Tag: M.W=200-250

Merchant, J. R. published the artcileSubstitution in the benzopyrone series. II. Sulfonation of coumarin derivatives, Related Products of chlorides-buliding-blocks, the publication is Journal of the Indian Chemical Society (1957), 35-41, database is CAplus.

ClSO₃H (2 moles) added gradually with cooling to coumarin, and the mixture heated 2 hrs. at 100°, cooled, and poured over crushed ice gave a mixture of the 6-SO₃H (I) and 6-SO₂Cl (m. 119-20°) compounds; S-benzylisothiuronium (II) derivative of I, m. 212-14°. The following compounds were treated similarly, the figures after each referring to moles ClSO₃H, temperature, and hrs. of heating, resp., and the products of sulfonation being given last: coumarin, 6, 130-40°, 3, the 3,6-di-SO₃H (III) (II derivative, m. 194-6°) and 3,6-di-SO₂Cl (m. 173-5°) compounds (amide, m. above 270°; anilide, m. 218-20°); 6-nitrocoumarin, 10, 130-40°, 4, the 3-SO₃H (IV) (II derivative, m. 230-2°) and 3-SO₂Cl (m. 204-5°) compounds (amide, m. above 290°; anilide, m. 130°); 7-hydroxy-4-methylcoumarin (V), 4, 100°, 2, the 6-SO₃H (VI) (II derivative, m. 180-2°) and 6-SO₂Cl (VII) (m. 178-80°) compounds (amide, m. above 290°; anilide, m. 245-7°); V, 4, 130-40°, 4, the 6,8-di-SO₃H compound; V, 8, 140°, 4, the 3,6,8-tri-SO₃H compound; 7-hydroxy-3,6-dibromo-4-methylcoumarin, 10, 100°, 2, the 8-SO₃H compound (VIII) (II derivative, m. 205-6°); 7-hydroxy-3,8-dibromo-4-methylcoumarin, 7.5, 100°, 2, the 6-SO₃H [II derivative, m. 238° (decomposition)] and 6-SO₂Cl (IX) [m. 210° (decomposition)] compounds (anilide, m. 210-12°); 7-methoxy-4-methylcoumarin (X), 4.3, 100°, 2, the 6-SO₃H (XI) [m. 175° (decomposition); II derivative, m. 250°] and 6-SO₂Cl (XII) (m. 203-4°) compounds (amide, m. above 310°; anilide, m. 209-10°); X, 8, 60°, 3 (in dry CHCl₃), the 3,6-di-SO₃H (XIII) [II derivative, m. 244° (decomposition)] and 3,6-di-SO₂Cl (m. 230-2°) compounds (anilide, m. 245-7°); X, excess ClSO₃H, 130-40°, a demethylated trisulfonic acid; 7-methoxy-3-bromo-4-methylcoumarin, 4, 100°, 2, the 6-SO₃H [II derivative, m. 280° (decomposition)] and 6-SO₂Cl (XIV) (m. 227-9°) compounds (anilide, m. 236-8°); 7-hydroxy-6-carbomethoxy-4-methylcoumarin, 1, 60°, 2 (in dry CHCl₃); 7-hydroxy-6-carboxy-4-methyl-8-coumarin sulfonic acid (XV) (II derivative, m. 209-11°) + unchanged substance; 7-hydroxy-6-carboxy-4-methylcoumarin, 4, 100°, 2, the 3,8-di-SO₃H compound (XVI). The position of the SO₃H group in I and III was proved by oxidation of the Na salt with alk. permanganate to give, in each case, 5-sulfosalicylic acid (II derivative, m. 194-6°). The same treatment of IV gave 5-nitrosalicylic acid, m. 227-8°. Bromination of VI (Na salt) with 1 mole Br in HOAc gave the 3,6,8-tri-Br compound, m. 250-2°, as did also bromination of VIII. VII (1 g. in 10 cc. glacial HOAc) treated hot with 11 cc. 10% Br in HOAc and left 6 hrs. at room temperature gave IX. XII brominated likewise yielded XIV. The Na salt of XI heated 15 min. with 2 moles Br in HOAc and poured into H₂O gave the 3,6-di-Br compound, m. 240° (from HOAc), as did XIII (di-Na salt) when treated with 3 moles Br. Oxidation of XI with alk. permanganate gave 2,4,5-HO(MeO)(HO₃S)C₆H₂ CO₂H (XVII) [II derivative, m. 228-30° (decomposition)], which upon bromination of its Na salt yielded the 5-Br compound, m. 251-2°. The structure of 5,2,4-HO₃S(HO)₂C₆H₂CO₂H (II derivative, m. 201-2°) obtained by Senhöfer and Brünner [Chem. Zentr. 1, 566(1879)] by sulfonating β-resorcylic acid was confirmed by its methylation to XVII. Bromination of XV and XVI gave in each case the 3,8-di-Br compound, m. 284-6° (decomposition).

Journal of the Indian Chemical Society published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Related Products of chlorides-buliding-blocks.

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

Mukhtar, Asma published the artcileIndane-1,3-diones: As Potential and Selective α-glucosidase Inhibitors, their Synthesis, in vitro and in silico Studies, Computed Properties of 19652-33-6, the publication is Medicinal Chemistry (Sharjah, United Arab Emirates) (2021), 17(8), 887-902, database is CAplus and MEDLINE.

Diabetes mellitus is one of the most chronic metabolic disorders. Since past few years, our research group had synthesized and evaluated libraries of heterocyclic compounds against α and β-glucosidase enzymes and found encouraging results. The current study comprises of evaluation of indane-1,3-dione as antidiabetic agents based on our previously reported results obtained from closely related moiety isatin and its derivatives A library of twenty three indane-1,3-dione derivatives (1-23) was synthesized and evaluated for α and β-glucosidase inhibitions. Moreover, in silico docking studies were carried out to investigate the putative binding mode of selected compounds with the target enzyme. The indane-1,3-dione derivatives (1-23) were synthesized by Knoevenagel condensation of different substituted benzaldehydes with indane-1,3-dione under basic condition. The structures of synthetic mols. were deduced by using different spectroscopic techniques, including ¹H-, ¹³C-NMR, EI-MS, and CHN anal. Compounds (1-23) were evaluated for α and β-glucosidase inhibitions by adopting the literature protocols. Off twenty three, eleven compounds displayed good to moderate activity against α- glucosidase enzyme, nonetheless, all compounds exhibited less than 50% inhibition against β- glucosidase enzyme. Compounds 1, 14, and 23 displayed good activity against α-glucosidase enzyme with IC₅₀ values of 2.80 ± 0.11, 0.76 ± 0.01, and 2.17 ± 0.18 μM, resp. The results have shown that these compounds have selectively inhibited the α-glucosidase enzyme. The in silico docking studies also supported the above results and showed different types of interactions of synthetic mols. with the active site of enzyme. The compounds 1, 14, and 23 have shown good inhibition against α-glucosidase and may potentially serve as lead for the development of new therapeutic representatives.

Medicinal Chemistry (Sharjah, United Arab Emirates) published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C7H4BrClO2, Computed Properties of 19652-33-6.

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

Mukhtar, Asma published the artcileSynthesis of Chalcones as Potential α-Glucosidase Inhibitors, In-Vitro and In-Silico Studies, HPLC of Formula: 19652-33-6, the publication is ChemistrySelect (2021), 6(37), 9933-9940, database is CAplus.

Seventeen chalcones derivatives I [R = 2-HO-3-ClC₆H₃, 4-NMe₂C₆H₄, 2-Br-4,5-(OMe)₂C₆H₂, etc.; R¹ = 3-MeC₆H₄, 4-MeC₆H₄, 4-ClC₆H₄, etc.] were synthesized by reactions of diversely substituted aldehydes with various ketones. The structures of compounds were characterized by using NMR (NMR) spectroscopy, mass spectrometry (MS) and carbon, hydrogen, nitrogen (CHN) anal. These synthetic mols. were tested for α-glucosidase inhibitory activity. Acarbose was used as a standard drug and pos. control in this study. Compound I [R = 2-HO-3,5-Cl₂C₆H₂; R¹ = 4-MeC₆H₄] with hydroxy and chloro substitutions was found to be the most active compound and a novel compound of this library. Active mols. were subjected to in silico study to determine binding interactions with target site of α-glucosidase.

ChemistrySelect published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C7H4BrClO2, HPLC of Formula: 19652-33-6.

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

Dice, John R. published the artcileα,β-Diphenyl-α-trifluoromethyl-2-pyridineethanol and related compounds as synthetic estrogens, Formula: C8H4ClF3O, the publication is Journal of Medicinal Chemistry (1966), 9(2), 176-8, database is CAplus and MEDLINE.

A series of substituted α,β-diphenyl-α-trifluoromethyl-β-(2-pyridine)ethanols (I), where R¹ is H, Cl, or OMe, and R² is H, Cl, Me, Ph, or OMe, and II, where R¹ is H or Me, R² is CF₃ or C₂F₅ and R³ is H, Me, Pr, or Ph, were synthesized. Many were potent estrogens.

Journal of Medicinal Chemistry published new progress about 5860-95-7. 5860-95-7 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Benzene,Ketone, name is 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone, and the molecular formula is C8H4ClF3O, Formula: C8H4ClF3O.

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

Selmani, Aymane published the artcileTransition-Metal-Free, Formal C-H Germylation of Arenes and Styrenes via Dibenzothiophenium Salts, Application In Synthesis of 637-07-0, the publication is Organic Letters (2021), 23(12), 4779-4784, database is CAplus and MEDLINE.

We report an operationally simple, selective, and transition-metal-free germylation of arenes and styrenes at room temperature, using a robust and bench-stable Ge source (R₃Ge-SiR₃) and dibenzothiophenium salts as enabling intermediates. The first direct engagement in cross-coupling of the newly made E-alkenyl germanes is also presented, allowing the chemoselective arylation under air-tolerant nanoparticle catalysis.

Organic Letters 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 C16H12O, Application In Synthesis of 637-07-0.

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

Rehder, Dieter published the artcileWater and bromide in the active center of vanadate-dependent haloperoxidases, HPLC of Formula: 19652-33-6, the publication is Journal of Inorganic Biochemistry (2000), 80(1-2), 115-121, database is CAplus and MEDLINE.

Two aqua-oxovanadium complexes, viz. [A-VO(H₂O)(sal-L-Leu)] (I) and [VO(H₂O)₂(5-Br-sal-Gly)]·H₂O(II·H₂O ), containing the water ligands in cis- and trans-positions to the oxo group at V-OH₂ distances ranging from 2.008 to 2.228 Å, have been structurally characterized in order to model the apical electron d. feature found in the structures of fungal and algal vanadate-dependent peroxidases. Br K-edge XAS of bromide-treated bromoperoxidase from Ascophyllum nodosum and model compounds (including II·H₂O) has been used to show that the substrate bromide does not bind to active site vanadium but to a light atom, possibly carbon, in its vicinity.

Journal of Inorganic Biochemistry published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C7H4BrClO2, HPLC of Formula: 19652-33-6.

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

Abdeen, Sanofar published the artcileTargeting the HSP60/10 chaperonin systems of Trypanosoma brucei as a strategy for treating African sleeping sickness, SDS of cas: 10543-42-7, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(21), 5247-5253, database is CAplus and MEDLINE.

Trypanosoma brucei are protozoan parasites that cause African sleeping sickness in humans (also known as Human African Trypanosomiasis-HAT). Without treatment, T. brucei infections are fatal. There is an urgent need for new therapeutic strategies as current drugs are toxic, have complex treatment regimens, and are becoming less effective owing to rising antibiotic resistance in parasites. The authors hypothesize that targeting the HSP60/10 chaperonin systems in T. brucei is a viable anti-trypanosomal strategy as parasites rely on these stress response elements for their development and survival. The authors recently discovered several hundred inhibitors of the prototypical HSP60/10 chaperonin system from Escherichia coli, termed GroEL/ES. One of the most potent GroEL/ES inhibitors the authors discovered was compound (I). While examining the PubChem database, the authors found that a related analog, 4-methyl-N-(4-(5-((4-methylphenyl)sulfonamido)benzo[d]oxazol-2-yl)phenyl)benzenesulfonamide (2e-p), exhibited cytotoxicity to Leishmania major promastigotes, which are trypanosomatids highly related to Trypanosoma brucei. Through initial counter-screening, the authors found that compounds (I) and 2e-p were also cytotoxic to Trypanosoma brucei parasites (EC₅₀ = 7.9 and 3.1 μM, resp.). These encouraging initial results prompted the authors to develop a library of inhibitor analogs and examine their anti-parasitic potential in vitro. Of the 49 new chaperonin inhibitors developed, 39% exhibit greater cytotoxicity to T. brucei parasites than parent compound (I). While many analogs exhibit moderate cytotoxicity to human liver and kidney cells, the authors identified mol. substructures to pursue for further medicinal chem. optimization to increase the therapeutic windows of this novel class of chaperonin-targeting anti-parasitic candidates. An intriguing finding from this study is that suramin, the first-line drug for treating early stage T. brucei infections, is also a potent inhibitor of GroEL/ES and HSP60/10 chaperonin systems.

Bioorganic & Medicinal Chemistry Letters published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, SDS of cas: 10543-42-7.

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

Ibarra-Lara, L. published the artcileClofibrate improves myocardial ischemia-induced damage through regulation of renin-angiotensin system and favours a pro-vasodilator profile in left ventricle, Formula: C12H15ClO3, the publication is Journal of Pharmacological Sciences (Amsterdam, Netherlands) (2020), 144(4), 218-228, database is CAplus and MEDLINE.

Myocardial ischemia initiates a chain of pathol. conditions leading to cardiomyocyte death. Therefore, pharmacol. treatment to stop ischemia-induced damage is necessary. Fibrates, have been reported to decrease inflammatory markers and to modulate the renin-angiotensin system (RAS). Our aim was to explore if clofibrate treatment, administered one week after myocardial event, decreases MI-induced cardiac damage. Wistar rats were assigned to: 1. Sham or 2. Coronary artery ligation (MI). Seven days after, rats were subdivided to receive vehicle (V) or clofibrate [100 mg/kg (C)] daily for 7 days. Blood samples and left ventricle were analyzed. RAS components [angiotensin II, angiotensin converting enzyme (ACE), and AT1-receptor] decreased in MI-C compared to MI-V, while [Ang-(1-7), bradykinin, ACE-2, and AT2-receptor] raised in response to clofibrate treatment. Oxidative stress markers increased in MI-V rats, a profile reverted in MI-C rats. Nitric oxide (NO) pathway (Akt, eNOS, and NO) exhibits a lower participation in MI-V, but clofibrate raised NO-pathway components and its production MI-induced fibrosis and structural damage was also improved by clofibrate-treatment. In conclusion, clofibrate administration to 7 days MI-rats exerts an antioxidant, pro-vasodilator expression profile, and anti-fibrotic effect suggesting that PPARα activation can be considered a therapeutic target to improve cardiac condition posterior to ischemia.

Journal of Pharmacological Sciences (Amsterdam, Netherlands) 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

Rooney, John published the artcileA Gene Expression Biomarker Identifies Chemical Modulators of Estrogen Receptor α in an MCF-7 Microarray Compendium, Related Products of chlorides-buliding-blocks, the publication is Chemical Research in Toxicology (2021), 34(2), 313-329, database is CAplus and MEDLINE.

Identification of chems. that affect hormone-regulated systems will help to predict endocrine disruption. In our previous study, a 46 gene biomarker was found to be an accurate predictor of estrogen receptor (ER) α modulation in chem. treated MCF-7 cells. Here, potential ERα modulators were identified using the biomarker by screening a microarray compendium consisting of ∼1600 gene expression comparisons representing exposure to ∼1200 chems. A total of ∼170 chems. were identified as potential ERα modulators. In the Connectivity Map 2.0 collection, 75 and 39 chems. were predicted to activate or suppress ERα, and they included 12 and 6 known ERα agonists and antagonists/selective ERα modulators, resp. Nineteen and 8 of the total number were also identified as active in an ERα trans-activation assay carried out in a MCF-7-derived cell line used to screen the Tox21 10K chem. library in agonist or antagonist modes, resp. Chems. predicted to modulate ERα in MCF-7 cells were examined further using global and targeted gene expression in wild-type and ERα-null cells, trans-activation assays, and cell-free ERα coregulator interaction assays. Environmental chems. classified as weak and very weak agonists were confirmed to activate ERα including apigenin, kaempferol, and oxybenzone. Novel activators included digoxin, nabumetone, ivermectin, and six progestins. Novel suppressors included emetine, mifepristone, niclosamide, and proscillaridin. Our strategy will be useful to identify environmentally relevant ERα modulators in future high-throughput transcriptomic screens.

Chemical Research in Toxicology 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, Related Products of chlorides-buliding-blocks.

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

Onopchenko, Anatoli published the artcileTetraalkylsilanes via hydrosilylation of 1-alkenes, Recommanded Product: Dichloro(methyl)(octyl)silane, the publication is Journal of Chemical and Engineering Data (1988), 33(1), 64-6, database is CAplus.

Tetraalkylsilanes with 1 short and 3 long alkyl groups were prepared via a 2-step hydrosilylation procedure, which appears more suited for com. production than the Grignard or alkyllithium routes used previously. The viscosities of 2-component blends were treated by the ASTM D-341 procedure. The thermal stabilities of some silahydrocarbons and model paraffins, measured by the loss of their 40° viscosity, were determined at 371°.

Journal of Chemical and Engineering Data published new progress about 14799-93-0. 14799-93-0 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(methyl)(octyl)silane, and the molecular formula is C9H20Cl2Si, Recommanded Product: Dichloro(methyl)(octyl)silane.

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