21038-63-1Relevant academic research and scientific papers
Structure-activity relationship and molecular modelling studies of quinazolinedione derivatives MMV665916 as potential antimalarial agent
Albrecht, Sébastien,Florent, Isabelle,Mouray, Elisabeth,Mourot, Laura,Schmitt, Marjorie,Spichty, Martin
supporting information, (2021/11/22)
A series of new quinazolinedione derivatives have been readily synthesized and evaluated for their in vitro antiplasmodial growth inhibition activity. Most of the compounds inhibited P. falciparum FcB1 strain in the low to medium micromolar concentration. The 2-ethoxy 8ag’, 2-trifluoromethoxy 8ai’ and 4-fluoro-2-methoxy 8ak’ showed the best inhibitory activity with EC50 values around 5 μM and were non-toxic to the primary human fibroblast cell line AB943. However, these compounds were less potent than the original hit MMV665916, which showed remarkable growth inhibition with EC50 value of 0.4 μM and presented the highest selectivity index (SI > 250). In addition, a novel approach for determining the docking poses of these quinazolinedione derivatives with their potential protein target, the P. falciparum farnesyltransferase PfFT, was investigated.
Synthesis of novel 2,4-disubstituted 3H-pyrido[3,2-e][1,4]diazepin-5-ones and 2,4-disubstituted 3H-pyrido[2,3-e][1,4]diazepin-5-ones derivatives via regioselective thionation and nucleophilic substitutions reactions
El Bouakher, Abderrahman,Prié, Gildas,Aadil, Mina,Akssira, Mohamed,Viaud-Massuard, Marie-Claude
, p. 5086 - 5091 (2013/07/05)
An efficient synthesis leading to novel 2,4-disubstituted 3H-pyrido[3,2-e][1,4]diazepin-5-ones and 2,4-disubstituted 3H-pyrido[2,3-e][1,4] diazepin-5-ones derivatives is presented, using the condensation of ethyl 2-(benzylamino)acetate or ethyl 2-(4-methoxybenzylamino)acetate with 1H-pyrido[3,2-d][1,3]oxazine-2,4-diones and 1H-pyrido[2,3-d][1,3]oxazine-2,4- diones. This synthesis gives 4-substituted 3-hydro-1H-pyrido[3,2-e][1,4] diazepine-2,5-diones and 4-benzyl-3,4-dihydro-1H-pyrido[2,3-e][1,4]diazepine-2, 5-diones in good yields. Finally, after a regioselective thionation and nucleophilic substitutions reactions, various bis-functionalized 1,4-diazepines were easily obtained in excellent yields. These results open an access way to a library of novel bis-functionalized pyrido-1,4-diazepines.
A convenient synthesis of new pyrido[3,2-e][1,4]diazepine-2,5-diones and pyrido[2,3-e][1,4]diazepine-2,5-diones
El Bouakher, Abderrahman,Laborie, Hélne,Aadil, Mina,El Hakmaoui, Ahmed,Lazar, Said,Akssira, Mohamed,Viaud-Massuard, Marie-Claude
scheme or table, p. 5077 - 5080 (2011/10/09)
A convenient synthesis of a series of pyrido[3,2-e][1,4]-diazepine-2,5- diones 8 and pyrido[2,3-e][1,4]diazepine-2,5-diones 9, is reported using the condensation of α-amino acid methyl ester derivatives with 1H-pyrido[3,2-d][1,3]oxazine-2,4-dione and 1H-p
BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS
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Page/Page column 87-88, (2010/10/03)
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together
NOVEL 1,8-NAPHTHYRIDINE COMPOUNDS
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Page/Page column 21, (2008/12/08)
The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Anti-infective agents
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Page 37, (2010/02/06)
Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
Anti-infective agents
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Page/Page column 70, (2010/02/08)
The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HC
NOVEL COMPOUNDS
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Page/Page column 37, (2010/02/07)
Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula (I) R1, R2, R3, R4, R5, R6, X and Y are as d
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents
Norman, Mark H.,Navas III, Frank,Thompson, James B.,Rigdon, Greg C.
, p. 4692 - 4703 (2007/10/03)
Heterocyclic analogues of 1192U90, 2-amino-N-(4-(4-(1,2-benzisothiazol- 3-yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1), were prepared and evaluated as potential antipsychotic agents. These analogues were evaluated in vitro for their binding to the dopamine D2, serotonin 5-HT2, and serotonin 5-HT(1a) receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. Nine different types of heterocyclic carboxamides were studied in this investigation (i.e., pyridine- , thiophene-, benzothiophene-, quinoline-, 1,2,3,4-tetrahydroquinoline-, 2,3- dihydroindole-, indole-, benzimidazole-, and indazolecarbox-amides). Two derivatives exhibited potent in vivo activities comparable to 1: 3-amino-N- (4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2-pyridinecarboxamide (16) and 3-amino-N-(4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2- thiophenecarboxamide (29). Furthermore, these derivatives were found to be much less active in behavioral models predictive of extrapyramidal side effects than in the mouse climbing assay, which predicts antipsychotic activity. Carboxamides 16 and 29 were selected for further evaluation as potential backup compounds to 1.
