016/07/11)
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- Silica–ferric chloride (SiO2–FeCl3) catalyzed selective synthesis of 2-substituted benzimidazole through Csp2Csp3bond cleavage of β-ketoester/amide
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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.
- Majumdar, Swapan,Chakraborty, Ankita,Bhattacharjee, Subrata,Debnath, Sudipto,Maiti, Dilip K.
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supporting information
p. 4595 - 4598
(2016/09/23)
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- Trimethylsilyl chloride catalyzed synthesis of substituted benzimidazoles using two phase system under microwave conditions, and their antimicrobial studies
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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.
- Karuvalam, Ranjith P.,Haridas, Karickal R.,Shetty, Suchetha N.
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p. 1122 - 1125,4
(2020/08/24)
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- Synthesis and antibacterial activity of novel 4″-O-benzimidazolyl clarithromycin derivatives
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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.
- Cong, Chao,Wang, Haiyang,Hu, Yue,Liu, Chen,Ma, Siti,Li, Xin,Cao, Jichao,Ma, Shutao
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supporting information; experimental part
p. 3105 - 3111
(2011/07/08)
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- Tetra butyl ammonium chloride catalyzed synthesis of substituted benzimidazoles under microwave conditions
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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.
- Ranjith, P. Karuvalam,Siji,Divia,Karickal, R. Haridas
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experimental part
p. 589 - 593
(2011/01/12)
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- New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity
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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
- 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.
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experimental part
p. 1500 - 1508
(2009/07/11)
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- DICARBONYLIC COMPOUNDS WITH ANTIBACTERIAL ACTIVITY
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Compounds of formula (I), and their pharmaceutically acceptable salts and solvates, wherein X represents -O-, -NH-, -S-, -NHC(=O)- or -NHC(=S)-; R1 represents -H or a hydrocarbon chain; R2 represents -H, alkoxy, amino, a hydrocarbon chain or a radical of a cycle; R3 represents -H, a hydrocarbon chain or a radical of a cycle; R4 represents -H or a hydrocarbon chain; alternatively R3 and R4 form together a cycle; R5 and R6 represent -H or halogen, and R7 represents -H, a hydrocarbon chain or heteroaryl, are useful against bacterial infections in animals, including humans.
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Page/Page column 24
(2010/11/28)
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- Rapid one-pot preparation of 2-substituted benzimidazoles from 2-nitroanilines using microwave conditions
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A high yielding one-pot procedure for the generation of 2-substituted benzimidazoles directly from 2-nitroanilines by in situ reduction and cyclization using a microwave procedure is described.
- VanVliet, David S.,Gillespie, Paul,Scicinski, Jan J.
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p. 6741 - 6743
(2007/10/03)
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- Neutrophil inhibitors to reduce inflammatory response
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The invention provides novel compounds selected from the group consisting of: The compounds of the present invention are useful for the treatment and prevention of a variety of diseases and conditions associated with undesirable or abnormal inflammatory responses, such as ischemia-reperfusion injury. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment or prevention for the above disorders using theses compounds or the compositions containing them.
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Page/Page column 6
(2010/02/05)
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- RECHERCHES EN SERIE BENZODIAZEPINE-1,5: SYNTHESES DES DITRIAZOLO--BENZODIAZEPINES-1,5
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The action of several o-phenylenediamines on malonic acid was studied.Six new ditriazolo-1,5-benzodiazepines were prepared from 1,5-benzodiazepin-2,4-diones.Their structures are supported by 1H nmr,ir, mass spectrometry and elemental analysis.
- Essassi, E. M.,Lamkadem, A.,Zniber, R.
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p. 277 - 286
(2007/10/02)
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- Novel β-lactam antibiotics
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Antibacterially active and animal growth-promoting novel β-lactam compounds of the formula STR1 in which R1 represents the radical STR2 Y representing N or CR9, or Y--R7 representing >C=O or >C=N--R7, Z representing O, S, or NR10, and R2 represents hydrogen or a protective group.
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