Tag: M.W=200-250

Elkamhawy, Ahmed published the artcileDesign, synthesis and biological evaluation of novel thiazolidinedione derivatives as irreversible allosteric IKK-β modulators, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is benzylidene thiazolidinedione diastereoselective preparation antiinflammatory cytotoxicity allosteric IKKbeta modulator; thiazolidinedione benzaldehyde Knoevenagel condensation; Allosteric modulation; IKK-β modulators; NF-κB signaling pathway; Thiazolidinediones.

A series of thiazolidinedione-scaffold based chem. entities I [n = 3, 4, 5; R1 = 2-methoxyethyl, 3-methoxypropyl, cyclopropylmethyl, cyclopropanecarbonyl, methylsulfonyl; R2 = 4-(4-fluorophenoxy)phenyl, 4-(4-chlorophenoxy)phenyl, 4-(4-bromophenoxy)phenyl, 4-(4-nitrophenoxy)phenyl, 3-chloro-4-morpholino-phenyl] was synthesized and evaluated as potential allosteric covalent IKK-β modulators. Relative to the starting hit compound, derivatives I [n = 4, R1 = cyclopropylmethyl, R2 = 4-(4-nitrophenoxy)phenyl (II), 4-(4-fluorophenoxy)phenyl; n = 3, R1 = cyclopropylmethyl, R2 = 4-(4-nitrophenoxy)phenyl] elicited enhanced activity by 57-69 folds showing low micromolar IC50 values within the range of 1.4-1.7 mM. In addition, derivatives I [n = 5, R1 = cyclopropylmethyl, R2 = 4-(4-fluorophenoxy)phenyl (III), 3-chloro-4-morpholino-Ph; n = 3, R1 = cyclopropylmethyl, R2 = 3-chloro-4-morpholino-Ph (IV)] showed submicromolar IC50 values within the range of 0.4-0.9 mM, which was 243, 139 and 105 folds enhanced values. Kinetic study of compounds III and IV confirmed this class of modulators as irreversible inhibitors. Cellular assays presented compounds II and III as anti-inflammatory agents which suppressed both LPS-induced PGE2 and TNF-α production without non-specific cytotoxicity. Assay of hERG inhibition demonstrated a safe profile of compound II suggesting it as a lead for further development of IKK-β modulators.

European Journal of Medicinal Chemistry published new progress about Allosterism. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.

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

Hradil, Pavel published the artcileSynthesis, NMR spectra and X-ray data of chloro and dichloro derivatives of 3-hydroxy-2-phenylquinolin-4(1H)-ones and their cytostatic activity, Application of 2-Amino-3,6-dichlorobenzoic acid, the main research area is hydroxy phenylquinolinone preparation cytostatic agent.

As known, some derivatives of quinolin-4(1H)-one possess interesting biol. properties. The biol. and cytostatic activity of 2-substituted 3-hydroxyquinolin-4(1H)-ones has not been reported yet. In this paper the synthesis of a series of chloro and dichloro 2-phenyl-3-hydroxyquinolin-4(1H)-ones and their characterization by NMR spectra and X-ray data is described. Their cytostatic properties have been evaluated and the results are reported.

Journal of Heterocyclic Chemistry published new progress about Cyclization. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application of 2-Amino-3,6-dichlorobenzoic acid.

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

Casas-Solvas, Juan M. published the artcileA Practical, Large-Scale Synthesis of Pyrene-2-Carboxylic Acid, COA of Formula: C17H10O2, the main research area is pyrenecarboxylic acid preparation electrophilic aromatic substitution cyclization ring opening.

Pyrene-2-carboxylic acid is a versatile intermediate for introducing the unusual 2-pyrenyl unit into functional organic mols. A classical preparation for this mol. has been revised and improved to give a robust and efficient three-step process. The method has been applied on a multigram scale to give pyrene-2-carboxylic acid in >70% overall yield from pyrene.

Synlett published new progress about Cyclization. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, COA of Formula: C17H10O2.

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

Okuzumi, Tatsuya published the artcileEfficient solid-phase synthesis of quinazoline-2,4-diones with various substituents on aromatic rings, Product Details of C7H5Cl2NO2, the main research area is solid phase synthesis quinazolinedione electron withdrawing substituent; anthranilamide formation solid support cyclization carbonyldiimidazole.

The authors have developed a method for the solid-phase synthesis of quinazoline-2,4-diones with various substituents on the aromatic ring. Although there were numerous reports of the solid-phase synthesis of quinazoline-2,4-diones, they were not applicable to the synthesis of the quinazoline-2,4-diones with electron-withdrawing substituents on the aromatic ring. Considering the poor nucleophilicity of the amino group of anthranilic acids, coupling of anthranilic acids to solid-supported amines was studied without protecting the amino group. Various anthranilamides were prepared using anthranilic acids with electron-withdrawing substituents because a wide range of anthranilic acids are com. available. These anthranilamides were successfully cyclized with carbonyldiimidazole to give quinazoline-2,4-diones with high purity.

Tetrahedron published new progress about Cyclization. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Product Details of C7H5Cl2NO2.

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

Qiu, Li published the artcileReductive Ring Closure Methodology toward Heteroacenes Bearing a Dihydropyrrolo[3,2-b]pyrrole Core: Scope and Limitation, COA of Formula: C7H5Cl2NO2, the main research area is aminobenzoate cyclization chlorination reductive ring closure alkylation; heteroacene dihydropyrrolopyrrole preparation.

A newly developed reductive ring closure methodol. to heteroacenes bearing a dihydropyrrolo[3,2-b]pyrrole core, e.g., I (R = n-octyl), was systematically studied for its scope and limitation. The methodol. involves (i) the cyclization of an o-aminobenzoic acid ester derivative to give an eight-membered cyclic dilactam, and (ii) the conversion of the dilactams into the corresponding diimidoyl chloride, which undergoes (iii) reductive ring closure to install the dihydropyrrolo[3,2-b]pyrrole core. The first step of the methodol. plays the key role due to its substrate limitation, which suffers from the competition of oligomerization and hydrolysis. All the dilactams could successfully convert to the corresponding diimidoyl chlorides, most of which succeeded to give the dihydropyrrolo[3,2-b]pyrrole core. The influence of the substituents and the elongation of conjugated length on the photophys. properties of the obtained heteroacenes were then investigated systematically using UV-vis spectroscopy and cyclic voltammetry. It was found that chlorination and fluorination had quite a different effect on the photophys. properties of the heteroacene, and the ring fusing pattern also had a drastic influence on the band gap of the heteroacene. The successful preparation of a series of heteroacenes bearing a dihydropyrrolo[3,2-b]pyrrole core would provide a wide variety of candidates for further fabrication of organic field-effect transistor devices.

Journal of Organic Chemistry published new progress about Alkylation. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, COA of Formula: C7H5Cl2NO2.

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

Keith, John M. published the artcileAryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate, HPLC of Formula: 61343-99-5, the main research area is aryl piperazinyl urea preparation FAAH inhibitor SAR analgesic; FAAH; FAAH-2; anandamide; enzyme; ethanolamides; urea.

A series of aryl piperazinyl ureas that act as covalent inhibitors of fatty acid amide hydrolase (FAAH) is described. A potent and selective (does not inhibit FAAH-2) member of this class, JNJ-40355003 (I), was found to elevate the plasma levels of three fatty acid amides: anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide, in the rat, dog, and cynomolgous monkey. The elevation of the levels of these lipids in the plasma of monkeys suggests that FAAH-2 may not play a significant role in regulating plasma levels of fatty acid ethanolamides in primates.

ACS Medicinal Chemistry Letters published new progress about Analgesics. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, HPLC of Formula: 61343-99-5.

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

Nazarov, A. P. published the artcileElectron polarizability of molecules of carboxylic acids and their dimers and trimers, Recommanded Product: Pyrene-2-carboxylic acid, the main research area is carboxylic acid dimer trimer hydrogen bond electron polarizability.

Components of the tensor of the electron polarizability of mols. of carboxylic acids and their dimers and trimers with conjugated chem. bonds are calculated according the Hartree-Fock method. The dependences of a change in the anisotropy of polarizability on the average polarizability of a mol. and the number of electrons in a conjugated system are determined An increase in the anisotropy of electron polarizability during the formation of intermol. associates through hydrogen bonds is observed

Russian Journal of Physical Chemistry A published new progress about Anisotropy. 36428-96-3 belongs to class chlorides-buliding-blocks, name is Pyrene-2-carboxylic acid, and the molecular formula is C17H10O2, Recommanded Product: Pyrene-2-carboxylic acid.

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

Yin, Lu published the artcileA rapid and green approach to chiral α-hydroxy esters: asymmetric transfer hydrogenation (ATH) of α-keto esters in water by use of surfactants, HPLC of Formula: 32345-60-1, the main research area is keto ester surfactant water ruthenium asym transfer hydrogenation; hydroxy ester stereoselective preparation green chem.

A series of α-hydroxy esters were rapidly prepared (1.5 h) from α-keto esters via asym. transfer hydrogenation in water by the use of surfactants. This green method, catalyzed by a water-soluble and recyclable Ru(II) complex, gave moderate to high enantioselectivities (up to 99.7% ee) with DTAB as an additive and HCO2Na as the hydrogen source.

Tetrahedron: Asymmetry published new progress about Green chemistry. 32345-60-1 belongs to class chlorides-buliding-blocks, name is (S)-Methyl 2-(2-chlorophenyl)-2-hydroxyacetate, and the molecular formula is C9H9ClO3, HPLC of Formula: 32345-60-1.

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

Kim, Doyeon published the artcileIdentification and characterization of potent, selective and metabolically stable IKKβ inhibitor, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is rhodanine derivative preparation IKKbeta inhibitor structure activity; Allosteric inhibitor; IKKβ inhibitor; NF-κB; Reumatoid arthritis.

The authors have previously reported the identification of a rhodanine compound (I) with well-balanced inhibitory activity against IKKβ and collagen-induced TNFα activated cells. However, the authors need more optimized compounds because of its instability over plasma and microsome. As part of a program directed toward the optimization of IKKβ inhibitor, the authors modified a substituent of parent compound to a series of functional groups. Among substituted compounds, fluorine substituent (II) on the para position of Ph ring restored the stability toward plasma and microsome while retaining inhibitory potency and selectivity against IKKβ over other kinases. Also, the authors have demonstrated that compound (II) is an ATP non-competitive inhibitor and safe enough to apply to animal experiment from an acute toxicity test.

Bioorganic & Medicinal Chemistry Letters published new progress about Acute toxicity. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Recommanded Product: 4-(4-Chlorophenoxy)benzaldehyde.

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

Patel, Leena published the artcileDiscovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability, Synthetic Route of 3032-32-4, the main research area is phosphoinositide kinase inhibitor.

Aberrant signaling of phosphoinositide-3-kinase delta (PI3K-delta) has been implicated in numerous pathologies including hematol. malignancies and rheumatoid arthritis. Described in this manuscript is the discovery, optimization and in vivo evaluation of a novel series of pyridine-containing PI3K-delta inhibitors. This work led to the discovery of I, a highly selective inhibitor of PI3K-delta which displays an excellent pharmacokinetic profile and is efficacious in a rodent model of rheumatoid arthritis.

Journal of Medicinal Chemistry published new progress about Antiarthritics. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Synthetic Route of 3032-32-4.

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