Author: tianli

Bharate, Sandip B.; Khan, Shabana I.; Tekwani, Babu L.; Jacob, Melissa; Khan, Ikhlas A.; Singh, Inder Pal published the artcile< S-Euglobals: Biomimetic synthesis, antileishmanial, antimalarial, and antimicrobial activities>, SDS of cas: 4396-13-8, the main research area is euglobal analog preparation antileishmanial antimalarial antimicrobial structure.

Several new euglobal analogs (named as S-euglobals) were synthesized from phloroglucinol using a biomimetic three-component reaction involving Knoevenagel condensation and Diels-Alder cycloaddition with a monoterpene. Newly synthesized euglobal analogs involve monoterpenes that have not yet been encountered in natural euglobals. S-Euglobals along with previously synthesized robustadial A and B were evaluated for in vitro antileishmanial, antimalarial, antimicrobial, and cytotoxic activities. Out of sixteen analogs prepared, nine analogs were found to exhibit antileishmanial activity against Leishmania donovani promastigotes. A 2-carene-derived S-euglobal was the most potent antileishmanial with IC50 of 2.4 μg/mL and IC90 of 8 μg/mL, followed by a second 2-carene-derived S-euglobal and a nopol-derived S-euglobal (IC50 5.5 and 9.5 μg/mL). Antileishmanial activity of robustadial A (5) and B (6) was moderate with IC50 of 20 and 16 μg/mL, resp. Robustadial A and B and a 2-carene-derived S-euglobal exhibited weak antimalarial activity against Plasmodium falciparum (IC50 of 2.7-4.76 μg/mL). Few of the euglobal analogs showed antibacterial activity against methicillin-resistant Staphylococcus aureus. Amongst these, a nopol-derived S-euglobal was the most potent with IC50 of 1.0 μg/mL and MIC of 5.0 μg/mL. Most of the compounds were not cytotoxic up to 25 μg/mL in a panel of cell lines consisting of both cancer (SK-MEL, KB, BT-549, and SK-OV-3) as well as non-cancer kidney (Vero and LLC-PK11) cells.

Bioorganic & Medicinal Chemistry published new progress about Antimalarials. 4396-13-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H6O5, SDS of cas: 4396-13-8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mikami, Satoshi; Kawasaki, Masanori; Ikeda, Shuhei; Negoro, Nobuyuki; Nakamura, Shinji; Nomura, Izumi; Ashizawa, Tomoko; Kokubo, Hironori; Hoffman, Isaac Dylan; Zou, Hua; Oki, Hideyuki; Uchiyama, Noriko; Hiura, Yuuto; Miyamoto, Maki; Itou, Yuuki; Nakashima, Masato; Iwashita, Hiroki; Taniguchi, Takahiko published the artcile< Discovery of a novel series of pyrazolo[1,5-a]pyrimidine-based phosphodiesterase 2A inhibitors structurally different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the treatment of cognitive disorders>, Electric Literature of 660867-80-1, the main research area is pyrazolopyrimidine preparation phosphodiesterase inhibitor SAR; intramolecular hydrogen bond; phospodiesterase 2A; phototoxicity; pyrazolo[1,5-a]pyrimidine; schizophrenia; structure-based drug design.

This article described a drug design strategy for a new series of lead compounds structurally distinct from the clin. candidate TAK-915, and subsequent medicinal chem. efforts to optimize potency, selectivity over other PDE families, and other preclin. properties including in-vitro phototoxicity and in-vivo rat plasma clearance. These efforts resulted in the discovery of N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, which robustly increased 3′,5′-cyclic guanosine monophosphate (cGMP) levels in the rat brain following an oral dose, and moreover, attenuated MK-801-induced episodic memory deficits in a passive avoidance task in rats. These data provide further support to the potential therapeutic utility of PDE2A inhibitors in enhancing cognitive performance.

Chemical & Pharmaceutical Bulletin published new progress about Bioavailability. 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Electric Literature of 660867-80-1.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Jung, Jong-Woon; Damodar, Kongara; Kim, Jin-Kyung; Jun, Jong-Gab published the artcile< First synthesis and in vitro biological assessment of isosideroxylin, 6,8-dimethylgenistein and their analogues as nitric oxide production inhibition agents>, Related Products of 4396-13-8, the main research area is isosideroxylin preparation nitric oxide inhibitory antiinflammatory activity; dimethylgenistein preparation nitric oxide inhibitory antiinflammatory activity; Vilsmeier Haack Friedel Crafts acylation Gammill protocol Suzuki.

A modular and efficient synthesis of the biol. significant C-methylisoflavones isosideroxylin (I), 6,8-dimethylgenistein (II) and their analogs is established for the first time. The synthesis is realized in 7-8 steps in overall yields of 16%-24% from com. inexpensive phloroglucinol and features a high yielding Vilsmeier-Haack reaction, Friedel-Crafts acylation, Gammill’s protocol and Suzuki coupling as the pivotal transformations. Next, these compounds evaluated for their inhibitory potency on the production of nitric oxide (NO) in lipopolysaccharide (LPS)-activated RAW-264.7 cells as an indicator of anti-inflammatory activity. The results showed that all the compounds decreased NO production in a dose-dependent manner without marked cytotoxicity and IC50 values are found in the range of 10.17-33.88 μmol/L. Of note, some compounds show comparable inhibitory activity with pos. control (N-monomethyl-L-arginine, L-NMMA).

Chinese Chemical Letters published new progress about Anti-inflammatory agents. 4396-13-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H6O5, Related Products of 4396-13-8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Megias-Sayago, Cristina; Reina, Tomas Ramirez; Ivanova, Svetlana; Odriozola, Jose A. published the artcile< Au/CeO2-ZnO/Al2O3 as versatile catalysts for oxidation reactions: application in gas/liquid environmental processes>, Application In Synthesis of 87-73-0, the main research area is gold cerium zinc aluminum oxide catalyst oxidation reaction; CO oxidation; CeO2-ZnO/Al2O3 catalysts; biomass upgrading; glucose oxidation; gold catalysts.

The present work showcases the versatility of nanogold systems supported on Zn-doped ceria when applied in two important environmental processes, the total CO oxidation, and the liquid phase oxidation of glucose to gluconic acid. In the CO oxidation the suitability of these materials is clearly demonstrated achieving full conversions even at sub-ambient conditions. Regarding the glucose oxidation our materials display high conversion values (always over 50%) and very importantly full or almost full selectivity toward gluconic acid-an added value platform chem. in the context of biomass upgrading routes. The key factors controlling the successful performance on both reactions are carefully discussed and compared to previous studies in literature. To our knowledge this is one of the very few works in catalysis by gold combining liquid and gas phase reactions and represents a step forward in the flexible behavior of nano gold catalysts.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Biomass. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, Application In Synthesis of 87-73-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Patel, Bhargavi J.; Patel, Chetna R. published the artcile< Assessment of causality, severity and preventability of adverse drug reactions of cancer chemotherapy in a tertiary care teaching hospital, Gujarat, India>, Recommanded Product: Calcium folinate, the main research area is adverse drug reaction causality cancer chemotherapy human.

To evaluate the various adverse drug reactions with different cancer chemotherapy regimens, severity, causality assessment and preventability. This cross-sectional, observational study was carried out in the oncol. department at a tertiary care teaching hospital over a period of one year. Data on Adverse Drug Reactions (ADRs) of anticancer drugs were collected of cancer patients diagnosed by a concerned clinician from the oncol. department. These ADRs were assessed for causality using Naranjo’s probability scale. The severity and preventability of the reported reactions were assessed using the modified Hartwig and Siegel scale and modified Schumock and Thornton scale, resp. Data were analyzed using Descriptive Statistics and Microsoft Excel. Out of 683 ADRs recorded from 198 patients, m/c ADRs were alopecia (21.08%), n/v (17.27%) & nail pigmentation (11.56%), etc. Taxanes, Platinum compounds, Nitrogen mustards, Antibiotics, and Antimetabolites were the most common group of drugs causing ADRs. On Causality Assessment showed highest ADRs were ‘possible’ (49.34%), ‘probable’ (47.58%) & few were ‘doubtful’ (3.07%). Severity Assessment showed a majority of the ADRs belonged to ‘mild’ grade (91.21%), then ‘moderate’ (8.05%) & ‘severe’ (0.73%). It was observed that most of the ADRs were ‘Not Preventable’ (57.83%), ‘Probably Preventable’ (24.3%) & lastly ‘Definitely Preventable’ (17.86%). The study shows that most of ADRs due to anticancer drugs belonged to ‘possible’ grade as per Causality assessment, ‘mild’ as per Severity Assessment, and ‘Not Preventable’ as per Preventability Assessment.

International Journal of Pharmaceutical Sciences and Research published new progress about Alopecia. 1492-18-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C20H21CaN7O7, Recommanded Product: Calcium folinate.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ubeda, Cristina; Kania-Zelada, Ingeborg; del Barrio-Galan, Ruben; Medel-Maraboli, Marcela; Gil, Mariona; Pena-Neira, Alvaro published the artcile< Study of the changes in volatile compounds, aroma and sensory attributes during the production process of sparkling wine by traditional method>, Application In Synthesis of 104-76-7, the main research area is sparkling wine aroma sensory property volatile compound; Aging; Impact aroma compounds; Olfactometry; País grape variety; Sensory analysis; Volatile compounds; sparkling wine.

One of the strongest factors that affects the volatile profile of sparkling wine is the winemaking process. Here we focus on determining the effects of the second fermentation and aging on lees of sparkling wine from Pais grape variety combining different anal. techniques for the first time in sparkling wine: gas chromatog./mass spectrometry/olfactometry and sensorial anal. During the second fermentation and aging, there was a significant loss of esters that might be related to the adsorption on lees and ester volatility and chem. hydrolysis. The concentration of several compounds such as some esters (di-Et succinate, Et lactate, and Et isovalerate) increased during aging and could be used as aging markers. Vitispiranes were identified as the best norisoprenoids aging markers for young sparkling wines (12 mo of aging). Also, PCA showed that time of aging on lees affected mostly esters and terpenes. On the other hand, the diminution of fruity/floral impact odorants during aging was not perceived in sensorial trials. Our results suggest that the responsibility for fruity/floral nuances in sparkling wine might reside in a few high-impact aromatic compounds, such as Et isobutyrate, isoamyl acetate, Et hexanoate, β-phenylethanol and di-Et succinate.

Food Research International published new progress about Acids Role: BSU (Biological Study, Unclassified), PUR (Purification or Recovery), BIOL (Biological Study), PREP (Preparation). 104-76-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H18O, Application In Synthesis of 104-76-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wu, Xu; Pan, Xiaoli; Cao, Sumei; Xu, Faqiong; Lan, Liming; Zhang, Yingyan; Lian, Senyang; Yan, Meijiao; Li, Ang published the artcile< iTRAQ-based quantitative proteomic analysis provides insights into strong broodiness in Muscovy duck (Cairina moschata) combined with metabolomics analysis>, Formula: C27H44O, the main research area is proteome metabolome APOV1 SAA VLDLR Cairina; Broodiness; Metabolomics; Muscovy duck; Ovary; Proteomics; iTRAQ.

Much attention has been paid to the broodiness of the Muscovy duck, but the mol. mechanism of broodiness remains largely unknown. In this study, the ovary tissues of Muscovy ducks during the broody and laying periods were used to investigate differentially expressed proteins (DEPs) by the iTRAQ-based proteomics approach. A total of 335 DEPs were identified, including 139 up-regulated and 196 down-regulated proteins. Six proteins (APOV1, GAL, SAA, GNB5, VLDLR and CDK1) with higher changes in expression were selected, and these proteins are mainly involved in the pathways related to reproductive performance, such as Oocyte meiosis, and PI3K-Akt signaling pathway. Steroid biosynthesis was the most significantly enriched pathway by KEGG pathway enriched anal. The qRT-PCR anal. was applied to verify the proteomic anal. Meanwhile, metabolomics anal. found that several important differentially expressed metabolites (DEMs) (7-dehydrodesmosterol, 25-Hydroxyvitamin D3, 7-Dehydrocholesterol, Pregnanolone, Allopregnanolone and estrogen) that were also mainly involved in Steroid biosynthesis, Steroid hormone biosynthesis and Metabolic pathways. Crucially, the changes in the abundance of these metabolites are closely related to the changes in the protein abundance of proteins identified in the same pathway, and it is always the upstream key enzymes that influence the production of downstream metabolites.

Journal of Proteomics published new progress about Cairina moschata Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Formula: C27H44O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts