Month: November 2022

Sanderson, John M. published the artcilePreparation of novel 3H-trifluoromethyldiazirine-based photoactivatable potassium channel antagonists, Name: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Tetrahedron (2005), 61(47), 11244-11252, database is CAplus.

The preparation of a series of photoactivatable precursors for use in photoaffinity labeling of potassium channels is described. 3H-Diazirine functionalities were incorporated into previously described potassium channel antagonists. The ability to perform enantioselective reductions and Wittig reactions in the presence of a diaziridine group was central to this work.

Tetrahedron published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Name: N,N-Diethyl-2,2,2-trifluoroacetamide.

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

Haffar, Amer published the artcileMeloxicam versus Celecoxib for Postoperative Analgesia after Total Knee Arthroplasty: Safety, Efficacy and Cost., Related Products of amides-buliding-blocks, the publication is Journal of the American Academy of Orthopaedic Surgeons. Global research & reviews (2022), 6(4), database is MEDLINE.

INTRODUCTION: Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used as part of multimodal analgesia in total knee arthroplasty (TKA). Selective cyclooxygenase (COX)-2 inhibitors (e.g., celecoxib) are believed to have fewer gastrointestinal (GI) adverse effects than nonselective NSAIDS. Meloxicam is less selective for COX-2 than celecoxib is and partially inhibits COX-1 at higher doses. Nonetheless, some surgeons prefer using nonselective NSAIDs because of their lower expense. METHODS: Four thousand nine hundred ninety-four patients who underwent TKA between January 2015 and February 2020 and took either celecoxib (n = 3,174), meloxicam 15 mg/d (n = 1,819), or meloxicam 7.5 mg/d (n = 451) were studied. Mutlimodal postoperative analgesia protocols were otherwise similar. GI bleeding and wound complication incidence were determined, as well as average 30-day prescription costs. RESULTS: GI bleeding incidence was similar in the three cohorts (P = 0.4). The incidence of wound complications did not significantly differ between the groups: 0.06%, 0.07%, and 0.22% in the celecoxib, meloxicam 15 mg/d, and meloxicam 7.5 mg/d groups, respectively (P = 0.06). Subsituting meloxicam for celecoxib results in an average savings of $183 per prescription. DISCUSSION: Meloxicam used at higher doses (15 mg/d) does not markedly increase the risk of GI or wound complications associated with COX-1 inhibition and is less costly for multimodal analgesia after TKA.

Journal of the American Academy of Orthopaedic Surgeons. Global research & reviews 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, Related Products of amides-buliding-blocks.

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

Tomlinson, Matthew L. published the artcileXenopus as a model organism in developmental chemical genetic screens, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Molecular BioSystems (2005), 1(3), 223-228, database is CAplus and MEDLINE.

Chem. genetics is a potentially powerful tool for studying developmental processes in vertebrate systems. The authors present data showing X. laevis as a model organism in which systematic chem. genetic screens can be carried out. Previous forward chem. genetic screens, including those with developing zebrafish embryos, have demonstrated the nature and value of biol. information gained with this approach. The authors show how amenable Xenopus is to chem. genetics by investigating a series of compounds either with known biochem. effects, or previously identified to give developmental phenotypes, on a range of biol. functions, including the development of pigmentation, the heart, and the central nervous system in zebrafish. The authors have found that the compounds give comparable phenotypes when applied to developing Xenopus embryos. The authors have also studied the penetrance and expressivity of these chem. genetic phenotypes in relation to genetic variation and the developmental window during which the compound is present. Finally, the authors assess the feasibility and the potential throughput of a screen in this vertebrate species.

Molecular BioSystems 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 C5H10Cl3O3P, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Vincent, Christelle published the artcile5-LOX, 12-LOX and 15-LOX in immature forms of human leukemic blasts, Application In Synthesis of 321673-30-7, the publication is Leukemia Research (2008), 32(11), 1756-1762, database is CAplus and MEDLINE.

Several reports have demonstrated an important role of leukotriene B₄ (LTB₄) in the immune system. We investigated whether leukemic blasts from acute myeloid leukemic (AML) and acute lymphoid leukemic (ALL) patients produced LTB₄, 12- and 15-hydroxyeicosatetraenoic acids (12-HETE and 15-HETE) and whether these compounds affected blast proliferation and apoptosis. Leukemic blasts from AML M_0-2 and ALL patients expressed 5-LOX, 12-LOX and 15-LOX transcripts. Quant. polymerase chain reaction indicated that 5-LOX transcripts were far more abundant than 12-LOX and 15-LOX ones. Leukemic blasts expressed 5-LOX activating protein (FLAP) transcripts and produced LTB₄ in response to calcium ionophore. In contrast no 15-HETE production was found. Calcium ionophore-stimulated leukemic blasts produced 12-HETE but also released thromboxane A₂ suggesting that contaminating platelets accounted for the release of these compounds No significant effect of LTB₄, 12-HETE or 15-HETE could be documented on leukemic blast growth and on their apoptose rate. Results of the present study indicate that immature form of leukemic blasts produce LTB₄. However, the three major lipoxygenase metabolites of arachidonic acid; i.e., LTB₄, 12-HETE or 15-HETE, had no evident effect on their growth and apoptosis. We may speculate that LTB₄-derived blast cells might initiate, augment or prolong tissue inflammation and damages by affecting the marrow and blood cytokine network.

Leukemia Research 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 C14H20BNO4, Application In Synthesis of 321673-30-7.

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

Wu, Patrick published the artcileIntegrating gene expression and clinical data to identify drug repurposing candidates for hyperlipidemia and hypertension, Application In Synthesis of 169590-42-5, the publication is Nature Communications (2022), 13(1), 46, database is CAplus and MEDLINE.

Discovering novel uses for existing drugs, through drug repurposing, can reduce the time, costs, and risk of failure associated with new drug development. However, prioritizing drug repurposing candidates for downstream studies remains challenging. Here, we present a high-throughput approach to identify and validate drug repurposing candidates. This approach integrates human gene expression, drug perturbation, and clin. data from publicly available resources. We apply this approach to find drug repurposing candidates for two diseases, hyperlipidemia and hypertension. We screen >21,000 compounds and replicate ten approved drugs. We also identify 25 (seven for hyperlipidemia, eighteen for hypertension) drugs approved for other indications with therapeutic effects on clin. relevant biomarkers. For five of these drugs, the therapeutic effects are replicated in the All of Us Research Program database. We anticipate our approach will enable researchers to integrate multiple publicly available datasets to identify high priority drug repurposing opportunities for human diseases.

Nature Communications 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 C4HN5, Application In Synthesis of 169590-42-5.

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

Chu, Te-Wei published the artcileHybrid polymeric hydrogels via peptide nucleic acid (PNA)/DNA complexation, Synthetic Route of 186046-83-3, the publication is Journal of Controlled Release (2015), 220(Part_B), 608-616, database is CAplus and MEDLINE.

This work presents a new concept in hybrid hydrogel design. Synthetic water-soluble N-(2-hydroxypropyl)methacrylamide (HPMA) polymers grafted with multiple peptide nucleic acids (PNAs) are crosslinked upon addition of the linker DNA. The self-assembly is mediated by the PNA-DNA complexation, which results in the formation of hydrophilic polymer networks. We show that the hydrogels can be produced through two different types of complexations. Type I hydrogel is formed via the PNA/DNA double-helix hybridization. Type II hydrogel utilizes a unique “P-form” oligonucleotide triple-helix that comprises two PNA sequences and one DNA. Microrheol. studies confirm the resp. gelation processes and disclose a higher critical gelation concentration for the type I gel when compared to the type II design. SEM reveals the interconnected microporous structure of both types of hydrogels. Type I double-helix hydrogel exhibits larger pore sizes than type II triple-helix gel. The latter apparently contains denser structure and displays greater elasticity as well. The designed hybrid hydrogels have potential as novel biomaterials for pharmaceutical and biomedical applications.

Journal of Controlled Release published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Synthetic Route of 186046-83-3.

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

Markovskii, L. N. published the artcileIminothionyl chlorides. X. Synthesis from iminoester. Infrared spectra, Computed Properties of 2447-79-2, the publication is Zhurnal Organicheskoi Khimii (1974), 10(5), 992-7, database is CAplus.

RN:SCl2 [R = Cl3CCO (I), Bz (II), p-ClC6H4CO (III), p-BrC6H4CO (IV), 2,4-Cl2C6H3CO (V), p-O2NC6H4CO (VI), MeSO2 (VII), PhSO2 (VIII)] were prepared by different methods. II, V, VI, VII, and VIII were prepared (60-89%) by reaction of RNH2 with SCl2. I, II, III, IV, V and VI were prepared (57-90%) by reaction of the corresponding alkyl arenecarboximidate with SCl2. II and VI were prepared (59-95%) by reaction of SCl2 with PhC(:NCl)OR (R = alkyl) and p-O2NC6-H4C(:NCl)OR, resp. Reaction of p-O2NC6H4C(OEt):NSN:-C(OEt)C6H4NO2-p with SCl2 gave 62% VI. The ir spectra depended on R.

Zhurnal Organicheskoi Khimii published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Computed Properties of 2447-79-2.

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

Bolla, Giovanni Battista published the artcileEffects of Sacubitril/Valsartan on biomarkers of fibrosis and inflammation in patients with heart failure with reduced ejection fraction, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is BMC Cardiovascular Disorders (2022), 22(1), 217, database is CAplus and MEDLINE.

Abstract: Aims: To evaluate the circulating levels of remodeling biomarkers procollagen type 1 C-terminal propeptide (PICP), human cartilage glycoprotein-39 (YKL-40), plasma renin activity (PRA), aldosterone (Aldo) as well as clin. and echocardiog. parameters in patients with heart failure with reduced ejection fraction (HFrEF), before and after treatment with Sacubitril/Valsartan (S/V). Methods and results: A total of 26 consecutive patients with HFrEF on stable clin. conditions were studied. Clin., echocardiog. parameters and circulating biomarkers were measured at baseline, after 30 and 60 days of S/V treatment. Both systolic blood pressure (SBP) and diastolic blood pressure (DBP) decreased, from 126 ± 15 to 113 ± 4 mmHg (p < 0.001) and from 77 ± 11 to 72 ± 9 mmHg (p = 0.005), resp., at the end of study. Concomitantly, left ventricular ejection fraction (LVEF) increased by 22.8% from 29.5 ± 5% to 36.2 ± 5%, (p < 0.001) and indexed left ventricular end-systolic volume (LVESVi) decreased by 12% from 38.6 ± 8.7 mL/m² to 34.0 ± 10.0 mL/m². (p = 0.007). Circulating levels of PICP, YKL-40, PRA and Aldo decreased by – 42.2%, – 46.8%, – 79.1% and – 76.7%, resp. (p < 0.001 for all), the decrements being already maximal within 30 days of S/V treatment. No significant changes of plasma electrolytes and creatinine were observed during the study (all p > 0.05). Conclusions: A decrease of circulating markers of inflammation and fibrosis during chronic treatment with S/V is associated with an improvement of hemodynamic and echog. parameters in patients with HRrEF. These data are compatible with an anti-fibrotic and anti-inflammatory effect of S/V, that may contribute to the beneficial outcomes of the drug in this clin. setting.

BMC Cardiovascular Disorders published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

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

Neta, Pedatsur published the artcileUnexpected peaks in tandem mass spectra due to reaction of product ions with residual water in mass spectrometer collision cells, Product Details of C10H14N2O, the publication is Rapid Communications in Mass Spectrometry (2014), 28(23), 2645-2660, database is CAplus and MEDLINE.

Certain product ions in electrospray ionization tandem mass spectrometry react with residual water in the collision cell. This reaction often gives ions that cannot be formed directly from the precursor ions, and this complicates the mass spectra and may distort MRM (multiple reaction monitoring) results. Various drugs, pesticides, metabolites, and other compounds were dissolved in acetonitrile/water/formic acid and studied by electrospray ionization mass spectrometry to record their MS² and MSⁿ spectra in several mass spectrometers (QqQ, QTOF, IT, and Orbitrap HCD). Certain product ions react with residual water in collision cells. The reaction was confirmed by MSⁿ studies and the rate of reaction was determined in the IT instrument using zero collision energy and variable activation times. Examples of product ions reacting with water include Ph and certain substituted Ph cations, benzoyl-type cations formed from protonated folic acid and similar compounds by loss of the glutamate moiety, product ions formed from protonated cyclic siloxanes by loss of methane, product ions formed from organic phosphates, and certain neg. ions. The reactions of product ions with residual water varied greatly in their rate constant and in the extent of reaction (due to isomerization). Thus, various types of product ions react with residual water in mass spectrometer collision cells. As a result, tandem mass spectra may contain unexplained peaks and MRM results may be distorted by the occurrence of such reactions. These often unavoidable reactions must be taken into account when annotating peaks in tandem mass spectra and when interpreting MRM results.

Rapid Communications in Mass Spectrometry published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, Product Details of C10H14N2O.

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

Cai, Zhaohua published the artcileAngiotensin II Promotes White Adipose Tissue Browning and Lipolysis in Mice., Related Products of amides-buliding-blocks, the publication is Oxidative medicine and cellular longevity (2022), 6022601, database is MEDLINE.

Emerging evidence has revealed that all components of the renin-angiotensin system (RAS) are present in adipose tissue. Angiotensin II (Ang II), the major bioactive component of the RAS, has been recognized as an adipokine involved in regulating energy homeostasis. However, the precise role of Ang II in white adipose tissue (WAT) remodeling remains to be elucidated. In this present study, C57BL/C male mice were continuously infused with different doses of Ang II (1.44 mg/kg/d or 2.5 mg/kg/d) or saline for 2 weeks and treated with or without the Ang II type 1 receptor blocker valsartan. H&E staining and immunohistochemistry were conducted to investigate the white-to-brown fat conversion. The level of serum total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C) was measured. RNA sequencing was employed to explore the differentially expressed genes and their enriched pathways between control and Ang II groups. Our results showed that Ang II substantially resulted in loss of body weight and fat mass. Most importantly, Ang II treatment induced WAT browning in mice, which was partially attenuated by valsartan treatment. Furthermore, Ang II perturbed the serum lipid profiles. Ang II treatment elevated serum levels of TC, TG, LDL-C, and HDL-C in mice. Mechanistically, thermogenesis, cell respiration, and lipid metabolism-associated mRNAs showed significantly increased expression profiling in Ang II-treated WATs compared with control WATs. Moreover, we found that Ang II treatment enhanced AMPK phosphorylation in adipocytes. Therefore, Ang II promotes WAT browning and lipolysis via activating the AMPK signaling pathway.

Oxidative medicine and cellular longevity published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Related Products of amides-buliding-blocks.

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