- Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications
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Reversible inhibitors (e.g., pyridostigmine bromide, neostigmine bromide) of carbamate origin are used in the early treatment of Myasthenia gravis (MG) to block acetylcholinesterase (AChE) native function and conserve efficient amount of acetylcholine for
- Musilek, Kamil,Komloova, Marketa,Zavadova, Vlasta,Holas, Ondrej,Hrabinova, Martina,Pohanka, Miroslav,Dohnal, Vlastimil,Nachon, Florian,Dolezal, Martin,Kuca, Kamil,Jung, Young-Sik
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p. 1763 - 1766
(2010/08/21)
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- Dependence of amine-accelerated silicate condensation on amine structure
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Diatoms are known to grow elaborate nano- and microstructured silica shells by depositing material from precursor-containing vesicles at mild temperature and pH. Oligo(1-methylazetane) and related moieties, in some cases attached to proteins, are believed
- Robinson, David B.,Rognlien, Judith L.,Bauer, Christina A.,Simmons, Blake A.
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p. 2113 - 2119
(2008/02/07)
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- Binding selectivity of cucurbit[7]uril: Bis(pyridinium)-1,4-xylylene versus 4,4′-bipyridinium guest sites
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The binding interactions between the host cucurbit[7]uril (CB7) and a series of linear guests containing bis(pyridinium)-1,4-xylylene and/or 4,4′-bipyridinium residues were investigated by 1H NMR spectroscopy. CB7 was found to exhibit considerable binding selectivity for bis-(pyridinium)-1,4-xylylene over 4,4′-bipyridinium sites. New pseudo-rotaxane and rotaxane compounds were synthesized utilizing the host-guest interactions between CB7 and the surveyed guests.
- Sindelar, Vladimir,Moon, Kwangyul,Kaifer, Angel E.
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p. 2665 - 2668
(2007/10/03)
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- Design and synthesis of piperidine-3-carboxamides as human platelet aggregation inhibitors
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A detailed structure-activity analysis was carried out using eight 1- alkyl(aralkyl)nipecotamides (type 5), 33 bis-nipecotamidoalkanes and aralkanes (type 6), and 7 N,N'-bis(nipecotoyl)-piperazines (type 7) as inhibitors of human platelet aggregation. Steric factors played an important role in determining the activity of type 5 compounds possessing an appropriate degree of hydrophobic character. Types 6 and 7 compounds were more potent than the corresponding type 5 molecules. Hydrophobic character appeared to influence the activity of type 6 compounds. A 3-substituent on the piperidine ring was necessary for antiplatelet activity; the substituent should be preferably an amide with its C attached directly to the ring. 3,5- Disubstitution and 2-substitution led to a decline in activity. Optimal activity was attained when the two nipecotoyl ring N atoms were connected by an aralkyl group, and separated by ~7 ?. It is suggested that van der Waals forces and π interactions may govern the inhibitor-platelet interaction. The most potent type 6 inhibitor was α,α'-bis[3-(N-ethyl-N- butylcarbamoyl)piperidino]-p-xylene (6i). The most potent type 5 compound was 1-decyl-3-(N,N-diethylcarbamoyl)piperidine (5a). Any substitution on the piperazine ring of type 7 compounds led to a decline in activity, the most active analog being N,N'-bis(1-decylnipecotoyl)piperazine (7a). It is suggested that nipecotamides interact with anionic platelet sites located 7 ? from each other and connected by a hydrophobic well.
- Zheng,Salgia,Thompson,Dillingham,Bond,Feng,Prasad,Gollamudi
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p. 180 - 188
(2007/10/02)
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