Category: amides-buliding-blocks

Donetti, Arturo published the artcileMild and effective two-step conversion of disubstituted cyanamides to secondary amines, SDS of cas: 2451-91-4, the publication is Journal of Organic Chemistry (1972), 37(21), 3352-3, database is CAplus.

A convenient procedure was developed to convert disubstituted cyanamides into secondary amines under mild conditions. Disubstituted cyanamides, R2NCN were obtained from the halides and Na cyanamide in Me2SO. Equimolar amounts of R2NCN and KCN refluxed in MeOH, gave the intermediate o-methylisoureas, which were hydrolyzed to secondary amines with dilute HOAc.

Journal of Organic Chemistry published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, SDS of cas: 2451-91-4.

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

Vivier, Delphine published the artcileDevelopment of the First Two-Pore Domain Potassium Channel TWIK-Related K⁺ Channel 1-Selective Agonist Possessing in Vivo Antinociceptive Activity, Product Details of C5H8N2O, the publication is Journal of Medicinal Chemistry (2017), 60(3), 1076-1088, database is CAplus and MEDLINE.

The TWIK-Related K⁺ channel, TREK-1, has recently emerged as an attractive therapeutic target for the development of a novel class of analgesic drugs, suggesting that activation of TREK-1 could result in pain inhibition. Here the authors report the synthesis of a series of substituted acrylic acids (1-54) based on the previous work with caffeate esters. The analogs were evaluated for their ability to modulate TREK-1 channel by electrophysiol. and for their in vivo antinociceptive activity (acetic acid-induced writhing and hot-plate assays), leading to the identification of a series of novel mols. able to activate TREK-1 and displaying potent antinociceptive activity in vivo. The furyl analog I is the most promising of these series.

Journal of Medicinal Chemistry published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C13H24INO4, Product Details of C5H8N2O.

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

Colombo, Andrea published the artcileThe proposal of architecture for chemical splitting to optimize QSAR models for aquatic toxicity, Application of 2,4-Dichlorobenzamide, the publication is Chemosphere (2008), 72(5), 772-780, database is CAplus and MEDLINE.

One of the challenges in the field of quant. structure-activity relationship (QSAR) anal. is the correct classification of a chem. compound to an appropriate model for the prediction of activity. Thus, in previous studies, compounds have been divided into distinct groups according to their mode of action or chem. class. In the current study, theor. mol. descriptors were used to divide 568 organic substances into subsets with toxicity measured for the 96-h lethal median concentration for the Fathead minnow (Pimephales promelas). Simple constitutional descriptors such as the number of aliphatic and aromatic rings and a quantum chem. descriptor, maximum bond order of a carbon atom divide compounds into nine subsets. For each subset of compounds the automatic forward selection of descriptors was applied to construct QSAR models. Significant correlations were achieved for each subset of chems. and all models were validated with the leave-one-out internal validation procedure (R²_cv ≈ 0.80). The results encourage to consider this alternative way for the prediction of toxicity using QSAR subset models without direct reference to the mechanism of toxic action or the traditional chem. classification.

Chemosphere 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, Application of 2,4-Dichlorobenzamide.

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

Vettori, L. Pecori published the artcileSynthesis of 4,9-dimethoxy-5-methyl-7H-furo[3,2-g]-1-benzopyran-7-one-6-carboxylic acid derivatives, COA of Formula: C5H8N2O, the publication is Farmaco, Edizione Scientifica (1975), 30(9), 754-60, database is CAplus.

The title compounds I (X = O, R = CN, CO2Et, CO2H, COCl, H, CONH2, CONEt2, CONH(CH2)4OH, NHCH2CHMe2, NHCH2CH2NEt2, morpholino, 2-pyridylamino, OCH2CH2NMe2, OCHMeCH2NEt2, O(CH2)3NEt2, OCH2CH2NEt2; X = NH, R = CN) were prepared from Khellinone. Thus condensation of Khellinone with NCCH2CONHR1 (R1 = H, Me, Et), CH2(CO2Et)2, CH2(CONH2)2, and CH2(CN)2 gave I (X = O, R = CN, CO2Et, CONH2; X = NH, R = CN). Hydrolysis of the ester gave I (R = CO2H), which was chlorinated and aminated.

Farmaco, Edizione Scientifica published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C8H11NO, COA of Formula: C5H8N2O.

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

Pascual-Alfonso, Eva published the artcileEfficient synthesis of the pyrido[2,3,4-kl]acridin-4-one system common to several cytotoxic marine alkaloids, Application of (2-Pivalamidophenyl)boronic acid, the publication is Tetrahedron Letters (2003), 44(32), 6003-6005, database is CAplus.

An efficient, four-step synthesis of the pyrido[2,3,4-kl]acridin-4-one system is described, using a Suzuki coupling of a 4-iodoquinoline and a oxidative demethylation of a dimethoxyquinoline containing an anilino unit with cobalt trifluoride as the key steps.

Tetrahedron Letters published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Application of (2-Pivalamidophenyl)boronic acid.

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

Repova, Kristina published the artcileCardiovascular therapeutics: A new potential for anxiety treatment?, Related Products of amides-buliding-blocks, the publication is Medicinal Research Reviews (2022), 42(3), 1202-1245, database is CAplus and MEDLINE.

A review. Besides the well-recognized risk factors, novel conditions increasing cardiovascular morbidity and mortality are emerging. Undesirable emotions and behavior such as anxiety and depression, appear to participate in worsening cardiovascular pathologies. On the other hand, deteriorating conditions of the heart and vasculature result in disturbed mental and emotional health. The pathophysiol. background of this bidirectional interplay could reside in an inappropriate activation of vegetative neurohormonal and other humoral systems in both cardiovascular and psychol. disturbances. This results in circulus vitiosus potentiating mental and circulatory disorders. Thus, it appears to be of utmost importance to examine the alteration of emotions, cognition, and behavior in cardiovascular patients. In terms of this consideration, recognizing the potential of principal cardiovascular drugs to interact with the mental state in patients with heart or vasculature disturbances is unavoidable, to optimize their therapeutic benefit. In general, beta-blockers, central sympatholytics, ACE inhibitors, ARBs, aldosterone receptor blockers, sacubitril/valsartan, and fibrates are considered to exert anxiolytic effect in animal experiments and clin. settings. Statins and some beta-blockers appear to have an equivocal impact on mood and anxiety and ivabradine expressed neutral psychol. impact. It seems reasonable to suppose that the knowledge of a patient’s mood, cognition, and behavior, along with applying careful consideration of the choice of the particular cardiovascular drug and respecting its potential psychol. benefit or harm might improve the individualized approach to the treatment of cardiovascular disorders.

Medicinal Research Reviews 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

Li, Jiafu published the artcileAre Disinfection Byproducts (DBPs) Formed in My Cup of Tea? Regulated, Priority, and Unknown DBPs, Name: 2-Chloroacetamide, the publication is Environmental Science & Technology (2021), 55(19), 12994-13004, database is CAplus and MEDLINE.

Globally, tea is the second most consumed nonalcoholic beverage next to drinking water and is an important pathway of disinfection byproduct (DBP) exposure. When boiled tap water is used to brew tea, residual chlorine can produce DBPs by the reaction of chlorine with tea compounds In this study, 60 regulated and priority DBPs were measured in Twinings green tea, Earl Gray tea, and Lipton tea that was brewed using tap water or simulated tap water (nanopure water with chlorine). In many cases, measured DBP levels in tea were lower than in the tap water itself due to volatilization and sorption onto tea leaves. DBPs formed by the reaction of residual chlorine with tea precursors contributed ~12% of total DBPs in real tap water brewed tea, with the remaining 88% introduced by the tap water itself. Of that 12%, dichloroacetic acid, trichloroacetic acid, and chloroform were the only contributing DBPs. Total organic halogen in tea nearly doubled relative to tap water, with 96% of the halogenated DBPs unknown. Much of this unknown total organic halogen (TOX) may be high-mol.-weight haloarom. compounds, formed by the reaction of chlorine with polyphenols present in tea leaves. The identification of 15 haloarom. DBPs using gas chromatog.-high-resolution mass spectrometry indicates that this may be the case. Further studies on the identity and formation of these aromatic DBPs should be conducted since haloarom. DBPs can have significant toxicity.

Environmental Science & Technology 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, Name: 2-Chloroacetamide.

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

Hammerman, Ariel published the artcileDapagliflozin Versus Sacubitril-Valsartan to Improve Outcomes of Patients with Reduced Ejection Fraction and Diabetes Mellitus, Quality Control of 137862-53-4, the publication is American Journal of Cardiovascular Drugs (2022), 22(3), 325-331, database is CAplus and MEDLINE.

Abstract: Background: Comorbid heart failure with reduced ejection fraction (HFrEF) and type 2 diabetes mellitus (DM) is associated with a very high risk of HF events. Sacubitril-valsartan, an angiotensin receptor-neprilysin inhibitor (ARNI), and dapagliflozin, a sodium-glucose cotransporter-2 inhibitor, improve HF outcomes in these patients, but their comparative value for money in this patient population has not yet been determined Objective: We aimed to compare the cost needed to treat (CNT) to avoid an HF event with each drug. Methods: CNT was estimated by multiplying the annualized number needed to treat (NNT) to prevent one HF event by the annual cost of each therapy. HF events were defined as the first event of hospitalization for HF or cardiovascular mortality. Drug efficacy data were extracted from published secondary analyses of patients with DM in the DAPA-HF and PARADIGM-HF trials. Drug costs were estimated as 75‰ of the 2021 US National Average Drug Acquisition Cost listing. Sensitivity anal. was performed on parameters that may have affected the CNT. Results: The annualized NNT was 24 (95‰ confidence interval [CI] 16-54) for dapagliflozin and 57 (95‰ CI 31-433) for the ARNI. At an annual cost of $US4523 and 5099, resp., the CNT was $US108,563 (95‰ CI 72,375-244,267) for dapagliflozin and $US290,671 (95‰ CI 158,084-2,208,079) for the ARNI. Conclusions: Dapagliflozin seems to offer greater value for money than the ARNI for patients with HFrEF and DM. Our results provide support for contemporary guidelines advocating the use of dapagliflozin in these patients.

American Journal of Cardiovascular Drugs 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, Quality Control of 137862-53-4.

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

Zingg, Jean-Marc published the artcileα-Tocopheryl Phosphate Induces VEGF Expression via CD36/PI3Kγ in THP-1 Monocytes, SDS of cas: 321673-30-7, the publication is Journal of Cellular Biochemistry (2017), 118(7), 1855-1867, database is CAplus and MEDLINE.

The CD36 scavenger receptor binds several ligands and mediates ligand uptake and ligand-dependent signal transduction and gene expression, events that may involve CD36 internalization. Here we show that CD36 internalization in THP-1 monocytes is triggered by α-tocopherol (αT) and more strongly by α-tocopheryl phosphate (αTP) and EPC-K1, a phosphate diester of αTP and L-ascorbic acid. αTP-triggered CD36 internalization is prevented by the specific covalent inhibitor of selective lipid transport by CD36, sulfo-N-succinimidyl oleate (SSO). Moreover, SSO inhibited the CD36-mediated uptake of 14C-labeled αTP suggesting that αTP binding and internalization of CD36 is involved in cellular αTP uptake, whereas the uptake of αT was less affected. Similar to that, inhibition of selective lipid transport of the SR-BI scavenger receptor resulted mainly in reduction of αTP and not αT uptake. In contrast, uptake of αT was mainly inhibited by Dynasore, an inhibitor of clathrin-mediated endocytosis, suggesting that the differential regulatory effects of αTP and αT on signaling may be influenced by their different routes of uptake. Interestingly, αTP and EPC-K1 also reduced the neutral lipid content of THP-1 cells and the phagocytosis of fluorescent Staphylococcus aureus bioparticles. Moreover, induction of the vascular endothelial growth factor (VEGF) promoter activity by αTP occurred via CD36/PI3Kγ/Akt, as it could be inhibited by specific inhibitors of this pathway (SSO, Wortmannin, AS-605240). These results suggest that αTP activates PI3Kγ/Akt signaling leading to VEGF expression in monocytes after binding to and/or transport by CD36, a receptor known to modulate angiogenesis in response to amyloid beta, oxLDL, and thrombospondin. J. Cell. Biochem. 9999: 1-13, 2017. © 2017 Wiley Periodicals, Inc.

Journal of Cellular Biochemistry 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 C5H9IO2, SDS of cas: 321673-30-7.

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

Nosaka, Takuto published the artcileAlveolar Macrophages Drive Hepatocellular Carcinoma Lung Metastasis by Generating Leukotriene B₄, Category: amides-buliding-blocks, the publication is Journal of Immunology (2018), 200(5), 1839-1852, database is CAplus and MEDLINE.

Macrophages in lungs can be classified into two subpopulations, alveolar macrophages (AMs) and interstitial macrophages (IMs), which reside in the alveolar and interstitial spaces, resp. An i.v. injection of a mouse hepatocellular carcinoma (HCC) cell line, BNL, caused lung metastasis foci with infiltration of AMs and IMs. A 5-lipoxygenase (LOX) inhibitor but not a cyclooxygenase inhibitor reduced the numbers of metastatic foci, particularly those of a larger size. A major 5-LOX metabolite, LTB₄, augmented in vitro cell proliferation of human HCC cell lines as well as BNL cells. Moreover, in this lung metastasis course, AMs exhibited higher expression levels of the 5-LOX and LTB₄ than IMs. Consistently, 5-LOX-expressing AMs increased in the lungs of human HCC patients with lung metastasis, compared with those without lung metastasis. Furthermore, intratracheal clodronate liposome injection selectively depleted AMs but not IMs, together with reduced LTB₄ content and metastatic foci numbers in this lung metastasis process. Finally, IMs in mouse metastatic foci produced CCL2, thereby recruiting blood-borne, CCR2-expressing AMs into lungs. Thus, AMs can be recruited under the guidance of IM-derived CCL2 into metastatic lungs and can eventually contribute to the progression of lung metastasis by providing a potent arachidonic acid-derived tumor growth promoting mediator, LTB₄.

Journal of Immunology 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, Category: amides-buliding-blocks.

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