20033-96-9Relevant academic research and scientific papers
Synthesis and antimicrobial activity of some new pyrimidines of 6-chlorobenzimidazoles
Mdawali, Indira M.,Kalyane, Navanath V.,Gaviraj,Shivakumar
, p. 1633 - 1637 (2018)
A new series of pyrimidines of 6-chlorobenzimidazoles have been synthesized by the reaction of chalcone derivatives of 6-chlorobenzimidazole with guanidine nitrate in ethanol and aqueous solution of sodium hydroxide for evaluating them as potent antimicrobial agents. Results reveal that, compounds exhibited significant antibacterial and antifungal activities.
Novel cathepsin K inhibitors block osteoclasts in vitro and increase spinal bone density in zebrafish
Xue, Si-Tu,Wang, Ya-Li,Han, Xiao-Wan,Yi, Hong,Jiang, Wei,Si, Shu-Yi,Guo, Hui-Fang,Li, Zhuo-Rong
, p. 8600 - 8607 (2019/03/21)
Cathepsin K (Cat K) is a predominant cysteine protease and highly potent collagenase expressed in osteoclasts. Cat K inhibitors are anti-resorptive agents to treat osteoporosis. A novel scaffold of cathepsin K inhibitors, exemplified by lead compound 1x, was used as the template for designing and synthesizing a total of 61 derivatives that have not been reported before. An exploratory structure-activity relationship analysis identified the potent Cat K inhibitor A22, which displayed an IC50 value of 0.44 μM against Cat K. A22 was very specific for Cat K and caused a significantly higher in vitro inhibition of the enzyme as compared to that of lead compound 1x. A surface plasmon resonance analysis confirmed in vitro binding of A22 to Cat K. Molecular docking studies indicated several favourable interaction sites for A22 within the active pocket of Cat K. Furthermore, A22 also blocked active osteoclasts in vitro and increased spinal bone density in zebrafish, in which it showed an activity that was higher than that of the marketed therapeutic bone metabolizer etidronate disodium. A22 represents a very promising lead compound for the development of novel antiresorptive agents functioning as orthosteric inhibitors of Cat K.
Compositions containing five-membered unsaturated heterocyclic structure of the α, β unsaturated ketone compound and its preparation method and application
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Paragraph 0383, (2017/07/14)
The invention provides alpha, beta unsaturated ketone compounds containing benzo five-membered unsaturated heterocycle structures as well as a preparation method and an application and use of the compounds. The alpha, beta unsaturated ketone compounds containing the benzo five-membered unsaturated heterocycle structures have the structure of a formula (I). In addition, the invention further provides a method for preparing the compounds and a pharmaceutical composition containing the components as active components. In vitro activity tests show that the compounds provided by the invention show a remarkable inhibiting effect on tumor cells. Therefore, the invention lays a foundation for lucubrating and developing anti-tumor medicines in the future and meanwhile further provides a new technical means for treating tumor diseases.
Synthesis and in vitro antifungal evaluation of benzoimidazolyl-piperazinyl-phenylmethanone derivatives
Kankate, Rani S.,Gide, Parag S.,Belsare, Deepak P.
, p. 1855 - 1863 (2015/04/22)
Benzimidazole and piperazines are the important pharmacophores in the structures of many antifungal compounds. Further, the phenylmethanone are also a unique class of compounds whose antifungal profile is not much exploited. So to exploit their antifungal potential we have selected these three combinations and framed the novel parent structure for our research work. In this study a novel series of benzimidazoles derivatives was synthesized by microwave irradiation and characterized by 1H NMR, 13C NMR, Infra Red (IR), and Mass Spectroscopy (MS), and by elemental analysis. The screening of compound for in vitro (turbidimetric method) antifungal activity against C.albicans revealed activity in many of the compounds as comparable to that of ketoconazole.
Synthesis of some novel thiosemicarbazone derivatives having anti-cancer, anti-HIV as well as anti-bacterial activity
Patel, Hitesh Dahyabhai,Divatia, Saavani Malove,De Clercq, Erik
, p. 535 - 545 (2013/06/26)
Some new thiosemicarbazones containing benzimidazole moiety have been synthesized and their ability to inhibit growth of 60 human cancer cell lines, in vitro replication of HIV virus strains as well as inhibition capacity for various bacterial strains have been evaluated. One compound 2-|l-(5-chloro-l//- benzimidazol-2-yl) ethylidene] N-phenylhydrazincarbothioamide (S2) (NSC 92491) has been selected for five dosage screening and shows remarkable anticancer activity along with good anti-HIV and anti-bacterial activities. The structures of all the compounds have been confirmed by FT-IR, NMR, and Mass spectra and by elemental analysis.
Synthesis and antimicrobial activity of some novel 4-(1H-benz[d]imidazol- 2yl)-1,3-thiazol-2-amines
Reddy, Vanga Malla,Reddy, Kunduru Ravinder
experimental part, p. 953 - 956 (2010/09/09)
A new series of novel 4-(1H-benz[d]imidazol-2yl)-1,3-thiazol-2-amines 5a-d and 4-(1H-benz[d]imidazol-2yl)-3-alkyl-2,3-dihydro-1,3-thiazol-2-amine 8a-d has been synthesized by the cyclocondensation of 2-acetyl benzimidiazoles 4a-d and 2-bromo-1-(1-alkyl-1H
Synthesis and antibacterial activity of some novel 6-(1H-benz[d] imidazol-2-yl)-8-(5-nitro-2-furyl)-3-(4-pyridyl)-7,8-dihydro[1,2,4] triazolo[3,4-b][1,3,4]thiadiazepines
Reddy, Vanga Malla,Reddy, Kunduru Ravinder
experimental part, p. 1081 - 1084 (2010/11/02)
A new series of novel 6-(1H-benz[d]imidazol-2-yl)-8-(5-nitro-2-furyl)-3-(4- pyridyl)-7,8-dihydro[1,2,4]triazolo[ 3,4-b][1,3,4]thiadiazepines 8a - d has been synthesized. These compounds were evaluated for their efficiency as antibacterial agents against two Gram-positive and Gram-negative strains of bacteria along with anti-fungal activity against two fungal organisms. The antibacterial and antifungal activities of the present compounds were not comparable with those of the standard drugs employed. But, however, all the test compounds could exhibit notable activities only at higher concentrations (250, 500 μg/ml). The chemical structures of these compounds were confirmed on the basis of spectral data.
Synthesis and biological evaluation of some novel-3-(5-substituted benzimidazol-2-yl)-5-arylisoxazolines
Reddy, Vanga Malla,Reddy, Kunduru Ravinder
experimental part, p. 1145 - 1148 (2011/10/08)
The synthesis of a new series of 3-(5-substituted benzimidazol-2-yl)-5-arylisoxazolines (6a-h) was achieved in excellent yields by the condensation of 1-(1H-benzimidazol-2-yl)-3-(substituted phenyl)prop-2-en-1-ones (5a-h) with hydroxylamine at room temperature. These 1-(1H-benzimidazol-2-yl)-3-(substituted phenyl)prop-2-en-1-ones (5a-h) were obtained by the condensation of 2-acetyl benzimidazoles (4a-d) with different aromatic aldehydes, which in turn were obtained by the oxidation of 2-(α-hydroxy)ethyl benzimidazoles (3a-d) prepared by the reaction of o-phenylenediamines (1a-d) with α-hydroxy propionic acid 2. The synthesized compounds were characterized by their IR, 1H NMR and MS analyses. These compounds were screened for their antibacterial and antifungal activity by standard methods and found some of them active.
