- 3H-THIENO[3,4]PYRIMIDIN-4-ONEAND PYRROLOPYRIMID-4-ONE AS GRAM-POSITIVE ANTIBACTERIAL AGENTS
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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,
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Page/Page column 93
(2015/09/28)
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- Catalytic phosphorus(V)-mediated nucleophilic substitution reactions: Development of a catalytic appel reaction
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Catalytic phosphorus(V)-mediated chlorination and bromination reactions of alcohols have been developed. The new reactions constitute a catalytic version of the classical Appel halogenation reaction. In these new reactions oxalyl chloride is used as a consumable stoichiometric reagent to generate the halophosphonium salts responsible for halogenation from catalytic phosphine oxides. Thus, phosphine oxides have been transformed from stoichiometric waste products into catalysts and a new concept for catalytic phosphorus-based activation and nucleophilic substitution of alcohols has been validated. The present study has focused on a full exploration of the scope and limitations of phosphine oxide catalyzed chlorination reactions as well as the development of the analogous bromination reactions. Further mechanistic studies, including density functional theory calculations on proposed intermediates of the catalytic cycle, are consistent with a catalytic cycle involving halo- and alkoxyphosphonium salts as intermediates.
- Denton, Ross M.,An, Jie,Adeniran, Beatrice,Blake, Alexander J.,Lewis, William,Poulton, Andrew M.
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p. 6749 - 6767
(2011/10/02)
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- Synthesis and pharmacological evaluation of benzamide derivatives as selective 5-HT4 receptor agonists
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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.
- Sonda, Shuji,Kawahara, Toshio,Katayama, Kenichi,Sato, Noriko,Asano, Kiyoshi
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p. 3295 - 3308
(2007/10/03)
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- Benzylation of alcoholic hydroxyl groups with benzyl mesylate by using a catalytic amount of lithium tetrakis(pentafluorophenyl)borate in the coexistence of lithium triflate and magnesium oxide
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Several alcohols possessing alkali-labile substituents such as halogen, ester and ketone were effectively benzylated with benzyl mesylate by using a catalytic amount of lithium tetrakis(pentafluorophenyl)borate [LiB(C6F5)4] in the coexistence of lithium triflate (LiOTf) and magnesium oxide (MgO) to afford the corresponding benzyl ethers in good to excellent yields.
- Nakano, Masakazu,Matsuo, Jun-Ichi,Mukaiyama, Teruaki
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p. 1352 - 1353
(2007/10/03)
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- The Acceptor Binding Area of (1->4)-β-D-Galactosyltransferase Can Be Covalently Modified by Photoaffinity Labelling in the Presence of Photolabile Ligands
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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
- Lehmann, Jochen,Petry, Stefan
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p. 1111 - 1116
(2007/10/02)
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- Synthesis of the Cyclophane Tetramethoxyturriane: a Derivative of the Phenolic Cyclophanes of Grevillea striata R. Br.
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The synthesis of 9,10,11,12,13,14,15,16,17,18,19,20,21,22-tetradecahydro-2,4,6,24-tetramethoxy-5,8-ethenobenzocycloeicosene (tetramethoxyturriane) (9) a derivative of the phenolic cyclophanes extracted from the wood of Grevillea striata R.Br., is reported.The key steps in this synthesis were the construction of the biphenyl linkage of the molecule using dihydro-oxazole chemistry and the closure of the macrocycle by oxidative coupling of a diacetylene.
- Sargent, Melvyn V.,Wangchareontrakul, Sirichai
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p. 129 - 132
(2007/10/02)
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