38250-16-7Relevant academic research and scientific papers
Radiolysis of kaempferol in water/methanol mixtures. Evaluation of antioxidant activity of kaempferol and products formed
Marfak, Abdelghafour,Trouillas, Patrick,Allais, Daovy-Paulette,Champavier, Yves,Calliste, Claude-Alain,Duroux, Jean-Luc
, p. 1270 - 1277 (2003)
Oxidative reaction between hydroxymethyl radical (CH2OH) and kaempferol, in methanol and methanol/water mixtures, was studied by γ-radiolysis using a 60Co source. Radiolysis was performed with concentrations and doses ranging from 5 × 10-5 M to 5 × 10-3 M and from 0.5 kGy to 14 kGy, respectively. Kaempferol degradation was followed by HPLC, Results showed that CH2OH reacts with kaempferol at the 3-OH group and produces two depsides (K1 and K2) and other products including K3. K1, K2, and K3 were identified by NMR, LC-MS, and HRMS. The kaempferol degradation pathway leading to the K1, K2, and K3 formation is proposed. It was observed that the more water concentration in the irradiation medium increases, the more K2 concentration increases. Comprehension of food preservation is not clear because many phenomena occurring during irradiation are not established. Radiolysis of kaempferol in water/methanol mixtures helps to elucidate the phenomenon and it is possible that during the treatment of nutriments by γ-irradiation, a series of products such as depside K2 could be formed. Antioxidant properties of kaempferol radiolysis products were evaluated according to their capacity to decrease the EPR DPPH (1,1 -diphenyl2-picrylhydrazil) signal and to inhibit superoxide radicals formed by the enzyme reaction xanthine + xanthine oxidase .
ANTIFUNGAL ANTIBIOTICS FROM PISOLITHUS TINCTORIUS
Tsantrizos, Youla S.,Kope, Harry H.,Fortin, J. Andre,Ogilvie, Kelvin K.
, p. 1113 - 1118 (1991)
The antibiotic compounds p-hydroxybenzoylformic acid and (R)-(-)-p-hydroxymandelic acid were isolated from the growth culture Pisolithus ti
A COMPOUND FOR THE DETERMINATION OF THE PROTEIN FKBP12 AND A SENSOR UNIT COMPRISING IT
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, (2021/06/26)
The present invention relates to novel compounds useful as sensors for the rapid and specific determination of the FKBP12 protein, a peptidyl-prolyl cis-trans isomerase (PPlase), the levels of which in the biological fluids of a subject change if the subject is affected by pathological conditions, in particular neurodegenerative diseases, such as the Parkinson's disease and the Alzheimer's syndrome, tumour pathologies, autoimmune diseases, or if that subject is in a phase of acute rejection after organ transplantation.
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
Le Manach, Claire,Dam, Jean,Woodland, John G.,Kaur, Gurminder,Khonde, Lutete P.,Brunschwig, Christel,Njoroge, Mathew,Wicht, Kathryn J.,Horatscheck, André,Paquet, Tanya,Boyle, Grant A.,Gibhard, Liezl,Taylor, Dale,Lawrence, Nina,Yeo, Tomas,Mok, Sachel,Eastman, Richard T.,Dorjsuren, Dorjbal,Talley, Daniel C.,Guo, Hui,Simeonov, Anton,Reader, Janette,Van Der Watt, Mari?tte,Erlank, Erica,Venter, Nelius,Zawada, Jacek W.,Aswat, Ayesha,Nardini, Luisa,Coetzer, Theresa L.,Lauterbach, Sonja B.,Bezuidenhout, Belinda C.,Theron, Anjo,Mancama, Dalu,Koekemoer, Lizette L.,Birkholtz, Lyn-Marie,Wittlin, Sergio,Delves, Michael,Ottilie, Sabine,Winzeler, Elizabeth A.,Smith, Dennis,Fidock, David A.,Street, Leslie J.,Basarab, Gregory S.,Duffy, James,Chibale, Kelly
supporting information, p. 2291 - 2309 (2021/03/01)
A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity (50 nM) together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay. Mechanistic studies through resistance selection with one of the analogues followed by whole-genome sequencing implicated the P. falciparum cyclic amine resistance locus in the mode of resistance.
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
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, (2013/03/28)
The invention provides compounds of formula I: (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing com-pounds of formula I, intermediates useful for preparing com-pounds of formula I and therapeutic methods for suppressing an immune response or treating cancer, including a hematologic malignancy, using compounds of formula I
Novel steroid mimics: synthesis of tri- and tetra-substituted oxamides and oxoamides
Jones, Ian L.,Schofield, Daniel J.,Strevens, Robert R.,Horton, Peter N.,Hursthouse, Michael B.,Tomkinson, Nicholas C.O.
, p. 521 - 525 (2007/10/03)
A series of dicarbonyl compounds have been designed and prepared to mimic the rigid tetracyclic core of estradiol and dihydrotestosterone. Non-symmetrical tri- and tetra-substituted oxamides were prepared by the sequential addition of primary and secondary amines to phenyl cholorooxoacetate. Oxoamides were prepared via a Friedel-Crafts acylation/amide coupling protocol. Crystallographic data shows a good correlation between the structure of the dicarbonyl mimic and dihydrotestosterone complexed with the androgen receptor suggesting the molecular scaffolds may well prove versatile platforms for ligand design.
Divalent and trivalent α-ketocarboxylic acids as inhibitors of protein tyrosine phosphatases
Chen, Yen Ting,Seto, Christopher T.
, p. 3946 - 3952 (2007/10/03)
Protein tyrosine phosphatases (PTPases) are important targets for the treatment of insulin resistance in patients with type II diabetes and as antibacterial agents. As a result, there is a growing interest in the development of potent and specific inhibitors for these enzymes. This paper describes a series of inhibitors that contain two or three α-ketocarboxylic acid groups that are designed to form multiple contacts with residues inside or near the active site of phosphatases. The inhibitors have been assayed against three PTPases: the Yersinia PTPase, PTP1B, and LAR. The best of the inhibitors has IC50 values against the Yersinia PTPase and PTP1B of 0.7 and 2.7 μM, respectively. These divalent and trivalent compounds are significantly more potent than their corresponding monovalent analogues. In addition, they show good selectivity for PTP1B and the Yersinia PTPase as compared to LAR.
Polypeptide compound and a process for preparation thereof
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, (2008/06/13)
A polypeptide compound having antimicrobial activity of the following general formula: STR1 wherein R1 is hydrogen or acyl group, R2 is hydroxy or acyloxy, R3 is hydroxysulfonyloxy, and R4 is hydrogen or carbamoyl, with proviso that R1 is not palmitoyl, when R2 is hydroxy, R3 is hydroxysulfonyloxy and R4 is carbamoyl, and a pharmaceutically acceptable salt thereof.
Dihalogenation of β-ketosulfides. Synthesis of α-keto methyl esters and α-keto S-phenyl thioesters
Fortes,Souto,Okino
, p. 2045 - 2052 (2007/10/02)
α-Keto esters and α-keto S-phenyl thioesters are synthesized from β-keto sulfides by dihalogenation with sulfuryl chloride followed by solvolysis with methanol and acetone/water respectively.
Total syntheses of (-)-nocardicins A-G: A biogenetic approach
Salituro, Gino M.,Townsend, Craig A.
, p. 760 - 770 (2007/10/02)
The known nocardicins A-G have been synthesized, several for the first time, having geometric and stereoisomeric purities of a high order. The syntheses proceed through the central intermediacy of tert-butyl (-)-3-aminocardicinate (14), which has been pre
