143426-39-5Relevant articles and documents
Design, synthesis, biological assessment and: In silico ADME prediction of new 2-(4-(methylsulfonyl) phenyl) benzimidazoles as selective cyclooxygenase-2 inhibitors
Badawy, Mohamed A. S.,Abdelall, Eman K. A.,El-Nahass, El-Shaymaa,Abdellatif, Khaled R. A.,Abdel-Rahman, Hamdy M.
, p. 27659 - 27673 (2021)
A novel series of benzimidazole derivatives wherein 4-(methylsulfonyl) phenyl pharmacophore attached via its C-2 position was designed and synthesized. These compounds were evaluated in vitro as cyclooxygenase-1(COX-1)/cyclooxygenese-2(COX-2) inhibitors. Furthermore, the synthesized compounds were also in vivo evaluated for their anti-inflammatory activity and ulcerogenic liability. Examination of histopathological lesions was also performed to evaluate the cariogenic effect of most active compounds. In silico prediction of physicochemical properties, ADME, and drug-likeness profiles were also studied. Several compounds as 11b, 11k, 12b, and 12d showed selective inhibition to (COX-2) isozyme. Compound 11b showed the most potent (COX-2) inhibitory activity with (IC50 = 0.10 μM) and selectivity index (SI = 134); the tested compounds also have shown good anti-inflammatory activity. Regarding the ulcerogenic liability, compound 11b was also safest one (Ulcer Index) (UI = 0.83). The results of the molecular docking studies is closely related to the results of the in vitro COX-2 inhibitory activities.
Oxidative Radical Relay Functionalization for the Synthesis of Benzimidazo[2,1-a]iso-quinolin-6(5H)-ones
Sun, Kai,Li, Guofeng,Li, Yuyang,Yu, Jie,Zhao, Qing,Zhang, Zhiguo,Zhang, Guisheng
, p. 1947 - 1954 (2020/03/23)
Here, a mild and general oxidative radical relay carbocyclization reaction with 2-arylbenzoimidazoles and cyclic ethers is reported. This method provides an efficient access to a wide range of structurally diverse benzimidazo[2,1-a]isoquinoline-6(5H)-ones under metal-free conditions. The wide substrate scope, good functional group tolerance, and scale-up operation of this method are expected to promote its potential applications in biotechnology and pharmacy. (Figure presented.).
Conventional and microwave-assisted synthesis of benzimidazole derivatives and their in vitro inhibition of human cyclooxygenase
Secci, Daniela,Bolasco, Adriana,D'Ascenzio, Melissa,Della Sala, Flavio,Yanez, Matilde,Carradori, Simone
, p. 1187 - 1195 (2013/01/15)
A large series of 1,2-diaryl-benzimidazole and 2-aryl-1H-benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained
N-hydroxyphthalimide/cobalt acetate, a new catalytic oxidative system for the synthesis of benzimidazoles
Coppola, Gary M.
, p. 3500 - 3507 (2008/12/23)
Benzimidazoles are readily prepared from 1,2-phenylenediamine and an aldehyde using air and catalytic N-hydroxyphthalimide/Co(OAc)2 as the oxidant. Both electron-donating and electron-withdrawing groups are tolerated. Copyright Taylor & Francis Group, LLC.
2-Aryl-substituted benzo-anellated 5-membered heterocycles as potential effectors in the cardiovascular system. Part 2
Rose
, p. 775 - 777 (2007/10/02)
In the course of investigations on structure-activity relationships of fostedil-and sulmazole-analoguesly fused 5-membered heterocycles, 1,3-benzimidazoles were obtained by simple cyclisation. In vitro experiments on isolated organs demonstrate markedly positive inotropic effects of some derivatives, whereas others exert both relaxing activity on smooth musculature in vitro and antihypertensive effects in vivo. Moreover they exhibit fungicide properties in vitro.
