Month: December 2022

Boyd, G. S. published the artcileThe interrelations and effects of iodothyronines and cholesterol on the myocardium of the rat, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, the publication is Journal of Atherosclerosis Research (1961), 470-88, database is CAplus and MEDLINE.

3,3′,5-Triiodo-L-thyronine (T₃) was administered to adult male rats at 50 γ/day. Serum cholesterol, O consumption, heart rate, and histology of the heart were studied in these animals. The hyperthyroid state in the rat was accompanied by an increase in O consumption, heart rate, and cardiac hypertrophy. Many of the hearts from hyperthyroid rats exhibited degenerative lesions of the cardiac muscle characterized by focal necrosis and fibrosis. The effect of varying the diet on the metabolic and histol. responses was studied. The inclusion of cholesterol and olive oil in the diet appeared to protect the animal against T₃-induced myocardial lesions. The time-course of these lesions with respect to the cardiac hypertrophy suggests that the effects may be causally related. The lesions can be produced by a wide variety of iodothyronines related to T₃, provided the dosage of the analog is adjusted to produce an approx. equivalent cardiac hypertrophy.

Journal of Atherosclerosis Research published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride.

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

D’Onofrio, Jennifer published the artcileAn Efficient and Versatile Solid-Phase Synthesis of 5′- and 3′-Conjugated Oligonucleotides, Application of 3-Chloro-4-hydroxyphenylacetic acid, the publication is Organic Letters (2005), 7(22), 4927-4930, database is CAplus and MEDLINE.

An easy and efficient solid-phase strategy to obtain 5′- and 3′-oligonucleotide conjugates in highly pure form has been developed. Ad hoc derivatized solid supports, to which the first nucleoside unit can be attached through a phosphate linkage, have been exploited both in a pre- and post-DNA assembly conjugation approach. A number of 5′- or 3′- oligonucleotide conjugates, incorporating a variety of labels covalently linked through a phosphodiester or a phosphoramidate bond, have been synthesized and characterized.

Organic Letters published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Application of 3-Chloro-4-hydroxyphenylacetic acid.

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

Lourenco, Nuno M. T. published the artcileIonic Acylating Agents for the Enzymatic Resolution of sec-Alcohols in Ionic Liquids, Related Products of chlorides-buliding-blocks, the publication is European Journal of Organic Chemistry (2010), 6938-6943, S6938/1-S6938/52, database is CAplus.

Potential acylating agents containing pendant ionic groups have been screened for the enzymic kinetic resolution of rac-secondary alcs. in ionic liquids with CAL-B as biocatalyst. This study has allowed the identification of the 1-methyl-3-alkylimidazolium cation attached to a carboxylate group through a C₁₀-alkyl chain as an efficient acylating agent for this transformation. This strategy was applied to the resolution of 2-hydroxycyclohexanecarbonitrile in which the 1R,2S enantiomer was isolated in 35 % ee (73 % yield) and the 1S,2R enantiomer in 97 % ee (23 % yield).

European Journal of Organic Chemistry published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, Related Products of chlorides-buliding-blocks.

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

Antczak, Monika I. published the artcileMild Synthesis of Organophosphorus Compounds: Reaction of Phosphorus-Containing Carbenoids with Organoboranes, Application of Diethyltrichloromethylphosphonate, the publication is Organic Letters (2008), 10(5), 977-980, database is CAplus and MEDLINE.

Organoboranes react with phosphorus-containing carbenoids to produce a variety of functionalized organophosphorus compounds under mild conditions. In some cases, selective migration of one group attached to boron can be observed Thus, reaction of (MeO)₂P(O)(CH₂N₂) with Bu₃B in THF/Et₂O at room temperature for 1h followed by hydrolysis (H₂O 2h reflux) gave 86% (MeO)₂P(O)CH₂Bu. Phosphonite-borane complexes are introduced as novel synthons for the synthesis of phosphinic esters.

Organic Letters published new progress about 866-23-9. 866-23-9 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Diethyltrichloromethylphosphonate, and the molecular formula is C5H10Cl3O3P, Application of Diethyltrichloromethylphosphonate.

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

Podtelezhnikov, Alexei A. published the artcileQuantitative transcriptional biomarkers of xenobiotic receptor activation in rat liver for the early assessment of drug safety liabilities, HPLC of Formula: 637-07-0, the publication is Toxicological Sciences (2020), 175(1), 98-112, database is CAplus and MEDLINE.

The robust transcriptional plasticity of liver mediated through xenobiotic receptors underlies its ability to respond rapidly and effectively to diverse chem. stressors. Thus, drug-induced gene expression changes in liver serve not only as biomarkers of liver injury, but also as mechanistic sentinels of adaptation in metabolism, detoxification, and tissue protection from chems. Modern RNA sequencing methods offer an unmatched opportunity to quant. monitor these processes in parallel and to contextualize the spectrum of dose-dependent stress, adaptation, protection, and injury responses induced in liver by drug treatments. Using this approach, we profiled the transcriptional changes in rat liver following daily oral administration of 120 different compounds, many of which are known to be associated with clin. risk for drug-induced liver injury by diverse mechanisms. Clustering, correlation, and linear modeling analyses were used to identify and optimize coexpressed gene signatures modulated by drug treatment. Here, we specifically focused on prioritizing 9 key signatures for their pragmatic utility for routine monitoring in initial rat tolerability studies just prior to entering drug development. These signatures are associated with 5 canonical xenobiotic nuclear receptors (AHR, CAR, PXR, PPARα, ER), 3 mediators of reactive metabolite-mediated stress responses (NRF2, NRF1, P53), and 1 liver response following activation of the innate immune response. Comparing paradigm chem. inducers of each receptor to the other compounds surveyed enabled us to identify sets of optimized gene expression panels and associated scoring algorithms proposed as quant. mechanistic biomarkers with high sensitivity, specificity, and quant. accuracy. These findings were further qualified using public datasets, Open TG-GATEs and DrugMatrix, and internal development compounds With broader collaboration and addnl. qualification, the quant. toxicogenomic framework described here could inform candidate selection prior to committing to drug development, as well as complement and provide a deeper understanding of the conventional toxicol. study endpoints used later in drug development.

Toxicological Sciences published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, HPLC of Formula: 637-07-0.

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

Farizyan, Mirxan published the artcilePalladium-Catalyzed Nondirected Late-Stage C-H Deuteration of Arenes, Recommanded Product: Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, the publication is Journal of the American Chemical Society (2021), 143(40), 16370-16376, database is CAplus and MEDLINE.

Herein, palladium catalyzed nondirected late-stage deuteration of arenes is discussed. Key aspects include the use of D₂O as a convenient and easily available deuterium source and the discovery of highly active N,N-bidentate ligands containing an N-acyl sulfonamide group. The reported protocol enables high degrees of deuterium incorporation via a reversible C-H activation step and features an extraordinary functional group tolerance, allowing for the deuteration of complex substrates. This is exemplified by the late-stage isotopic labeling of various pharmaceutically relevant motifs and related scaffolds. This method, among other applications, will prove useful as a tool in drug development processes and for mechanistic studies.

Journal of the American Chemical Society published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Recommanded Product: Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate.

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

Joyeau, Roger published the artcileN-Aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of β-lactamases, HPLC of Formula: 18791-02-1, the publication is Journal of Medicinal Chemistry (1988), 31(2), 370-4, database is CAplus and MEDLINE.

N-Aryl-3-haloazetidinones I (R = F, R¹ = H, F, Br; R = Br, R¹ = H, Br) were prepared by amidating BrCH₂CRR¹COCl, ring closure of BrCH₂CRR¹CONHC₆H₃(Me)CO₂CMe₃-2,5, and ester hydrolysis. Their affinities for the TEM-1 β-lactamase were determined and compared with those of the benzocarbacephems II (R² = H, Cl, F), and known β-lactamase inhibitors. I and II behave as competitive inhibitors and not as substrates of the enzyme; neither halogen substitution nor ring strain induces enzymic hydrolysis.

Journal of Medicinal Chemistry published new progress about 18791-02-1. 18791-02-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 2,3-Dibromopropionylchloride, and the molecular formula is C3H3Br2ClO, HPLC of Formula: 18791-02-1.

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

Park, Jung Gyu published the artcileConnectivity mapping of angiotensin-PPAR interactions involved in the amelioration of non-alcoholic steatohepatitis by Telmisartan, Application In Synthesis of 637-07-0, the publication is Scientific Reports (2019), 9(1), 1-11, database is CAplus and MEDLINE.

Nonalcoholic fatty liver disease (NAFLD) is a global health problem that is associated with various metabolic disorders. Telmisartan is a potential treatment for NAFLD due to its ability to improve insulin sensitivity and decrease hepatic fat accumulation via modulation of PPARγ, and to suppress hepatic fibrosis by blocking angiotensin II receptors. However, the underlying mechanisms of action of telmisartan have yet to be fully elucidated. In the present study, diabetic nonalcoholic steatohepatitis (NASH) mice (STAM mice) received daily administrations of telmisartan for 6 wk to assess the improvements in NASH. Hepatic transcriptome analyses revealed that the amelioration of NASH likely occurred through the regulation of inflammatory- and fibrosis-related gene responses. An integrated network anal. including transcriptional and non-transcriptional genes regulated by telmisartan showed that the NAFLD pathway is interconnected with the dysregulated RAS-PPAR-NFκB pathways. The downstream targets of PPARα, PPARδ, and RELA in this network significantly overlapped with telmisartan-induced differentially expressed genes (DEGs), which were verified in palmitate-treated Hepa1c1c7 cell line. This transcriptome approach accompanied with cell-based mol. analyses provided the opportunity to understand the fundamental mol. mechanisms underpinning the therapeutic effects of telmisartan, and will contribute to the establishment of a novel pharmacol. treatment for NASH patients.

Scientific Reports published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Application In Synthesis of 637-07-0.

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

Ahdenov, Reza published the artcileEelectrosynthesis of benzothiazole derivatives via C-H thiolation, Synthetic Route of 3696-23-9, the publication is Heterocyclic Communications (2022), 28(1), 67-74, database is CAplus.

Benzothiazole derivatives are essential intermediates in synthesizing a wide variety of medical and pharmaceutical compounds, and there is a great demand for a simple and efficient method to synthesize benzothiazoles under mild reaction conditions. Organic electrosynthesis as an energy-efficient process represents an environmentally benign and safer method than traditional methods for organic synthesis. Herein, authors present bromine-free and straightforward synthesis of 2-amino benzothiazole derivatives via the reaction of aniline derivatives and ammonium thiocyanate using electrosynthesis in the presence of sodium bromide both as an electrolyte and as a brominating agent at room temperature in iso-Pr alc. (i-PrOH) as a solvent. The reaction of ammonium thiocyanate via C-H thiolation routes, using various aniline derivatives, resulted in a simple, green, and bromine-free synthesis of 2-amino benzothiazole in moderate to good yields under mild reaction conditions. Riluzole drug can be produced using the same procedure in moderate yields.

Heterocyclic Communications published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Synthetic Route of 3696-23-9.

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

Khayyat, Ahdab N. published the artcileDesign, Synthesis, and Antipoliferative Activities of Novel Substituted Imidazole-Thione Linked Benzotriazole Derivatives, Application In Synthesis of 3696-23-9, the publication is Molecules (2021), 26(19), 5983, database is CAplus and MEDLINE.

A new series of benzotriazole moiety bearing substituted imidazol-2-thiones I [R = H, 4-Me, 2-F, etc.] at N1 was designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogs exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, I [R = 2,4-di-Cl] showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC₅₀ 3.57, 0.40 and 2.63μM, resp. Compound I [R = 2,4-di-Cl] was taken up for elaborate biol. studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound I [R = 2,4-di-Cl] showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound I [R = 2,4-di-Cl] promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.

Molecules published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, Application In Synthesis of 3696-23-9.

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