128164-72-7Relevant academic research and scientific papers
Cephem derivatives and antimicrobial agents containing the same
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, (2008/06/13)
Herein disclosed are novel cephem compounds represented by the following general formula (I), and antimicrobial agents which contains at least one of such novel cephem compounds as an active ingredient.
Tetrahydropyridyloxadiazoles: Semirigid Muscarinic Ligands
Showell, Graham A.,Gibbons, Tracey L.,Kneen, Clare O.,MacLeod, Angus M.,Merchant, Kevin,et al.
, p. 1086 - 1094 (2007/10/02)
Recent studies have described novel azabicycle-based muscarinic agonists which readily penetrate into the central nervous system and are capable of displaying high efficacy at cortical sites.The current paper describes the synthesis and biochemical assesment of semirigid muscarinic ligands which were used to map the requirements of the cortical muscarinic receptor and to study the degree of conformational flexibility required to cause receptor activation.Analogues 6 and 9 provide high-efficacy muscarinic agonist at cortical sites; however, C-alkylation on the tetrahydropyridine ring resulted in more rigid analogues and showed lower predicted efficacy.Molecular mechanics calculations indicated a preference for the E rotameric form.This conformation was also observed in the X-ray crystal structure of ethenyloxadiazole 12.The new compounds were tested in biochemical assay designed to measure receptor affinity and to predict cortical efficacy.
Synthesis and muscarinic activities of 1,2,4-thiadiazoles
MacLeod,Baker,Freedman,Patel,Merchant,Roe,Saunders
, p. 2052 - 2059 (2007/10/02)
A series of novel 1,2,4-thiadiazoles bearing a mono- or bicyclic amine at C5 were prepared. Quinuclidine and 1-azabicyclo[2.2.1]heptane derivatives were synthesized by reaction of the lithium enolate of the 3-methoxycarbonyl compounds followed by ester hy
