100847-50-5Relevant articles and documents
3H-THIENO[3,4]PYRIMIDIN-4-ONEAND PYRROLOPYRIMID-4-ONE AS GRAM-POSITIVE ANTIBACTERIAL AGENTS
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Page/Page column 93, (2015/09/28)
The invention relates to novel heteroaromatic derivatives of formula (I) and their addition salts thereof with acids and bases; their preparation, their use as drugs and pharmaceutical compositions and associations containing them. wherein A, B, T, V, X and Y represent organic substituents as defined herein, The compounds of formula (I) are able to inhibit the activity of the Gram-positive bacterial DltA enzyme and they are used to prevent and/or treat Gram-positive bacterial infections in humans or animals, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity,
Synthesis and pharmacological evaluation of benzamide derivatives as selective 5-HT4 receptor agonists
Sonda, Shuji,Kawahara, Toshio,Katayama, Kenichi,Sato, Noriko,Asano, Kiyoshi
, p. 3295 - 3308 (2007/10/03)
It is thought that selective 5-HT4 receptor agonists-such as 4-amino-5-chloro-2-methoxy-N-[1-(6-oxo-6-phenylhexyl)piperidin-4-ylmethyl] benzamide (2)-have the ability to enhance both upper and lower gastrointestinal motility without any significant adverse effects. Modification of 2 was performed. Variation of the piperidin-4-ylmethyl moiety of 2 led to a decrease in the binding affinity for the 5-HT4 receptor. Following conversion of the carbonyl group on the benzoyl part to a hydroxyl or sulfoxide group, the binding affinity for the 5-HT4 receptor was retained although the effect on defecation was reduced. Many of the 4-amino-5-chloro-2-methoxy-N- (piperidin-4-ylmethyl)benzamides that had a ether or sulfide moiety in the side-chain part at the 1-position of the piperidine exhibited high affinity for the 5-HT4 receptor. Among these, phenylthio 41c and benzylthio derivative 44 were selective 5-HT4 receptor agonists, and had a similar effect on defecation to compound 2.
The Acceptor Binding Area of (1->4)-β-D-Galactosyltransferase Can Be Covalently Modified by Photoaffinity Labelling in the Presence of Photolabile Ligands
Lehmann, Jochen,Petry, Stefan
, p. 1111 - 1116 (2007/10/02)
Three spacer-modified oligosaccharides (SMOs) 2, 3, and 4, consisting of two nonreducing GlcNAc end groups, O-linked by an acyclic 10-membered spacer carrying azi groups in positions 2, 3, or 5, proved to be acceptor substrates for (1->4)-β-D-Galactosyltransferase (Gal-T) and models of the natural biantennary core heptasaccharide of N-glycoproteins.Photoaffinity labelling with each compound takes place with different efficiencies.This is an indication of regioselective chemical modification of the enzyme's extended binding area, because the reactive carbene in each case is placed in a different chemical surrounding.A radioactive SMO was used to prove the irreversible chemical modification of the acceptor binding site. - Key Words: Photoaffinity labelling / Diazirines / Galactosyltransferase / Spacer-modified oligosaccharides