Category: 351003-34-4

Deprez-Poulain, Rebecca; Hennuyer, Nathalie; Bosc, Damien; Liang, Wenguang G.; Enee, Emmanuelle; Marechal, Xavier; Charton, Julie; Totobenazara, Jane; Berte, Gonzague; Jahklal, Jouda; Verdelet, Tristan; Dumont, Julie; Dassonneville, Sandrine; Woitrain, Eloise; Gauriot, Marion; Paquet, Charlotte; Duplan, Isabelle; Hermant, Paul; Cantrelle, Francois- Xavier; Sevin, Emmanuel; Culot, Maxime; Landry, Valerie; Herledan, Adrien; Piveteau, Catherine; Lippens, Guy; Leroux, Florence; Tang, Wei-Jen; van Endert, Peter; Staels, Bart; Deprez, Benoit published the artcile< Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice>, Quality Control of 351003-34-4, the main research area is insulin degrading enzyme glucose intolerance catalysis.

Insulin-degrading enzyme (IDE) is a protease that cleaves insulin and other bioactive peptides such as amyloid-β. Knockout and genetic studies have linked IDE to Alzheimer’s disease and type-2 diabetes. As the major insulin-degrading protease, IDE is a candidate drug target in diabetes. Here we have used kinetic target-guided synthesis to design the first catalytic site inhibitor of IDE suitable for in vivo studies (BDM44768). Crystallog. and small angle X-ray scattering analyses show that it locks IDE in a closed conformation. Among a panel of metalloproteases, BDM44768 selectively inhibits IDE. Acute treatment of mice with BDM44768 increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner. These results confirm that IDE is involved in pathways that modulate short-term glucose homeostasis, but casts doubt on the general usefulness of the inhibition of IDE catalytic activity to treat diabetes.

Nature Communications published new progress about Alzheimer disease. 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Quality Control of 351003-34-4.

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

Chiu, George; Li, Shengjian; Connolly, Peter J.; Pulito, Virginia; Liu, Jingchun; Middleton, Steven A. published the artcile< (Phenylpiperidinyl)cyclohexylsulfonamides: Development of α1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS)>, HPLC of Formula: 351003-34-4, the main research area is phenylpiperidinylcyclohexyl benzenesulfonamide preparation alpha1a alpha1d selective adrenergic receptor antagonist; benign prostatic hyperplasia lower urinary tract drug phenylpiperidinylcyclohexyl benzenesulfonamide.

Although α1 adrenergic receptor blockers can be very effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited by CV-related side-effects that are caused by the subtype non-selective nature of the current drugs. To overcome this problem, it was hypothesized that a α1a/1d subtype selective antagonist would bring more benefit for the therapy of BPH/LUTS. In developing such selective α1a/1d ligands, (phenylpiperidinyl)cyclohexylsulfonamides (e.g. N-[cis-4-[4-(2-isopropoxyphenyl)piperidin-1-yl]cyclohexyl]-3,4-dimethoxybenzenesulfonamide) were synthesized and evaluated for binding to three cloned human α1-adrenergic receptor subtypes. Many compounds showed equal affinity for both α1a and α1d subtypes with good selectivity vs. the α1b subtype.

Bioorganic & Medicinal Chemistry Letters published new progress about Arenesulfonamides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, HPLC of Formula: 351003-34-4.

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

Blades, Kevin; Demeritt, Julie; Fillery, Shaun; Foote, Kevin M.; Greenwood, Ryan; Gregson, Clare; Hassall, Lorraine A.; McGuire, Thomas M.; Pike, Kurt G.; Williams, Emma published the artcile< Expedient synthesis of biologically important sulfonylmethyl pyrimidines>, Computed Properties of 351003-34-4, the main research area is sulfonylmethyl pyrimidine preparation.

Two novel synthetic strategies that allow rapid diversification of the sulfone moiety in sulfonylmethyl pyrimidines, a class of compounds with a wide range of biol. activity, which are of interest in a wide variety of drug discovery programs, are described.

Tetrahedron Letters published new progress about Pyrimidines Role: SPN (Synthetic Preparation), PREP (Preparation). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Computed Properties of 351003-34-4.

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

Wang, Wentian; Zhang, Lu; Morlock, Lorraine; Williams, Noelle S.; Shay, Jerry W.; De Brabander, Jef K. published the artcile< Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)>, Application of C7H5ClF2O3S, the main research area is preparation TASIN analog targeting colorectal cancer.

Despite advances in targeted anticancer therapies, there are still no small-mol.-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small mol. that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chem. evaluation of a collection of TASIN analogs and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogs were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Application of C7H5ClF2O3S.

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

Luzina, Elena L.; Popov, Anatoliy V. published the artcile< Synthesis of 1-aroyl(1-arylsulfonyl)-4-bis(trifluoromethyl)alkyl semicarbazides as potential physiologically active compounds>, Name: 4-(Difluoromethoxy)benzene-1-sulfonyl chloride, the main research area is preparation semicarbazide physiol active compound Lipinski Gelovani parameter.

1,1-Bis(trifluoromethyl)alkyl isocyanates obtained from perfluoroisobutene (PFIB) react with aroyl(arylsulfonyl)hydrazines. Twenty eight prospective biol. active polyfluorinated 1,4-substituted semicarbazides, e.g. I, were synthesized. The structure of each new product was confirmed by anal. and spectroscopic methods. The Lipinski’s and Gelovani’s parameters were then calculated Two adjustments to the Lipinski rules of five are suggested for fluorinated drug candidates.

Journal of Fluorine Chemistry published new progress about Semicarbazides Role: SPN (Synthetic Preparation), PREP (Preparation). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Name: 4-(Difluoromethoxy)benzene-1-sulfonyl chloride.

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

Chupak, Louis S.; Zheng, Xiaofan; Hu, Shuanghua; Huang, Yazhong; Ding, Min; Lewis, Martin A.; Westphal, Ryan S.; Blat, Yuval; McClure, Andrea; Gentles, Robert G. published the artcile< Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase>, Computed Properties of 351003-34-4, the main research area is benzylic glycine sulfonamide preparation diacylglycerol lipase inhibitor structure activity; 2-Arachidonoylglycerol; Diacylglycerol; Endocannabinoid; Glycine; Lipase inhibitor; Sulfonamide.

N-Benzylic-substituted glycine sulfonamides that reversibly inhibit diacylglycerol (DAG) lipases are reported. Detailed herein are the structure activity relationships, profiling characteristics and physico-chem. properties for the first reported series of DAG lipase (DAGL) inhibitors that function without covalent attachment to the enzyme. Highly potent examples are presented that represent valuable tool compounds for studying DAGL inhibition and constitute important leads for future medicinal chem. efforts.

Bioorganic & Medicinal Chemistry published new progress about Diglycerides Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Computed Properties of 351003-34-4.

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