479079-15-7Relevant academic research and scientific papers
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
Camacho, Cristián M.,Pizzio, Marianela G.,Roces, David L.,Boggián, Dora B.,Mata, Ernesto G.,Bellizzi, Yanina,Barrionuevo, Elizabeth,Blank, Viviana C.,Roguin, Leonor P.
, p. 29741 - 29751 (2021/10/07)
The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridiz
Exploring Heteroaromatic Rings as a Replacement for the Labile Amide of Antiplasmodial Pantothenamides
Guan, Jinming,Spry, Christina,Tjhin, Erick T.,Yang, Penghui,Kittikool, Tanakorn,Howieson, Vanessa M.,Ling, Harriet,Starrs, Lora,Duncan, Dustin,Burgio, Gaetan,Saliba, Kevin J.,Auclair, Karine
, p. 4478 - 4497 (2021/05/04)
Malaria-causing Plasmodium parasites are developing resistance to antimalarial drugs, providing the impetus for new antiplasmodials. Although pantothenamides show potent antiplasmodial activity, hydrolysis by pantetheinases/vanins present in blood rapidly inactivates them. We herein report the facile synthesis and biological activity of a small library of pantothenamide analogues in which the labile amide group is replaced with a heteroaromatic ring. Several of these analogues display nanomolar antiplasmodial activity against Plasmodium falciparum and/or Plasmodium knowlesi, and are stable in the presence of pantetheinase. Both a known triazole and a novel isoxazole derivative were further characterized and found to possess high selectivity indices, medium or high Caco-2 permeability, and medium or low microsomal clearance in vitro. Although they fail to suppress Plasmodium berghei proliferation in vivo, the pharmacokinetic and contact time data presented provide a benchmark for the compound profile likely required to achieve antiplasmodial activity in mice and should facilitate lead optimization.
Preparation method and intermediate of benzodiazepine compound
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, (2020/09/16)
The invention discloses a preparation method of a benzodiazepine compound and an intermediate compound K. The compound K disclosed by the invention can be used for preparing the compound shown as theformula I in one step at high yield. The preparation met
Five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor
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Paragraph 0076; 0077; 0078; 0079, (2017/08/29)
The present invention discloses a five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor, belonging to a compound capable of adjusting the activity of a Wnt single pathway; and the present invention also provides a preparation method of the compound, and application of the compound in preparation of a drug antagonizing the Wnt single pathway. The five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor provided by the present invention is based on a reasonable drug design of a target, is obvious in antineoplastic activity, can be used for developing a new-generation Wnt pathway inhibitor, has an excellent clinical application value and is considerable in market potential.
OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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Page/Page column 83, (2012/05/05)
The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.
Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Page/Page column 32, (2012/08/28)
Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
COMPOUNDS CONTAINING FUSED RINGS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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Page/Page column 82, (2011/11/01)
The invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
INDAZOLE DERIVATIVES AND THEIR USE FOR BLOCKADING VOLTAGE DEPENDENT SODIUM CHANNELS
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Page/Page column 24, (2011/06/19)
The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1, R2, R3 and R4 are as defined herein. The indazole derivatives are capable of bl
TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page/Page column 72-73, (2011/06/11)
Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
(3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING
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Page/Page column 97, (2009/05/29)
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. (Formula)
