Tag: M.W=200-250

Deka, Nabajyoti published the artcileSynthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives for the treatment of metabolic syndrome, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is piperazinyl pyridinyl benzenesulfonamide preparation metabolic syndrome.

Metabolic syndrome is a widely prevalent multifactorial disorder associated with an increased risk of cardiovascular disease and type 2 diabetes mellitus. High plasma levels of insulin and glucose due to insulin resistance are a major component of the metabolic disorder. Thiazolidinediones (TZDs) are potent PPARγ ligands and used as insulin sensitizers in the treatment of type 2 diabetes mellitus. They are potent insulin-sensitizing agents but due to adverse effects like hepatotoxicity, a safer alternative of TZDs is highly demanded. The synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives I (R = 2,4-Cl2C6H3, 2,5-(OCH3)2C6H3, 2-thienyl, etc.) an alternate remedy for insulin resistance is reported.

International Journal of Medicinal Chemistry published new progress about Adipogenesis. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bajare, Swapnil published the artcileSynthesis of N-(5-chloro-6-(quinolin-3-yloxy)pyridin-3-yl)benzenesulfonamide derivatives as non-TZD peroxisome proliferator-activated receptor γ (PPARγ) agonist, Category: chlorides-buliding-blocks, the main research area is PPARgamma agonist quinolinyloxypyridinylbenzenesulfonamide preparation; benzenesulfonamide quinolinyloxypyridinyl preparation PPARgamma agonist.

The thiazolidinediones (TZDs) are a class of oral antidiabetic drugs that improve insulin sensitivity in patients with type 2 diabetes. Although the mechanism by which the TZDs lower insulin resistance is unclear, they are known to target the peroxisome proliferator-activated receptor γ (PPARγ), a nuclear hormone receptor. Ligands for PPARγ regulate adipocyte production and secretion of fatty acids as well as glucose metabolism, resulting in increased insulin sensitivity in adipose tissue, liver, and skeletal muscle. However, TZDs have several adverse effects, including weight gain and liver toxicity. Herein we report identification of non-TZD PPARγ agonists [I, Ar = substituted Ph] which exhibit beneficial effects similar to that of TZDs in animal models, but without the associated adverse effects.

European Journal of Medicinal Chemistry published new progress about Adipogenesis. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kursun Aktar, Bedriye Seda published the artcileDesigning heterocyclic chalcones, benzoyl/sulfonyl hydrazones: An insight into their biological activities and molecular docking study, Application of 4-(4-Chlorophenoxy)benzaldehyde, the main research area is BChE chalcone antiproliferative antioxidant anticholinesterase mol docking.

The aim of this study is to investigate the antioxidant, anticholinesterase and the antiproliferative activities of some chalcones, benzoyl and sulfonyl hydrazones. The antioxidant activity was studied by way of four complimentary assays and the anticholinesterase activity was studied using the Ellman method. The antiproliferative activity of the compounds was determined using a BrdU cell proliferation ELISA assay. Compound 32 (IC50: 15.58 ± 0.01μg/mL) against the brain (C6) and 29 (IC50: 5.02 ± 0.05μg/mL) against cervical (HeLa) cancer cell lines exhibited higher antiproliferative activity than the other compounds Two sulfonyl hydrazone derivatives 45 and 47 exhibited very good antioxidant activity. The results of anticholinesterase activity indicated that nine compounds 3, 8, 10, 14, 24, 25, 27, 38, and 45 significantly inhibited acetylcholinesterase enzymes and thirty-three compounds 1-4, 7-14, 22-28, 32-41, 44-47 inhibited butyrylcholinesterase enzymes (BChE) more than galantamine. In addition, virtual screening methods based on ligand 45 having the best activity against BChE was used to define new human BChE inhibitors. The interactions of ligand 8 against acetylcholinesterase (AChE) were also examined Important key residues were determined and visualized on completion of the methodol. All calculations indicated the suitability of use of the mol. docking approach for understanding interaction mechanisms and crucial fragments of novel hit compounds such as the potential lead AChE and BChE inhibitor candidates.

Journal of Molecular Structure published new progress about Antioxidants. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Application of 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Teng, Ming-yu published the artcileSynthesis, chemo-selective properties of substituted 9-aryl-9H-fluorenes from triarylcarbinols and enantiomerical kinetics of chiral 9-methoxy-11-(naphthalen-1-yl)-11H-benzo[a]fluorene, Quality Control of 35112-27-7, the main research area is fluorene aryl preparation crystal mol structure; triarylcarbinol acidification.

9-Aryl-fluorenes were synthesized conveniently from triarylcarbinols in the presence of TsOH. Notably, the orientation of the intramol. aromatic substitution reaction was dictated by the nature of the substituents on the aryl rings of triarylcarbinols, owing to electronic and conjugated effects. In particular, triarylcarbinols with (3-methoxy)phenyl and naphthalenyl groups formed benzo[a]fluorenes selectively. Moreover, 9-methoxy-11-(naphthalen-1-yl)-11H-benzo[a] fluorene, with a center of chirality, exists as a mixture of diastereoisomers, due to the restricted rotation of a C-C single bond. First-order rate constants for the enantiomerization of 9-methoxy-11-(naphthalen-1-yl)-11H-benzo[a] fluorene in DMSO were obtained over the temperature from 297 K to 393 K, and thermodn. parameters were determined as ΔH‡ = 99.7 kJ mol-1, ΔS‡373 K = 37.7 J mol-1 K-1, and ΔG‡373 K = 85.6 kJ mol-1 by Eyring plot anal.

RSC Advances published new progress about Atropisomers. 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, Quality Control of 35112-27-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rolt, Adam published the artcileDiscovery and Optimization of a 4-Aminopiperidine Scaffold for Inhibition of Hepatitis C Virus Assembly, SDS of cas: 93118-03-7, the main research area is HCV 4AP life cycle viral replication antivirals SAR ADME.

The majority of FDA-approved HCV therapeutics target the viral replicative machinery. An automated high-throughput phenotypic screen identified several small mols. as potent inhibitors of hepatitis C virus replication. Here, we disclose the discovery and optimization of a 4-aminopiperidine (4AP) scaffold targeting the assembly stages of the HCV life cycle. The original screening hit (1) demonstrates efficacy in the HCVcc assay but does not show potency prior to or during viral replication. Colocalization and infectivity studies indicate that the 4AP chemotype inhibits the assembly and release of infectious HCV. Compound 1 acts synergistically with FDA-approved direct-acting antiviral compounds Telaprevir and Daclatasvir, as well as broad spectrum antivirals Ribavirin and cyclosporin A. Following an SAR campaign, several derivatives of the 4AP series, including 77b (I), have been identified with increased potency against HCV, reduced in vitro toxicity, as well as improved in vitro and in vivo ADME properties.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, SDS of cas: 93118-03-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Cakir, Gizem published the artcileNovel 4-Thiazolidinones as Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase, Related Products of chlorides-buliding-blocks, the main research area is thiazolidinone hepatitis C virus NS5B RNA dependent polymerase inhibitor; 4-Thiazolidinones; Antiviral agents; HCV NS5B polymerase; Hepatitis C; Molecular modeling.

In continuation of the authors efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, the authors synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29-42, together with their synthetic precursors 22-28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 μM. Compound 33, an arylidene derivative, was the most active compound in this series with an IC50 value of 25.3 μM. Mol. docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds

Archiv der Pharmazie (Weinheim, Germany) published new progress about Antiviral agents. 89978-31-4 belongs to class chlorides-buliding-blocks, name is 5-(2,6-Dichlorophenyl)-1,3,4-thiadiazol-2-amine, and the molecular formula is C8H5Cl2N3S, Related Products of chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Villalonga, Reynaldo published the artcileImmobilization of Xanthine Oxidase on Carbon Nanotubes Through Double Supramolecular Junctions for Biosensor Construction, Synthetic Route of 36428-96-3, the main research area is xanthine oxidase immobilization carbon nanotube double supramol junction biosensor.

A novel approach for the noncovalent functionalization of single-walled carbon nanotubes with enzymes, using a β-cyclodextrin-modified pyrene derivative, mono-6-ethylenediamino-(2-pyrene carboxamido)-6-deoxy-β-cyclodextrin (Pyr-βCD), as a mol. bridge for the construction of a supramol. assembly between the nanotube surface and an adamantane-modified enzyme, is reported. The Pyr-βCD derivative was synthesized and its stacking to SWNT through π-π interactions accomplished. The functionalized nanotubes showed low capacity for the nonspecific adsorption of proteins, but were able to immobilize adamantane-modified xanthine oxidase via host-guest associations This double supramol. junctions-based approach was employed to modify a glassy carbon electrode with the enzyme/nanotubes complex for designing a biosensor device toward xanthine. The biosensor showed fast electroanal. response (10 s), high sensitivity (5.9 mA/M cm2) low detection limit (2 μM) and high stability.

Electroanalysis published new progress about Carbon nanotubes. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Synthetic Route of 36428-96-3.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Puleo, Thomas R. published the artcileCatalytic α-Selective Deuteration of Styrene Derivatives, Quality Control of 93118-03-7, the main research area is deuterostyrene regioselective chemoselective preparation; regioselective monodeuteration electron deficient styrene base catalyzed addition alc; dependence styrene deuteration chemoselectivity alc concentration.

Styrenes such as 4-trifluoromethylstyrene (particularly electron-deficient styrenes) underwent chemoselective and regioselective α-deuteration with DMSO-d6 in the presence of alcs. (either methanol or 1-cyclopropylethanol) and KO-t-Bu via base-catalyzed reversible addition of alkoxides to styrenes. The concentration of methanol is critical for high yields and selectivities to maximize the yield of deuteration over formation of polystyrenes; 1-cyclopropylethanol minimized the formation of nucleophilic substitution product in the monodeuteration of 2-chloro-3-vinylpyridine. The deuterated styrenes were used in the preparation of compounds with deuterated benzylic stereocenters.

Journal of the American Chemical Society published new progress about Chemoselectivity. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Quality Control of 93118-03-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yamamura, Ei-Tora published the artcileA novel method of producing the pharmaceutical intermediate (R)-2-chloromandelic acid by bioconversion, Safety of (S)-Methyl 2-(2-chlorophenyl)-2-hydroxyacetate, the main research area is chloromandelic Exophiala dermatitidis hydrolysis bioconversion; 2-chloromandelic acid; Asymmetric hydrolysis; bioconversion; esterase; expression.

(R)-2-Chloromandelic acid (RCM) is one of the chiral building blocks used in the pharmaceutical industry. As a result of screening for microorganisms that asym. hydrolyze racemic 2chloromandelic acid Me ester (CMM), Exophiala dermatitidis NBRC6857 was found to produce RCM at optical purity of 97% ee. The esterase that produces RCM, EstE, was purified from E. dermatitidis NBRC6857, and the optimal temperature and pH of EstE were 30°C and 7.0, resp. The estE gene that encodes EstE was isolated and overexpressed in Escherichia coli JM109. The activity of recombinant E. coli JM109 cells overexpressing estE was 553 times higher than that of E. dermatitidis NBRC6857. RCM was produced at conversion rate of 49% and at optical purity of 97% ee from 10% CMM with 0.45 mg-dry-cell/L recombinant E. coli JM109 cells. Based on these findings, RCM production by bioconversion of CMM may be of interest for future industrial applications.

Bioscience, Biotechnology, and Biochemistry published new progress about Escherichia coli. 32345-60-1 belongs to class chlorides-buliding-blocks, name is (S)-Methyl 2-(2-chlorophenyl)-2-hydroxyacetate, and the molecular formula is C9H9ClO3, Safety of (S)-Methyl 2-(2-chlorophenyl)-2-hydroxyacetate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ohi, Nobuhiro published the artcileSemisynthetic β-lactam antibiotics. III. Effect on antibacterial activity and COMT susceptibility of chlorine introduction into the catechol nucleus of 6-[(R)-2-[3-(3,4-dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido]penicillanic acid, Name: 3-Chloro-4-hydroxy-5-methoxybenzoic acid, the main research area is penicillanic acid antibacterial; catechol methyl transferase metabolism penicillinate.

The resistance of 6-[(R)-2-[3-(3,4-dihydroxybenzoyl)-3-(3-hydroxypropyl)-1-ureido]-2-phenylacetamido]penicillanic acid (I) [81819-61-6] to metabolism by catechol-O-methyl-transferase  [9012-25-3] was increased by introduction of the Cl atom into the catechol moiety. Penicillins having 1 or 2 Cl atoms at the positions adjacent to the OH had greater stability to COMT. This resulted in greater efficiency in vivo in exptl. Pseudomonas aeruginosa and Escherichia coli infections. In vitro activities were essentially unchanged.

Journal of Antibiotics published new progress about Escherichia coli. 62936-23-6 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-hydroxy-5-methoxybenzoic acid, and the molecular formula is C8H7ClO4, Name: 3-Chloro-4-hydroxy-5-methoxybenzoic acid.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics