Category: chlorides-buliding-blocks

Wan, Zhao-Kui published the artcileEfficacious 11β-Hydroxysteroid Dehydrogenase Type I Inhibitors in the Diet-Induced Obesity Mouse Model, Name: 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, the publication is Journal of Medicinal Chemistry (2009), 52(17), 5449-5461, database is CAplus and MEDLINE.

Cortisol and the glucocorticoid receptor signaling pathway have been implicated in the development of diabetes and obesity. The reduction of cortisone to cortisol is catalyzed by 11β-hydroxysteroid dehydrogenase type I (11β-HSD1). 2,4-Disubsituted benzenesulfonamides were identified as potent inhibitors of both the human and mouse enzymes. The lead compounds displayed good pharmacokinetics and ex vivo inhibition of the target in mice. Cocrystal structures of compounds I and II bound to human 11β-HSD1 were obtained. Compound II was found to achieve high concentrations in target tissues, resulting in 95% inhibition in the ex vivo assay when dosed with a food mix (0.5 mg of drug per g of food) after 4 days. Compound II was efficacious in a mouse diet-induced obesity model and significantly reduced fed glucose and fasted insulin levels. Our findings suggest that 11β-HSD1 inhibition may be a valid target for the treatment of diabetes.

Journal of Medicinal Chemistry published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C7H11N, Name: 2-Chloro-4-cyanobenzene-1-sulfonyl chloride.

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

Froneman, M. published the artcileDialkylamino group transfer from titanium(IV) to a phosphoryl center. Structure-reactivity studies, Recommanded Product: Diethyltrichloromethylphosphonate, the publication is Phosphorus, Sulfur and Silicon and the Related Elements (1990), 47(3-4), 273-81, database is CAplus.

Reaction between phosphoryl substrates (EtO)₂P(O)R (R = H, Me, OEt) and Ti(NR₂)_nCl_4-n (R¹ = Me, Et, n = 2, 3, 4) and Mn(NEt₂)₂ leads to the exchange of one or both EtO groups for the NR₂ substituent. The reactivity of the system depends on electronic as well as steric effects of both substrates, and approx. correlates with Lewis acid-base interactions between the substrates.

Phosphorus, Sulfur and Silicon and the Related Elements 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, Recommanded Product: Diethyltrichloromethylphosphonate.

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

Chu, Haoke published the artcileAsymmetric Dearomatization of Indole by Palladium/PC-Phos-Catalyzed Dynamic Kinetic Transformation, Synthetic Route of 1451393-45-5, the publication is Angewandte Chemie, International Edition (2020), 59(49), 21991-21996, database is CAplus and MEDLINE.

A palladium-catalyzed intermol. dynamic kinetic asym. dearomatization of 3-arylindoles with internal alkynes was developed with the use of achiral Xantphos and chiral sulfinamide phosphine ligand (PC-Phos) as the co-ligands. This method could deliver various spiro[indene-1,3′-indole] compounds in good yields (up to 95% yield) with up to 98% ee. The salient features of the transformation include the use of readily available substrates, ease of scale-up and the versatile functionalization of the products. The mechanistic experiments gave some insights on active intermediates.

Angewandte Chemie, International Edition published new progress about 1451393-45-5. 1451393-45-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (2-Bromo-4-chlorophenyl)boronic acid, and the molecular formula is C6H5BBrClO2, Synthetic Route of 1451393-45-5.

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

Hsu, Li-Na published the artcileCentral action of drugs for treatment of hypertension. I. Effect of reserpine on the conditioned response and blood pressure of normal dogs, Category: chlorides-buliding-blocks, the publication is Shengli Xuebao (1961), 24(3-4), 151-60, database is CAplus.

In 7 normal dogs given reserpine orally at 0.005-0.03 mg./kg. for 4-15 days, the positive conditioned response decreased and the reinforcement relation changed, sometimes with change in phase. The effect on the delayed conditioned response depends on dosage. A large dose (0.25 mg./kg.) seriously upset the equilibrium in stimulation-depression mechanisms to cause a nervous condition. With a daily dose of 0.005 or 0.01 mg./kg., no change in blood pressure was observed, but a change in conditioned response was quite distinct. This indicates that the cerebral cortex is more sensitive to resperine than the midbrain. It also indicates that the change in response is not induced by the action of resperine on the vasomotor center.

Shengli Xuebao 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, Category: chlorides-buliding-blocks.

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

Duan, Cancan published the artcilePharmacokinetics and tissue distribution of cantharidin after oral administration of aqueous extracts from Mylabris in rats, Formula: C12H15ClO3, the publication is Biomedical Chromatography (2021), 35(10), e5172, database is CAplus and MEDLINE.

A sensitive gas chromatog.-mass spectroscopy method was established for the determination of cantharidin (CTD) in rat plasma and liver homogenates. During the experiment, rats were randomly divided into two groups (low, high) and were administered aqueous extract of Mylabris compound for 7 days. Then, plasma and tissue samples were taken at different time points to study the pharmacokinetics and tissue distribution of CTD in rats. The selected reaction monitoring transitions for CTD and clofibrate (internal standard) were m/z 128 → 85 and m/z 169 → 141, resp. The calibration curve ranged from 10.26 to 3,078 ng/mL for plasma and from 10.26 to 246.24 ng/mL for liver homogenates. The lower limits of quantification were 10.26 ng/mL for both plasma and liver. The intra- and inter-day precision and accuracy were <20% for both plasma and liver homogenates. Extraction recovery ranged from 89.21 to 103.61% for CTD in rat plasma and liver and from 83.79 to 102.74% for IS in rat plasma and liver. Matrix effects ranged from 93.06 to 110.44% for CTD and from 91.65 to 110.80% for IS.

Biomedical Chromatography 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, Formula: C12H15ClO3.

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

Singh, Pankaj Kumar published the artcileStructure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC, Recommanded Product: 3-Chlorobenzylchloride, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(13), 1565-1571, database is CAplus and MEDLINE.

Secondary acquired mutant EGFR (L858R-T790M) overexpressed NSCLC forms one of the prevalent form of resistant NSCLC. Another subset of resistant NSCLC includes amplified cMET in mutant EGFR derived tumors. Thus, in continuation to our previous work on these two major targets of resistant NSCLC, i.e., EGFR (L858R-T790M) and cMET, we are hereby reporting reversible inhibitors of these kinases. Out of 11 lead mols. reported in our previous study, we selected triazolo-pyrimidone (BAS 09867482) scaffold for further development of small mol. dual and reversible inhibitors. Analogs of lead with different substituents on the side ring were sketched and docked in both the target kinases, followed by mol. dynamic simulations. Analogs maintaining hydrophobic interaction with M790 in secondary acquired mutant EGFR (L858R-T790M) were selected and duly synthesized. In vitro biochem. evaluation of these mols. against EGFR (L858R-T790M) and cMET kinase, along with EGFR (L858R) kinase disclosed that three mols. were having significant dual kinase inhibitory potential with IC₅₀ values well below 100 nM. Further, in vitro anti-proliferative assay against three cell lines (A549, A431 and H460) was performed. Out of all, two compounds were having significant potency against these cell lines.

Bioorganic & Medicinal Chemistry Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C6H13BO3, Recommanded Product: 3-Chlorobenzylchloride.

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

Patel, Hitesh published the artcileSynthesis and anti-inflammatory activity of some substituted benzothiazole derivatives of 3,5-dimethyl azopyrazole, Related Products of chlorides-buliding-blocks, the publication is Inventi Impact: Med Chem (2014), 118-128, 11 pp., database is CAplus.

A series of some novel 2-aminobenzothiazole derivatives were synthesized. These substituted 2-aminobenzothiazoles has been reacted with acetyl acetone and different hydrazines to give various (3,5-dimethyl-1-substituted phenyl-1H-pyrazole-4-yl)-(substituted benzothiazole-2-yl)-diazenes I (R = H, 6-Cl, 6-OMe, 6-Br, 6-NO₂, 4-Cl; R¹ = Ph, 4-ClC₆H₄, 2,4-di-O₂NC₆H₃). The synthesized compounds were screened for their anti-inflammatory activity by in-vitro method using analgin as a standard drug. Out of the eighteen test compounds, compounds I (R = 4-Cl, 4-OMe; R¹ = Ph, 2,4-di-O₂NC₆H₃, 4-ClC₆H₄) showed good anti-inflammatory activity.

Inventi Impact: Med Chem 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, Related Products of chlorides-buliding-blocks.

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

Weng, Qinjie published the artcilePhenotypic Screening-Based Identification of 3,4-Disubstituted Piperidine Derivatives as Macrophage M2 Polarization Modulators: An Opportunity for Treating Multiple Sclerosis, Application of Methyl 4-bromo-3-chlorobenzoate, the publication is Journal of Medicinal Chemistry (2019), 62(7), 3268-3285, database is CAplus and MEDLINE.

Multiple sclerosis (MS) is a disease of the autoimmune-mediated disorder in the central nervous system, for which no effective therapeutic agent is currently available. The regulation of macrophage polarization toward M2 is a general benefit for treating MS. The gene biomarker-based phenotypic screening approach was developed, and 3,4-disubstituted piperidine derivative S-28 was identified as a lead compound modulating macrophage M2 polarization. Further SAR studies resulted in the discovery of the most potent modulator D11 that showed good oral bioavailability and significant in vivo therapeutic effects. Mechanistic studies demonstrated that the M2 polarization macrophages modulated by D11 mainly functioned through inhibiting the proliferation of T-cells and activating the phosphorylation of Stat3 and Akt. Therefore, the gene biomarker-based phenotypic screening was demonstrated as a promising tool for the discovery of novel macrophage M2 polarization modulators. Compound D11 may serve as a promising starting point for the development of therapeutics to treat MS.

Journal of Medicinal Chemistry published new progress about 117738-74-6. 117738-74-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Ester, name is Methyl 4-bromo-3-chlorobenzoate, and the molecular formula is C8H7N3, Application of Methyl 4-bromo-3-chlorobenzoate.

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

Hodgson, Ernest published the artcileNutrition and metabolism of methyl donors and related compounds in the blowfly Phormia regina, Application In Synthesis of 6249-56-5, the publication is Archives of Biochemistry and Biophysics (1960), 48-54, database is CAplus and MEDLINE.

In the nutrition of P. regina (CA 51, 6894i), γ-butyrobetaine (I) or O-acetylcarnitine served as replacements for choline (II) (quant. data given), while 2-monomethylaminoethanol was a partial replacement. The relative effectiveness of the various compounds is discussed. Ethanolamine, β-hydroxybutyrate, γ-aminobutyrate, β-hydroxy-γ-aminobutyrate, trimethylamine, and sarcosine did not serve as replacements in promoting growth, even when supplemented by other metabolites (named). The II-inhibitor 2-amino-2-methylpropanol inhibited growth, but its effects could be reversed by II and compounds which could replace II. Phospholipides containing serine, ethanolamine, and II were found to be normal constituents of 3rd instar larvae. Formate was not utilized in the biosynthesis of Me groups in II synthesis, but was metabolized with liberation of CO₂, both by the living larvae and their homogenates. Biosynthesis of II from ethanolamine either did not occur or was of little importance. The effectiveness of I as a replacement for II was of interest, since I has been described as a carnitine inhibitor in other organisms. Possible mechanisms of utilization are discussed. Metabolic differences in different spp. of insects are interpreted in relation to dietary requirements. 33 references.

Archives of Biochemistry and Biophysics 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 In Synthesis of 6249-56-5.

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

Qin, Xubo published the artcilePalladium-catalyzed highly regioselective and stereoselective decarboxylative arylation of unactivated olefins with aryl carboxylic acids, Product Details of C9H9ClO4, the publication is Tetrahedron (2017), 73(16), 2242-2249, database is CAplus.

Palladium(II)-catalyzed highly regioselective and stereoselective decarboxylative arylation of unactivated olefins with aryl carboxylic acids was developed. This method was applicable to a variety of unactivated olefins, including allylamides, long chain functionalized olefins and purely aliphatic olefins, led to the formation of linear E-configured products in high yields. Both electron-rich and electron-deficient aryl carboxylic acids were suitable arylation reagents. It was found that the choice of solvent, catalyst precursor and oxidant had an important influence on reaction efficiency. As a co-solvent and ligand, DMSO was critical to catalysis. This chem. expanded the scope of decarboxylative arylation of olefins with aryl carboxylic acids, and provides a rapid access to useful linear arylation products of unactivated olefins.

Tetrahedron published new progress about 36335-47-4. 36335-47-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Ether, name is 3-Chloro-2,6-dimethoxybenzoic acid, and the molecular formula is C9H9ClO4, Product Details of C9H9ClO4.

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