26976-72-7Relevant academic research and scientific papers
PANTETHEINE DERIVATIVES AND USES THEREOF
-
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.
Reactions of hydrogen peroxide with acetylacetone and 2- acetylcyclopentanone
Novikov,Shestak
, p. 2171 - 2190 (2014/11/07)
A reaction of acetylacetone with equimolar amount of concentrated aqueous H2O2 in both organic solvents (ButOH, AcOH) and water at various temperatures gave the corresponding 3,5-dihydroxy-1,2- dioxolanes with different configuration of stereogenic centers. In the pres-ence of an excess of H2O2, 3,5-dihydroxy-1,2-dioxolanes were converted to a mixture of 5-hydroperoxy-3-hydroxy-1,2-dioxolanes and further to a mixture of dimeric 1,2-dioxolan-3-ylperoxides. All the peroxides formed exist in solutions as equilibrium mixtures with the starting reagents. A prolonged reflux of solutions of 3,5-dihydroxy-1,2-dioxolanes in ButOH in the presence of a large excess of H2O2 led to the skeletal rearrangements of the substrates to a mixture of propionic acid and hydroxyacetone, which underwent further oxidative transfor-mations. Unlike acetylacetone, 2-acetylcyclopentanone reacted with H2O2 in aqueous phase or in solutions in ButOH under thermodynamic or kinetic control with the formation of the corresponding 5-hydroperoxy-3-hydroxy- 1,2-dioxolanes, rather than 3,5-dihydroxy-1,2-di-oxolanes. Thermodynamically controlled process in solution in AcOH gave a mixture of all four possible hydroperoxyhydroxy-1,2-dioxolanes. These cyclic peroxides in solutions in ButOH or AcOH readily converted to a mixture of AcOH, glutaric, α-methyladipic, and α-hydroxy-α-methyladipic acids. An active α-hydroxylation of the substrate was observed upon reflux of a solution of 2-acetylcyclopentanone and H2O2 in AcOH.
Thermal and photochemical oxidation of 2-acetylcyclopentanone with atmospheric oxygen
Novikov,Shestak
, p. 1099 - 1110 (2013/07/26)
The major products of thermal (acetone, CaCl2 excess, reflux) and photochemical (acetone or CCl4, room temperature) oxidation of 2-acetylcyclopentanone with atmospheric oxygen are 2-acetyl-2- hydroxycyclopentanone, 2-acetyl-2-hydroxy
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: Identification of the cycloalkylcarboxylic acids
Lamarche, Matthew J.,Leeds, Jennifer A.,Amaral, Kerri,Brewer, Jason T.,Bushell, Simon M.,Dewhurst, Janetta M.,Dzink-Fox, Joanne,Gangl, Eric,Goldovitz, Julie,Jain, Akash,Mullin, Steve,Neckermann, Georg,Osborne, Colin,Palestrant, Deborah,Patane, Michael A.,Rann, Elin M.,Sachdeva, Meena,Shao, Jian,Tiamfook, Stacey,Whitehead, Lewis,Yu, Donghui
supporting information; experimental part, p. 8099 - 8109 (2012/01/30)
4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for their activity against Gram positive bacterial infections. Optimization efforts focused on improving the physicochemical properties (e.g., aqueous solubility and chemical stability) of the 4-aminothiazolyl natural product template while improving the in vitro and in vivo antibacterial activity. Structure-activity relationships were defined, and the solubility and efficacy profiles were improved over those of previous analogues and 1. These studies identified novel, potent, soluble, and efficacious elongation factor-Tu inhibitors, which bear cycloalkylcarboxylic acid side chains, and culminated in the selection of development candidates amide 48 and urethane 58.
NOVEL NITROSO COMPOUNDS AS NITROXYL DONORS AND METHODS OF USE THEREOF
-
Page/Page column 44, (2009/12/04)
The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
BORON-CONTAINING SMALL MOLECULES
-
Page/Page column 179-180, (2009/01/23)
This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
ENHANCED TISSUE PENETRATION PRODRUGS
-
Page/Page column 38, (2010/11/25)
The present invention relates to derivatives of carboxy-containing drugs for enhancing tissue penetration and pharmaceutical compositions comprising such derivatives.
A prodrug system for hydroxylamines based on esterase catalysis
Conejo-Garcia, Ana,Schofield, Christopher J.
, p. 4004 - 4009 (2007/10/03)
The synthesis and reactivity of hydroxy hydroxamates as models for a prodrug form of hydroxylamine are described. γ-Hydroxy hydroxamates were found to enable hydroxylamine release via lactonisation. Hydroxamates were found to undergo esterase catalysed hydrolysis.
Acyl guanidine and amidine prodrugs
-
, (2008/06/13)
Acyl guanidine, thioguanidine and amidine compounds are provided which have the structure*(formula 06)* wherein Z is a substructure which when linked to*(formula 07)* forms a prodrug of compounds with pharmaceutically active properties. In preferred embodiments, Z is a thrombin inhibitor substructure containing residues binding at the distal and proximal sites with the proviso that Z does not contain boron or a boron-containing moiety. Ax and A'x may be the same or different and are independently selected from Acyl, H or alkyl, at least one of Ax and A'x being Acyl; and including all stereoisomers thereof, and pharmaceutically acceptable salts thereof.
