Month: October 2022

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

Larsen, Finn Ole; Jensen, Benny V.; Norgaard, Hans Henrik; Hermann, Helle Kirstine; Larsen, Peter N.; Markussen, Alice; Hogdall, Estrid; Nielsen, Dorte published the artcile< Intrahepatic Oxaliplatin and Systemic 5-FU +/- Cetuximab in Chemo-Naive Patients with Liver Metastases from Colorectal Cancer>, COA of Formula: C20H21CaN7O7, the main research area is oxaliplatin fluorouracil cetuximab anticancer agent liver metastasis colorectal cancer; Colorectal cancer; Intrahepatic infusion; Oxaliplatin; Transarterial chemoembolization.

In case of response to chemotherapy, unresectable liver metastases from colorectal cancer can be converted to resectable and thereby obtain a chance of cure. The primary aim of this trial was to evaluate the response rate with intrahepatic oxaliplatin in combination with systemic 5-FU +/- cetuximab. Secondary aims were to evaluate the conversion rate from unresectable to resectable liver metastases, median progression-free survival, median overall survival, and toxicity. Forty-five chemo-naive patients with liver metastases from colorectal cancer were treated in a prospective phase II trial. Calcium folinate and 5-FU were delivered systemically while oxaliplatin was delivered alternating between systemic and intrahepatic administration. When oxaliplatin was delivered intrahepatic-ally, infusion time was reduced to 10 min followed by embolic material. In patients with KRAS wild-type tumors, cetuximab was added. The treatment was well tolerated and only pain in the liver and a mild increase in liver enzymes were observed after intrahepatic oxaliplatin. The patients obtained a response rate of 82%. Further, 58% converted from having unresectable to resectable liver metastases. The median overall survival and progression-free survival were 38.7 mo (95% confidence interval [CI] 33.0-44.3) and 12.9 mo (95% CI 10.2-15.6), resp. Intrahepatic infusion of oxaliplatin in 10 min with systemic 5-FU to patients with chemo-naive colorectal cancer is feasible and with low toxicity. A high response rate and long median overall survival were obtained.

Oncology published new progress about Animal gene, N-ras Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1492-18-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C20H21CaN7O7, COA of Formula: C20H21CaN7O7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts