101351-75-1Relevant academic research and scientific papers
Synthetic access to the chemical diversity of DNA and RNA 5′-aldehyde lesions
Lartia, Rémy,Constant, Jean-Francois
, p. 705 - 710 (2015/03/05)
Hydrogen atom abstraction from the C5′-position of nucleotides in DNA results in direct strand scission by generating alkali-labile fragments from the oxidized nucleotide. The major damage consists in a terminus containing a 5′-aldehyde as part of an othe
1,4-Diarylpiperazines and analogs as anti-tubercular agents: Synthesis and biological evaluation
Forge,Cappoen,Laurent,Stanicki,Mayence,Huang,Verschaeve,Huygen,Vanden Eynde
scheme or table, p. 95 - 101 (2012/04/10)
Despite progress in modern chemotherapy to combat tuberculosis, the causative pathogen Mycobacterium tuberculosis (M.tb.) is far from eradicated. Bacillary resistance to anti-mycobacterial agents, bacillary persistence and human immunodeficiency virus (HIV) co-infection hamper current drug treatment to completely cure the infection, generating a constant demand for novel drug candidates to tackle these problems. A small library of novel heterocyclic compounds was screened in a rapid luminometric in vitro assay against the laboratory M.tb. strain H37Rv. A group of amidines was found to have the highest potency and was further evaluated for acute toxicity against C3A hepatocytes. Next, the most promising compounds were evaluated for activity against a multi-drug resistant clinical isolate. The group of amidines was also tested for their ability to kill intracellular M.tb. residing in mouse J774A.1 macrophages. Finally, we report on a correlation between the structural differences of the compounds and their anti-mycobacterial activity.
1,2-Ethane bis-1-amino-4-benzamidine is active against several brain insult and seizure challenges through anti-NMDA mechanisms targeting the 3H-TCP binding site and antioxidant action
Vamecq, Joseph,Maurois, Pierre,Pages, Nicole,Bac, Pierre,Stables, James P.,Gressens, Pierre,Stanicki, Dimitri,Eynde, Jean Jacques Vanden
experimental part, p. 3101 - 3110 (2010/09/03)
Five bis-benzamidines were screened towards murine magnesium deficiency-dependent audiogenic seizures, unravelling two compounds with efficacious doses 50 (ED50) less than 10 mg/kg. They were also screened against maximal electroshock and subcutaneous pentylenetetrazole- induced seizures, and explored for superoxide -scavenging activity. 1,2-Ethane bis-1-amino-4-benzamidine (EBAB) was selected and evaluated in 6 Hz seizure test (ED50= 49 mg/kg) and at 4 μg/kg in focal cerebral ibotenate poisoning in pups (sizes of both white and grey matter wounds were halved). EBAB was further tested on NMDA-induced seizures in mice (ED50=6 mg/kg) and on 3H-TC -binding to a rodent cerebral preparation (IC50=1.4 μM). Taken as a whole, present data emphasise the suitability of bis-benzamidines as templates for designing brain protective compounds.
