8-Aminobicyclo[3.2.1]octanes: synthesis and anti-viral activity

Exploring the Requirements for the Hydrophobic Scaffold and Polar Amine in Inhibitors of M2 from Influenza A Virus

“…However, very few chemotypes other than the adamantane scaffold have been studied for A/M2 channel inhibition 2, 13. One exception is a spiro-piperidine 1 , which emerged from our previous structure-activity relationship (SAR) study of 2-[3-azaspiro(5,5)undecanol]-2-imidazoline (BL-1743) 14.…”

Green synthesis of fluorinated biaryl derivatives via thermoregulated ligand/palladium-catalyzed Suzuki reaction

“…1 H NMR spectra were recorded on a Brucker Advance II 400 spectrometer. 13 C NMR spectra were recorded at 100 MHz using TMS as internal standard. Mass spectroscopy data of the products were collected on an MS-EI instrument.…”

“…Generally, synthetic methods for fluorinated biaryls are classified into two types: carbon-fluorine bond-forming reactions and carbonecarbon bond-forming reactions [1,2]. In the synthesis of fluorinated biaryls via the carbonecarbon bond-forming reactions, the cross-couplings involving organochlorosilanes [7,8], potassium aryltrifluoroborates [9e11], Grignard reagents [12,13] or organolithium reagents [14], have been developed, respectively. However, these methods require the use of highly specialized reagents.…”

Synthesis, anticonvulsant activity and <i>in silico</i> study of some novel amino acids incorporated bicyclo compounds

“…Hence, with all of these factors in mind, it has been suggested that the focus of epilepsy research should be directed to identifying the underlying mechanism of epileptogenesis and the subsequent "expression" of seizure activity, rather than resorting primarily to symptom control, that is, mere suppression of seizures (McNamara, 2001). The analogues of bicyclic systems, 8, 10-diza-bicyclo [4.3.1] decane and 3, 10-diza-bicyclo [4.3.1] decane bicyclo compounds, have been found to possess a wide range of biological activities, which include analgesic, anti inflammatory (Peter 2008, Nagaev et al, 1999, Pinna et al, 2000, muscarinic receptor antagonist (Myoung et al, 2003), antibacterial (Smirnova et al, 1995), antiviral (Miller et al, 2001), antiprotozoal (Seeacher et al, 2005) and antispasmolytic (Rajdan et al, 1987) but still no one has reported/studied, such compounds as anticonvulsants. The reason to incorporate biologically friendly amino acids into pharmacologically active moiety is not only to minimize the side effects of the metabolites of the parent compound upon metabolism in the body but also to direct the drug for specific site and in order to enhance the hydrophilicity of the synthesized candidates, like bicyclo compounds may exhibit potent anticonvulsant activity.…”