874-61-3Relevant academic research and scientific papers
An endoperoxide-based hybrid approach to deliver falcipain inhibitors inside malaria parasites
Oliveira, Rudi,Newton, Ana S.,Guedes, Rita C.,Miranda, Daniela,Amewu, Richard K.,Srivastava, Abhishek,Gut, Jiri,Rosenthal, Philip J.,O'Neill, Paul M.,Ward, Stephen A.,Lopes, Francisca,Moreira, Rui
, p. 1528 - 1536 (2013)
The emergence of artemisinin-resistant Plasmodium falciparum malaria in Southeast Asia has reinforced the urgent need to discover novel chemotherapeutic strategies to treat and control malaria. To address this problem, we prepared a set of dual-acting tet
4-Oxocyclohexanecarboxylic acid: Hydrogen bonding in the monohydrate of a δ-keto acid
Barcon, Alan,Brunskill, Andrew P.J.,Thompson, Hugh W.,Lalancette, Roger A.
, p. o140-o142 (2004)
The title monohydrate, C7H10O 3·H2O, aggregates as a complex hydrogen-bonding network, in which the water molecule accepts a hydrogen bond from the carboxyl group of one molecule and donates hydrogen bonds to ketone and carboxyl C=O functions in two additional molecules, yielding a sheet-like structure of parallel ribbons. The keto acid adopts a chiral conformation through rotation of the carboxyl group by 62.50 (15)° relative to the plane defined by its point of attachment and the ketone C and O atoms. Two C - H=O close contacts exist in the structure.
TGF-betaR1 inhibitor and application thereof
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Paragraph 1061; 1063-1065, (2020/06/09)
The invention belongs to the field of medical chemistry, and particularly relates to a compound serving as a TGF-betaR1 inhibitor and application of the compound. Specifically, the invention providesa compound shown as a formula I or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the compounds or the composition to treatment and/or prevention of TGF-betaR1 related diseases, such as cancers, tissue hyperplasia diseases, fibrosis and inflammatory diseases. The compound provided by the invention shows significant inhibitory activity on TGF-betaR1 kinase, and is very expected to become a therapeutic agent for TGF-betaR1 related diseases.
BETUIN DERIVATIVES FOR PREVENTING OR TREATING HIV INFECTIONS
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Paragraph 00214, (2017/02/24)
The present invention relates to compounds characterized by having a structure according to the following Formula I, or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
COMPOUNDS WITH HIV MATURATION INHIBITORY ACTIVITY
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Paragraph 00216, (2017/04/11)
The present invention relates to compounds characterized by having a structure according to the following Formula (I), or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
Epsilon-caprolactone derivatives and preparation method and application thereof
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Paragraph 0040; 0041, (2017/11/16)
The invention relates to the field of biomedical materials, and concretely relates to novel water-soluble epsilon-caprolactone derivatives for preparing biomedical polymer materials with biodegradability, wherein the structural formula of the derivatives
NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
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Page/Page column 73; 223, (2016/06/28)
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
BENZOTHIAZOLE DERIVATIVES AND A USE THEREOF FOR THE TREATMENT OF CANCER
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Paragraph 0088; 0089; 0090, (2016/02/18)
Provided are a compound represented by Formula I, a pharmaceutically acceptable salt thereof, or a solvate thereof; and a pharmaceutical composition for cancer treatment and a pharmaceutical composition for a radiation sensitizer for cancer treatment, eac
Photoinduced Oxidation of Secondary Alcohols Using 4-Benzoylpyridine as an Oxidant
Kamijo, Shin,Tao, Keisuke,Takao, Go,Tonoda, Hiroshi,Murafuji, Toshihiro
supporting information, p. 3326 - 3329 (2015/07/15)
Photoinduced oxidation of secondary alcohols to ketones was achieved by utilizing an equimolar amount of 4-benzoylpyridine as an oxidant. This transformation proceeds at ambient temperature and exhibits high compatibility with polar functionalities including benzoyl, silyl, and methoxymethyl alcohol protecting groups as well as tosyloxy, bromo, sulfonyl, carbamate, ester, and carboxylic acid units. The present oxidation is solely promoted by the action of organic molecules without the aid of metallic reagents. (Chemical Equation Presented).
Discovery of 6-phenylpyrimido[4,5- B ][1,4]oxazines as potent and selective Acyl CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents
Fox, Brian M.,Sugimoto, Kazuyuki,Iio, Kiyosei,Yoshida, Atsuhito,Zhang, Jian,Li, Kexue,Hao, Xiaolin,Labelle, Marc,Smith, Marie-Louise,Rubenstein, Steven M.,Ye, Guosen,McMinn, Dustin,Jackson, Simon,Choi, Rebekah,Shan, Bei,Ma, Ji,Miao, Shichang,Matsui, Takuya,Ogawa, Nobuya,Suzuki, Masahiro,Kobayashi, Akio,Ozeki, Hidekazu,Okuma, Chihiro,Ishii, Yukihito,Tomimoto, Daisuke,Furakawa, Noboru,Tanaka, Masahiro,Matsushita, Mutsuyoshi,Takahashi, Mitsuru,Inaba, Takashi,Sagawa, Shoichi,Kayser, Frank
supporting information, p. 3464 - 3483 (2014/05/20)
The discovery and optimization of a series of acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors based on a pyrimido[4,5-b][1,4]oxazine scaffold is described. The SAR of a moderately potent HTS hit was investigated resulting in the discovery of phenylcyclohexylacetic acid 1, which displayed good DGAT1 inhibitory activity, selectivity, and PK properties. During preclinical toxicity studies a metabolite of 1 was observed that was responsible for elevating the levels of liver enzymes ALT and AST. Subsequently, analogues were synthesized to preclude the formation of the toxic metabolite. This effort resulted in the discovery of spiroindane 42, which displayed significantly improved DGAT1 inhibition compared to 1. Spiroindane 42 was well tolerated in rodents in vivo, demonstrated efficacy in an oral triglyceride uptake study in mice, and had an acceptable safety profile in preclinical toxicity studies.
