538-37-4Relevant articles and documents
Novel antibody-antibiotic conjugate eliminates intracellular S. aureus
Lehar, Sophie M.,Pillow, Thomas,Xu, Min,Staben, Leanna,Kajihara, Kimberly K.,Vandlen, Richard,DePalatis, Laura,Raab, Helga,Hazenbos, Wouter L.,Hiroshi Morisaki,Kim, Janice,Park, Summer,Darwish, Martine,Lee, Byoung-Chul,Hernandez, Hilda,Loyet, Kelly M.,Lupardus, Patrick,Fong, Rina,Yan, Donghong,Chalouni, Cecile,Luis, Elizabeth,Khalfin, Yana,Plise, Emile,Cheong, Jonathan,Lyssikatos, Joseph P.,Strandh, Magnus,Koefoed, Klaus,Andersen, Peter S.,Flygare, John A.,Wah Tan, Man,Brown, Eric J.,Mariathasan, Sanjeev
, p. 323 - 328 (2015)
Staphylococcus aureus is considered to be an extracellular pathogen. However, survival of S. aureus within host cells may provide a reservoir relatively protected from antibiotics, thus enabling long-term colonization of the host and explaining clinical f
Synthesis, anti-platelet aggregation activity evaluation and structure–activity relationships of a series of novel purine derivatives
Li, Shunlai,Zhou, Cheng,Yu, Mingwu,He, Qiwen,Du, Hongguang
, p. 2889 - 2903 (2020)
This article described how further extensive variation of the substituents on the purine scaffold of adenosine triphosphate (ATP), and the human anti-platelet aggregation activities were modified in order to find exploitation of the structure–activity relationships (SAR). A series of novel designed 6-alkylamino-2-alkylthio-9-hydroxyalkyl(carbalkoxy) purine derivatives were synthesized via a modification procedure, and the human anti-platelet aggregation activities were evaluated. The SAR of these compounds were analyzed in detail, and the results of the structural requirements of the substituents to improve potency may provide a basis for the development of potent P2Y12 antagonists.
Investigating the role of the geminal dimethyl groups of coenzyme A: Synthesis and studies of a didemethyl analogue
Vogel, Kurt W.,Stark, Lucy M.,Mishra, Pranab K.,Yang, Wei,Drueckhammer, Dale G.
, p. 2451 - 2460 (2000)
An analogue 2 of coenzyme A (CoA) has been prepared in which the geminal methyl groups are replaced with hydrogens. An NMR titration study was conducted and shifts in frequency of protons in the pantetheine portion of the molecule upon titration of the adenine base were observed as has been previously reported with CoA. These studies indicate that the geminal dimethyl groups are not essential for adoption of a partially folded conformation in solution. Based on 1H-1H coupling constants, the distribution of conformations about the carbon-carbon bonds in the region of the methyl deletion were estimated. The results suggest that the conformer distribution is similar to that of CoA, but with small increases in population of the anti conformers. A simple model compound containing the didemethyl pantoamide moiety was prepared and subjected to similar conformational analysis. The coupling constants and predicted conformer distribution were almost identical to that of the CoA analogue, indicating that the conformer distribution is controlled by local interactions and not influenced by interactions between distant parts of the CoA molecule. The acetyl derivative of 2 was a fairly good substrate for the acetyl-CoA utilizing enzymes carnitine acetyltransferase, chloramphenicol acetyltransferase, and citrate synthase, with 1.3- to 10-fold increased K(m) values and 2.5- to 11-fold decreases in V(max). The combined results indicate that the geminal dimethyl groups of CoA have modest effects on function and minimal effects on conformation. Copyright (C) 2000 Elsevier Science Ltd.
Antiplasmodial Mode of Action of Pantothenamides: Pantothenate Kinase Serves as a Metabolic Activator Not as a Target
De Villiers, Marianne,Spry, Christina,Macuamule, Cristiano J.,Barnard, Leanne,Wells, Gordon,Saliba, Kevin J.,Strauss, Erick
, p. 527 - 541 (2017)
N-Substituted pantothenamides (PanAms) are pantothenate analogues with up to nanomolar potency against blood-stage Plasmodium falciparum (the most virulent species responsible for malaria). Although these compounds are known to target coenzyme A (CoA) bio
Heterocyclic amide compound, pharmaceutical composition containing heterocyclic amide compound, preparation method of heterocyclic amide compound and application of heterocyclic amide compound
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Paragraph 0311-0314, (2020/04/17)
The invention relates to a heterocyclic amide compound, a pharmaceutical composition containing the heterocyclic amide compound, a preparation method of the heterocyclic amide compound and an application of the heterocyclic amide compound serving as an agonist of stimulator of interferon gene (STING). More specifically, the invention relates to the heterocyclic amide compound; the heterocyclic amide compound is capable of stimulating the production of interferon, thereby being used as an immunomodulator for treatment of STING-mediated diseases or disease conditions such as cancer, infectious diseases, inflammation, immune-related diseases and the like.
METHODS AND COMPOSITIONS FOR PRODRUG FORMS OF SPECTINOMYCIN AND SPECTINAMIDE ANALOGS
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Paragraph 0589-0590; 0602; 0609; 0615; 0621, (2020/06/01)
In one aspect, the disclosure relates to substituted spectinomycin analogs, including substituted aminomethyl spectinomycin analogs and substituted spectinamide analogs, with increased tolerability and safety, including improved tolerability to parenteral
PANTETHEINE DERIVATIVES AND USES THEREOF
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Paragraph 2121, (2020/06/19)
The present disclosure relates to compounds of Formula (I), (II), or (II'): (I), (II), (II'), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
COMPOSITIONS COMPRISING ENZYME CLEAVABLE LINKER PLATFORMS AND CONJUGATES THEREOF
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Page/Page column 71; 72, (2021/01/23)
The present invention relates to a cleavable linker platform. In particular, the invention relates to construction of an enzyme cleavable linker platform conjugated to a drug or a diagnostically relevant compound, a biomolecule, and an enzyme cleavable group, for which cleavage of the enzyme cleavable group leads to release of the drug or diagnostically relevant compound.
NEUROSTEROID COMPOUNDS AND METHODS FOR THEIR PREPARATION AND USE IN TREATING CENTRAL NERVOUS SYSTEM DISORDERS
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Paragraph 0103; 0144, (2019/11/12)
Described herein is the chemical structure of neurosteroid derivative compounds, methods of synthesizing the derivatives, and their uses in treating disorders, including those of the central nervous system. These compounds are readily synthesized and have improved pharmaceutical properties, including water solubility, compared to known neurosteroids.
UREA DERIVATIVES AS INHIBITORS OF ASK1
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Paragraph 0121, (2019/06/05)
The present technology is directed to compounds, compositions, and methods related to inhibition of ASK1. In particular, the present compounds (e.g., compounds of Formula I as defined herein) and compositions may be used to treat ASK1-mediated disorders and conditions, including, e.g., fibrotic diseases and acute and chronic liver diseases, among others.
