Month: December 2022

Drsata, J. published the artcileSide effects of potential antituberculotics. Part 10. Parabolic model of the relation between electronic parameters and the hepatotoxicity of thiobenzaamides, COA of Formula: C8H9NOS, the publication is Pharmazie (1985), 40(11), 809-10, database is CAplus and MEDLINE.

Thirteen thiobenzamides (I; R = H, Br, Cl, OMe, Me, NO₂, or SMe) which do not undergo metabolic reduction were given to rats (0.73 mmol/kg, orally), and the hepatotoxicity (as measured by serum alanine aminotransferase) was plotted against the Hammett σ-constant There was a parabolic relation: with increasing Hammett values the liver toxicity initially decreased and then increased. All I had some hepatotoxicity.

Pharmazie published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, COA of Formula: C8H9NOS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Merlo, Thais Cardoso published the artcileRelationship between volatile organic compounds, free amino acids, and sensory profile of smoked bacon, Synthetic Route of 1453-82-3, the publication is Meat Science (2021), 108596, database is CAplus and MEDLINE.

Flavor is one of the most important characteristics of smoked bacon, strongly affecting its liking by consumers. The smoking process, lipid oxidation and proteolysis contribute to bacon quality through the generation of odors and flavor compounds In this study, the relationships between free amino acids (FAAs), volatile organic compounds (VOCs) and sensory characteristics of smoked bacon stored for 60 days at 5°C were investigated. Smoked bacon stored for 30 days was characterized by VOCs associated with the smoking process and lipid oxidation After 30 days of storage, the bacon samples presented an increase in FAAs produced mainly by proteolysis. Smoked bacon was characterized by the attributes smoky, crunchy, salty, soft and bright. This study demonstrated that VOCs, FAAs and their interactions are responsible for generating sensory attributes and increasing overall liking.

Meat Science published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Synthetic Route of 1453-82-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Serfling, Robert published the artcileDesigner tRNAs for efficient incorporation of non-canonical amino acids by the pyrrolysine system in mammalian cells, Formula: C11H22N2O4, the publication is Nucleic Acids Research (2018), 46(1), 1-10, database is CAplus and MEDLINE.

The pyrrolysyl-tRNA synthetase/tRNAPyl pair is the most versatile and widespread system for the incorporation of non-canonical amino acids (ncAAs) into proteins in mammalian cells. However, low yields of ncAA incorporation severely limit its applicability to relevant biol. targets. Here, we generate two tRNAPyl variants that significantly boost the performance of the pyrrolysine system. Compared to the original tRNAPyl, the engineered tRNAs feature a canonical hinge between D- and T-loop, show higher intracellular concentrations and bear partially distinct post-transcriptional modifications. Using the new tRNAs, we demonstrate efficient ncAA incorporation into a G-protein coupled receptor (GPCR) and simultaneous ncAA incorporation at two GPCR sites. Moreover, by incorporating last-generation ncAAs for bioorthogonal chem., we achieve GPCR labeling with small organic fluorophores on the live cell and visualize stimulus-induced GPCR internalization. Such a robust system for incorporation of single or multiple ncAAs will facilitate the application of a wide pool of chem. tools for structural and functional studies of challenging biol. targets in live mammalian cells.

Nucleic Acids Research published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C5H4N2O, Formula: C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Toffa, Joelle published the artcileRice pests in the Republic of Benin : farmers’ perceptions, knowledge and management practices, Quality Control of 79-07-2, the publication is Pest Management Science (2021), 77(11), 5058-5071, database is CAplus and MEDLINE.

Rice (Oryza spp) is one of the most consumed cereals in the Republic of Benin. However, rice production is threatened by various pests, which lead to important yield losses. For the development of integrated management strategies responding to the farmers’ realities, it is important to document their perceptions, knowledge and management of rice pests. Surveys involving 418 rice farmers to 21 ethnic groups through 39 villages were performed using rural appraisal tools. Farmers perceived birds, specifically weavers as the most important rice pests. The surveyed farmers also identified the variegated grasshopper, Zonocerus variegatus L. and rice brown leaf spots [Curvularia lunata (Wakker) Boedijn] as the main pests in the northern region, the pink stem borer, Sesamia calamistis Hampson and rice blast (Magnaporthe grisea (Hebert) Barr) in the southern region, and Z. variegatus and rice yellow mottle virus (genus Sobemovirus) in central Benin. The most important rice storage constraint was rodent attacks and the surveyed farmers proposed 13 key solutions to minimize constraints related to rice storage. Among various pest control methods recorded, farmers used mainly synthetic chem. pesticides. However, the Beninese National Pesticide Management Committee (CNGP) does not recommend most of pesticides used by farmers for rice protection (prohibited pesticides or intended for the protection of other crops). Farming experience, family size, region and number of observed pests have significantly influenced farmers’ decision to use pesticides. The rice pests perceived by farmers as important vary significantly across regions. These results suggest that integrated pest management programs which target rice pests accounting for these regional differences will be more effective. The identified variables that influence the use of pesticides must be taken in account in the development of strategies which will encourage farmers to use ecofriendly pest management.

Pest Management Science published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C8H6F3NO, Quality Control of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Prado, Morgana K. B. published the artcileLeukotriene B₄ is essential for lung host defence and alpha-defensin-1 production during Achromobacter xylosoxidans infection, Related Products of amides-buliding-blocks, the publication is Scientific Reports (2017), 7(1), 1-13, database is CAplus and MEDLINE.

Leukotriene B₄ (LTB₄) is essential for host immune defense. It increases neutrophil recruitment, phagocytosis and pathogen clearance, and decreases edema and inflammasome activation. The host response and the role of LTB₄ during Achromobacter xylosoxidans infection remain unexplored. Wild-type (129sv) and LTB₄ deficient (Alox5^-/-) mice were intratracheally infected with A. xylosoxidans. Wild-type 129sv infected mice survived beyond the 8th day post-infection, exhibited increased levels of LTB₄ in the lung on the 1st day, while levels of PGE₂ increased on the 7th day post-infection. Infected Alox5^-/- mice showed impaired bacterial clearance, increased lung inflammation, and succumbed to the infection by the 7th day. We found that exogenous LTB₄ does not affect the phagocytosis of A. xylosoxidans by alveolar macrophages in vitro. However, treatment of infected animals with LTB₄ protected from mortality, by reducing the bacterial load and inflammation via BLT₁ signalling, the high affinity receptor for LTB₄. Of importance, we uncovered that LTB₄ induces gene and protein expression of α-defensin-1 during the infection. This mol. is essential for bacterial clearance and exhibits potent antimicrobial activity by disrupting A. xylosoxidans cell wall. Taken together, our data demonstrate a major role for LTB₄ on the control of A. xylosoxidans infection.

Scientific Reports published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tsai, Yu-Ting published the artcileReprogramming of arachidonate metabolism confers temozolomide resistance to glioblastoma through enhancing mitochondrial activity in fatty acid oxidation, Product Details of C17H14F3N3O2S, the publication is Journal of Biomedical Science (London, United Kingdom) (2022), 29(1), 21, database is CAplus and MEDLINE.

Sp1 is involved in the recurrence of glioblastoma (GBM) due to the acquirement of resistance to temozolomide (TMZ). Particularly, the role of Sp1 in metabolic reprogramming for drug resistance remains unknown. RNA-Seq and mass spectrometry were used to analyze gene expression and metabolites amounts in paired GBM specimens (primary vs. recurrent) and in paired GBM cells (sensitive vs. resistant). ω-3/6 fatty acid and arachidonic acid (AA) metabolism in GBM patients were analyzed by targeted metabolome. Mitochondrial functions were determined by Seahorse XF Mito Stress Test, RNA-Seq, metabolome and substrate utilization for producing ATP. Therapeutic options targeting prostaglandin (PG) E2 in TMZ-resistant GBM were validated in vitro and in vivo. Among the metabolic pathways, Sp1 increased the prostaglandin-endoperoxide synthase 2 expression and PGE2 production in TMZ-resistant GBM. Mitochondrial genes and metabolites were obviously increased by PGE2, and these characteristics were required for developing resistance in GBM cells. For inducing TMZ resistance, PGE2 activated mitochondrial functions, including fatty acid β-oxidation (FAO) and tricarboxylic acid (TCA) cycle progression, through PGE2 receptors, E-type prostanoid (EP)1 and EP3. Addnl., EP1 antagonist ONO-8713 inhibited the survival of TMZ-resistant GBM synergistically with TMZ. Sp1-regulated PGE2 production activates FAO and TCA cycle in mitochondria, through EP1 and EP3 receptors, resulting in TMZ resistance in GBM. These results will provide us a new strategy to attenuate drug resistance or to re-sensitize recurred GBM.

Journal of Biomedical Science (London, United Kingdom) published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C13H10O3, Product Details of C17H14F3N3O2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Yang, Fangping published the artcileFacile Preparation of Polysaccharide-Polypeptide Conjugates via a Biphasic Solution Ring-Opening Polymerization, Category: amides-buliding-blocks, the publication is ACS Macro Letters (2022), 11(5), 663-668, database is CAplus and MEDLINE.

Polysaccharide-polypeptide conjugates have gained a broad interest in mimicking the structure and bioactivity of peptidoglycans or proteoglycans for biomedical applications. Efficient and precise preparation of the conjugates is challenging and unresolved, mainly because of the mismatched solubility between polysaccharide initiators and N-carboxyanhydrides (NCAs), which frequently results in competing side reactions and oligomeric polypeptide chain. Herein, we report a facile and efficient strategy to prepare the conjugates with well-controlled polypeptide chain length (l_p) directly from unmodified polysaccharides via a biphasic solution ring-opening polymerization The effect of l_p on surface antibacterial properties has been investigated. Elongating the l_p can significantly potentiate the antibiofilm property of the conjugate coatings. Our results may provide opportunities to develop various polypeptide-based conjugates with well-defined structures toward versatile uses.

ACS Macro Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C8H11NO, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Guo, Wei published the artcileImrecoxib versus celecoxib as postoperative analgesia for patients receiving arthroscopic knee surgery: a randomized, controlled, non-inferiority study, HPLC of Formula: 169590-42-5, the publication is Inflammopharmacology (2022), 30(3), 875-881, database is CAplus and MEDLINE.

Objective: Imrecoxib is a novel cyclooxygenase-2 inhibitor independently developed in China, which exhibits a good efficacy and tolerance in orthopedic disorders. The current study aimed to further compare its efficacy and safety with celecoxib as postoperative analgesia in arthroscopic knee surgery (AKS). Methods: Patients receiving AKS were enrolled and randomly assigned to imrecoxib (n = 64) and celecoxib (n = 62) group to receive analgesia for 72 h after surgery. Pain at rest and movement, pethidine consumption, patient′s satisfaction, Lysholm score, and adverse events were assessed after AKS. Meanwhile the upper limit of 95CI of pain-score mean difference (MD) between imrecoxib and celecoxib was calculated, then, the non-inferiority was defined if the all-time-point upper limits of 95CI less than 1. Results: Imrecoxib was non-inferior to celecoxib for alleviating pain at rest (upper limit of 95CI of MD ranging from 0.443 to 0.782, all time-point values less than 1); as well as for attenuating pain at movement (upper limit of 95CI of MD ranging from 0.398 to 0.582, all time-point values less than 1). Moreover, rescue analgesia rate (P = 0.583), pethidine consumption (P = 0.454), patient′s satisfaction at 72 h (P = 0.408), and Lysholm score at M3 (P = 0.776) were of no difference between imrecoxib group and celecoxib group. Addnl., the main adverse events in two groups were nausea (P = 0.425), constipation (P = 1.000), vomiting (P = 0.715), headache (P = 1.000), and dizziness (P = 0.667), which were mild and manageable. Conclusion: Imrecoxib is non-inferior to celecoxib in postoperative analgesia and exhibits an acceptable tolerance in patients undergoing AKS.

Inflammopharmacology published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Han, Lingxi published the artcileIndigenous functional microbial communities for the preferential degradation of chloroacetamide herbicide S-enantiomers in soil, Product Details of C2H4ClNO, the publication is Journal of Hazardous Materials (2022), 423(Part_B), 127135, database is CAplus and MEDLINE.

This study investigated indigenous functional microbial communities associated with the degradation of chloroacetamide herbicides acetochlor (ACE), S-metolachlor (S-MET) and their enantiomers in repeatedly treated soils. The results showed that biodegradation was the main process for the degradation of ACE, S-MET and their enantiomers. Eight dominant bacterial genera associated with the degradation were found: Amycolatopsis, Saccharomonospora, Mycoplasma, Myroides, Mycobacterium, Burkholderia, Afipia, and Kribbella. The S-enantiomers of ACE and S-MET were preferentially degraded, which mainly relied on Amycolatopsis, Saccharomonospora and Kribbella for the ACE S-enantiomer and Amycolatopsis and Saccharomonospora for the S-MET S-enantiomer. Importantly, the relative abundances of Amycolatopsis and Saccharomonospora increased by 146.3%-4467.2% in the S-enantiomer treatments of ACE and S-MET compared with the control, which were significantly higher than that in the corresponding R-enantiomer treatments (25.3%-4168.2%). Both metagenomic and qPCR analyses demonstrated that four genes, ppah, alkb, benA, and P 450, were the dominant biodegradation genes (BDGs) potentially involved in the preferential degradation of the S-enantiomers of ACE and S-MET. Furthermore, network anal. suggested that Amycolatopsis, Saccharomonospora, Mycoplasma, Myroides, and Mycobacterium were the potential hosts of these four BDGs. Our findings indicated that Amycolatopsis and Saccharomonospora might play pivotal roles in the preferential degradation of the S-enantiomers of ACE and S-MET.

Journal of Hazardous Materials published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Product Details of C2H4ClNO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Li, Wenjing published the artcileDiesel exhaust particle promotes tumor lung metastasis via the induction of BLT1-mediated neutrophilic lung inflammation, COA of Formula: C12H23N3S, the publication is Cytokine+ (2018), 530-540, database is CAplus and MEDLINE.

BLT1, the primary functional receptor of Leukotriene B4 (LTB4), is involved in tissue inflammation by mediating leukocyte recruitment, and recently LTB4-dependent inflammation was reported to promote lung tumor growth. In this study, we found that DEP exposure led to acute lung inflammation, characterized by abundant infiltration of neutrophils and elevated lung levels in LTB4, as well as several pro-inflammatory cytokines and chemokines, including IL-1β, IL-6, TNF-α, CXCL1/2. BLT1 blockade by its specific antagonist U75302 significantly inhibited neutrophilic lung inflammation following DEP exposure. Importantly, BLT1 blockade before the onset of inflammation significantly reduced DEP-enhanced lung metastasis, which was associated with greatly decreased infiltrating neutrophils in lungs. Interestingly, BLT1 blockade after the occurrence of lung metastases had no effect on the magnitude of lung metastasis, suggesting that inhibition of BLT1-mediated lung inflammation was insufficient to suppress established metastatic tumor. Administration of BLT2 inhibitor LY255283 fails to inhibit DEP-induced lung inflammation and tumor metastasis. Collectively, our results demonstrate that DEP exposure causes BLT1-mediated lung neutrophilic inflammation, which is critical for tumor lung metastasis, and suggest that interruption of the LTB4-BLT1 axis could be useful for preventing PM_2.5-induced inflammation and subsequent susceptible to lung metastasis.

Cytokine+ published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, COA of Formula: C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics