20033-97-0Relevant academic research and scientific papers
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.
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.
