Preparation and synthetic utility of oxasilacyclopentane acetals derived from siliranes.
Shaw JT and Woerpel KA.
Tetrahedron, 53(48), 16597-16606 (1997)
Y Tanaka et al.
Journal of medicinal chemistry, 37(13), 2071-2078 (1994-06-24)
New compounds were synthesized by structural modification of 1-[1-(4-phenylbutanoyl)-L-prolyl]-pyrrolidine (SUAM-1221, 1) or 1-[1-(benzyloxycarbonyl)-L-proly]prolinal (Z-Pro-prolinal,2) and were tested for in vitro inhibitory activities against purified prolyl endopeptidase (PEP) from canine brain. In a series of compounds which lack a formyl or...
Marco Pallavicini et al.
Bioorganic & medicinal chemistry letters, 14(23), 5827-5830 (2004-10-27)
Homochiral E and Z isomers of N-methylprolinal O-isopropyloxime and (1-methyl-2-pyrrolidinyl)methoxyimines were synthesized as candidate bioisosteres of nicotine and its isoxazolic analogue ABT 418. Two of them, namely (S)-2-isopropylideneaminooxymethyl- and (Z)-(S)-2-ethylideneaminooxymethyl-1-methylpyrrolidine, proved to bind at alpha4beta2 nicotinic acetylcholine receptor with submicromolar...
M Nanri et al.
Nihon yakurigaku zasshi. Folia pharmacologica Japonica, 89(6), 323-329 (1987-06-01)
Based on the results of a previous report that prolyl endopeptidase (PPCE) inhibitors facilitated the acquisition of active avoidance response and retarded the extinction of the response, further studies were made on the effect of PPCE inhibitors on learning and...
Franck Sobrio et al.
Nuclear medicine and biology, 35(3), 377-385 (2008-03-22)
[11C]-SIB-1553A ((+/-)-4-[2-((N-[11C]-methyl)-2-pyrrolidinyl)ethyl]thiophenol) was labelled with carbon-11 (t1/2=20.4 min) and evaluated in vivo as potential radiotracer for noninvasive assessment of the beta4 subunit nicotinic acetylcholine neurotransmission system with positron emission tomography (PET). The labelling precursor was obtained within five steps from...