13935-80-3Relevant articles and documents
Glycinamide derivative as well as preparation method and application thereof
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Paragraph 0013; 0031; 0037, (2021/06/12)
The invention discloses a glycinamide derivative as well as a preparation method and application thereof. The derivative with a structural formula as shown in the following formula (I) is provided; and in the formula, R1 is selected from Cl and H, R2 is one selected from H, CH3 and CH2CH3; and X is one selected from NHCH3, NHCH2CH3, N (CH2CH3) 2, a pyrrolyl group and a piperidyl group. During preparation, different phenyl glutaric acid compounds are selected as raw materials and are respectively subjected to amidation reaction twice with an aminoindane hydrochloride derivative and an ethylenediamine derivative to obtain a target derivative. The prepared derivative or the pharmaceutically acceptable salt thereof, or the pharmaceutical composition thereof can be used as an S-adenosyl homocysteine hydrolase inhibitor for the development of antitumor drugs .
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity
Kokkonda, Sreekanth,Deng, Xiaoyi,White, Karen L.,Coteron, Jose M.,Marco, Maria,De Las Heras, Laura,White, John,El Mazouni, Farah,Tomchick, Diana R.,Manjalanagara, Krishne,Rudra, Kakali Rani,Chen, Gong,Morizzi, Julia,Ryan, Eileen,Kaminsky, Werner,Leroy, Didier,Martínez-Martínez, María Santos,Jimenez-Diaz, Maria Belen,Bazaga, Santiago Ferrer,Angulo-Barturen, I?igo,Waterson, David,Burrows, Jeremy N.,Matthews, Dave,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
, p. 5416 - 5431 (2016/07/06)
Malaria persists as one of the most devastating global infectious diseases. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) has been identified as a new malaria drug target, and a triazolopyrimidine-based DHODH inhibitor 1 (DSM265) is in clinical development. We sought to identify compounds with higher potency against Plasmodium DHODH while showing greater selectivity toward animal DHODHs. Herein we describe a series of novel triazolopyrimidines wherein the p-SF5-aniline was replaced with substituted 1,2,3,4-tetrahydro-2-naphthyl or 2-indanyl amines. These compounds showed strong species selectivity, and several highly potent tetrahydro-2-naphthyl derivatives were identified. Compounds with halogen substitutions displayed sustained plasma levels after oral dosing in rodents leading to efficacy in the P. falciparum SCID mouse malaria model. These data suggest that tetrahydro-2-naphthyl derivatives have the potential to be efficacious for the treatment of malaria, but due to higher metabolic clearance than 1, they most likely would need to be part of a multidose regimen.
Green synthesis of benzamides in solvent- and activation-free conditions
Alalla, Affef,Merabet-Khelassi, Mounia,Aribi-Zouioueche, Louisa,Riant, Olivier
supporting information, p. 2364 - 2376 (2014/07/22)
Herein, we describe a clean and ecocompatible pathway for both N-benzoylation and N-acetylation of anilines, amines, diamines, and aminoalcohols using three enol esters with good yields. We have improved the use of vinyl benzoate for the direct introduction of a benzamido-moiety under solvent- and activation-free conditions. The recovered amides are easily isolated by crystallization. Copyright