Category: 93118-03-7

Liu, Xiaoguang published the artcileDevelopment of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss, Category: chlorides-buliding-blocks, the main research area is mitochondrial pyruvate carrier inhibitors hair loss inhibition.

Herein, we report the synthesis and evaluation of novel analogs of UK-5099 both in vitro and in vivo for the development of mitochondrial pyruvate carrier (MPC) inhibitors to treat hair loss. A comprehensive understanding of the structure-activity relationship was obtained by varying four positions of the hit compound, namely, the alkyl group on the N1 position, substituents on the indole core, various aromatic and heteroaromatic core structures, and various Michael acceptors. The major discovery was that the inhibitors with a 3,5-bis(trifluoromethyl)benzyl group at the N1 position were shown to have much better activity than JXL001 (UK-5099) to increase cellular lactate production Addnl., analog JXL069, possessing a 7-azaindole heterocycle, was also shown to have significant MPC inhibition activity, which further increases the chem. space for drug design. Finally, more than 10 analogs were tested on shaved mice by topical treatment and promoted obvious hair growth on mice.

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

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

Arrowsmith, John E. published the artcileLong-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents, HPLC of Formula: 93118-03-7, the main research area is aminoalkoxymethyldihydropyridinedicarboxylate preparation calcium antagonist; pyridinedicarboxylate aminoalkoxymethyldihydro; vasodilator aminoalkoxymethyldihydropyridinedicarboxylate preparation.

Aminoalkoxymethyldihydropyridines I [R = Ph, substituted Ph, 1-naphthyl, 2-thienyl, 4-pyridyl; R1 = (un)substituted NH2; n = 2, 3] were prepared from RCHO, R1(CH2)nOCH2COCH2CO2Et, and H2NCMe:CHCO2Me or via I (R = N3, phthalimido). Their potencies as Ca antagonists were determined I (R = 2-ClC6H4, R1 = NH2, n = 2) (amlodipine) was comparable in potency to nifedipine and had an elimination half-life of 30 h in dogs. Oral bioavailability approached 100%, and hemodynamic responses were gradual in onset and long-lasting in effect. The two enantiomers were prepared; the bulk of the activity resided with the (-)-isomer. X-ray crystallog. studies, carried out on I (R = 2-ClC6H4, R = morpholinosulfonyl, n = 2) suggest the existence of a weak H bond between the side-chain O and the H on the ring N.

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

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

Gozde Gunduez, Miyase published the artcileSubstituted 9-aryl-1,8-acridinedione derivatives and their effects on potassium channels, Product Details of C8H4ClF3O, the main research area is acridinedione derivative SAR preparation potassium channel opener.

In this study, 12 new 3,6-dimethyl-9-aryl-3,4,6,7-tetrahydroacridine-1,8(2H,5H,9H,10H)-diones derivatives were synthesized. Synthesis of the compounds was realized by the reaction of 5-methyl-1,3-cyclohexanedione, the appropriate aromatic aldehyde, and ammonium acetate in methanol. The structure of the compounds was elucidated by IR, 1H-NMR, 13C-NMR, mass spectroscopy, and elemental anal. Functional effects of the compounds on vascular potassium channels and mechanism of phenylephrine-induced contractile responses were investigated in isolated rat aorta rings. Pinacidil was used as a standard potassium channel opener.

Medicinal Chemistry Research published new progress about Hypertension. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Product Details of C8H4ClF3O.

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

Ameriks, Michael K. published the artcilePreclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists, Category: chlorides-buliding-blocks, the main research area is dihydrotriazolopyrazinone P2X7 receptor antagonist SAR preparation; 6,7-Dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one; Autoradiography; CNS; Depression; P2X7.

The synthesis, SAR, and preclin. characterization of a series of substituted 6,7-dihydro[1,2,4]triazolo[4,3]pyrazin-8(5H)-one P2X7 receptor antagonists are described. Optimized leads from this series comprise some of the most potent human P2X7R antagonists reported to date (IC50s < 1 nM). They also exhibit sufficient potency and oral bioavailability in rat to enable extensive in vivo profiling. Although many of the disclosed compounds are peripherally restricted, compound I is brain penetrant and upon oral administration demonstrated dose-dependent target engagement in rat hippocampus as determined by ex vivo receptor occupancy with radiotracer II (ED50 = 0.8 mg/kg). Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Category: chlorides-buliding-blocks.

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

Archibald, John L. published the artcileDesign of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl substituted dihydropyridines, Recommanded Product: 2-Chloro-3-(trifluoromethyl)benzaldehyde, the main research area is pyridine heteroaryl preparation antithrombotic antihypertensive; antithrombotic antihypertensive heteroaryldihydropyridine.

An approach to the design of potential combined antithrombotic-antihypertensive agents is described. A series of 1,4-dihydropyridines bearing a 1H-imidazol-1-yl or pyrid-3-yl substituted side chain in the 2-position, e.g. I (R, R1 = Me, Et; R2 = 3-pyridyl, 1-imidazolyl, R3 = 2, 3-NO2, X = CH2, CH2O) were synthesized and tested for antihypertensive activity in spontaneously hypertensive rats and for inhibition of TXA2 synthetase in rabbit platelets, in vitro. I (R = Et, R1 = Me, R2 = 1-imidazolyl, R3 = 3-NO2, X = CH2) (II) was shown to be similar in potency to nitrendipine as an antihypertensive agent. II inhibited TXA2 synthetase in rabbit and human platelets in vitro and reduced plasma TXB2 levels in rats at antihypertensive dose levels. The reductions in thromboxane production observed in vivo and in vitro were accompanied by enhanced levels of 6-KPGF1α, reflecting diversion of the arachidonic acid cascade towards prostacyclin synthesis.

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

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

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

Dickens, Michael P. published the artcile5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2, Application In Synthesis of 93118-03-7, the main research area is deazaflavin derivative preparation p53 ubiquitination inhibitor SAR; Cancer; Deazaflavin; HDM2–p53; Ubiquitin E3 ligase; Ubiquitination inhibitors.

Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumor suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure-activity relation (SAR) anal. through systematic modification of the 5-deazaflavin template. This anal. shows that HDM2-inhibitory activity depends on a combination of factors. The most active compounds (e.g., I) contain a trifluoromethyl or chloro substituent at the deazaflavin C9 position and this activity depends to a large extent on the presence of at least one addnl. halogen or Me substituent of the Ph group at N10. Our SAR results, in combination with the HDM2 RING domain receptor recognition model we present, form the basis for the design of drug-like and potent activators of p53 for potential cancer therapy.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.

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

Wilson, Jennifer M. published the artcileSynthesis of 5-deazaflavin derivatives and their activation of p53 in cells, Name: 2-Chloro-3-(trifluoromethyl)benzaldehyde, the main research area is structure deazaflavin derivative preparation p53 antitumor apoptosis E3 HMD2.

A family of 5-deazaflavin derivatives has been synthesized using a two-step convergent strategy. The biol. activity of these compounds was evaluated in cells, by assessing their ability to stabilize and activate p53. These compounds may act as low mol. weight inhibitors of the E3 activity of HMD2 in tumors that retain wild-type p53. Importantly, we have demonstrated that the nitro group present in all three of the original lead compounds [1-3 (HL198C-E)] is not essential for observation of this biol. activity.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Name: 2-Chloro-3-(trifluoromethyl)benzaldehyde.

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

Senkardes, Sevil published the artcileSynthesis, molecular docking and evaluation of novel sulfonyl hydrazones as anticancer agents and COX-2 inhibitors, Product Details of C8H4ClF3O, the main research area is prostate breast cancer fibroblast cell COX2 inhibitor sulfonyl hydrazone; Anticancer activity; Apoptosis; Cyclooxygenase; Molecular docking; Sulfonylhydrazones.

In trying to develop new anticancer agents, a series of sulfonylhydrazones were synthesized. All synthesized compounds were checked for identity and purity using elemental anal., TLC and HPLC and were characterized by their m.ps., FT-IR and NMR spectral data and evaluated for their cytotoxic activity against prostate cancer (PC3), breast cancer (MCF-7) and L929 mouse fibroblast cell lines. Among them, N’-[(2-chloro-3-methoxyphenyl)methylidene]-4-methylbenzenesulfonohydrazide (3k) showed the potent anticancer activity against both cancer cells with good selectivity. Further investigation confirmed that 3k displayed morphol. alterations in PC3 and MCF-7 cells and promoted apoptosis through down-regulation of the Bcl-2 and upregulation of Bax expression. Addnl., compound 3k was identified as the most potent COX-2 inhibitor (91% inhibition) beside lower COX-1 inhibition. Mol. docking of the tested compounds represented important binding modes which may be responsible for their anticancer activity via inhibition of the COX-2 enzyme. Overall, the lead compound 3k deserves further development as a potential anticancer agent.

Molecular Diversity published new progress about Antitumor agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Product Details of C8H4ClF3O.

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