25084-14-4Relevant articles and documents
Structure-antibacterial activity relationships of n-substituted-(D-/l-alaninyl) 1h-1,2,3-triazolylmethyl oxazolidinones
Phillips, Oludotun Adebayo,Udo, Edet Ekpenyong,D’silva, Roselyn Jennifer
, (2018)
Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs’ approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of D-/L-alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate to strong antibacterial activity. Compounds 9d and 10d (D-and L-alaninyl derivatives bearing the 3,5-dinitrobenzoyl substituent), 10e (L-alaninyl derivative bearing the 5-nitrofurancarbonyl group) and 9f and 10f (D-and L-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety) demonstrated antibacterial activity (MIC: 2 μg/mL) against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and Moraxella catarrhalis standard bacterial strains. No significant differences were noticeable between the antibacterial activity of the D-and L-alaninyl derivatives as a result of the stereochemistry of the compounds.
Synthesis of N-methylpyridine-chlorofuranformamide analogs as novel OPG up-regulators and inhibitors of RANKL-induced osteoclastogenesis
Liu, Chao,Li, Yining,Sheng, Ren,Han, Xiaowan,Bao, Li,Wang, Chenyin,Wang, Weizhi,Jiang, Xinhai,Han, Jiangxue,Lei, Lijuan,Li, Ni,Zhang, Jing,Chen, Minghua,Li, Yan,Wu, Yexiang,Li, Shunwang,Ren, Yu,Xu, Yanni,Si, Shuyi
, (2021/09/28)
The OPG/RANKL/RANK pathway is a promising target for the design of therapeutic agents used in the treatment of osteoporosis. E09241 with an N-methylpyridine-chlorofuranformamide structural skeleton was previously identified to decrease bone loss and thus protect against osteoporosis in ovariectomized rats through increasing osteoprotegerin (OPG) expression. In this study, 36 derivatives of E09241 (3a) were prepared. The synthesis, up-regulation of OPG activities, SAR (structure–activity relationship), and cytotoxicity of these compounds are presented. Compounds with good up-regulating OPG activities could inhibit RANKL (the receptor activator of nuclear factor-kappa B ligand)-induced osteoclastogenesis in RAW264.7 cells. Particularly, compounds 3c and 3i1 significantly reduced NFATc1 and MMP-9 protein expression through inhibition of the NF-κB and MAPK pathways in RANKL induced RAW264.7 cells. In addition, compounds 3c and 3v significantly promoted osteoblast differentiation in MC3T3-E1 cells in osteogenic medium, and compounds 3c, 3v, and 3i1 obviously increased OPG protein expression and secretion in MC3T3-E1 cells. Furthermore, the pharmacokinetic profiles, acute toxicity, and hERG K+ channel effects of compounds 3a, 3c, 3e, 3v, and 3i1 were investigated. Taken together, these results indicate that N-methylpyridine-chlorofuranformamide analog 3i1 could serve as a promising lead for the development of new agents for treating osteoporosis.
ANTIBACTERIAL THERAPEUTICS AND PROPHYLACTICS
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Paragraph 00312; 00314, (2017/02/24)
The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.
