Category: 5335-40-0

Toja, E.; Gorini, C.; Zirotti, C.; Barzaghi, F.; Galliani, G. published the artcile< Amnesia-reversal activity of a series of 5-alkoxy-1-arylsulfonyl-2-pyrrolidinones>, Quality Control of 5335-40-0, the main research area is pyrrolidinone alkoxyarylsulfonyl preparation antiamnesic; alkoxyarylsulfonylpyrrolidinone preparation antiamnesic antihypoxic.

A series of 5-alkoxy-1-arylsulfonyl-2-pyrrolidinones were prepared by condensation of arylsulfonyl chlorides with 5-alkoxy-2-pyrrolidinones. Most compounds reversed electroconvulsive shock-induced amnesia in mice, showing the typical inverted U-shaped dose-response curve. The results for 58 compounds indicate that the potency is maximum when there is a 5-ethoxy group and progressively declines as the ether alkyl chain is either elongated or shortened. Substitution on the Ph ring or its replacement with heterocyclic rings or its hydrogenation decreases the activity. The most promising compounds, with anti-amnesic properties superior in many respects (greater potency, greater efficacy and broader active dose-range) to those of piracetam and antiracetam were further evaluated for reversing scopolamine-induced amnesia and for their antihypoxic activity. 5-Ethoxy-1-phenylsulfonyl-2-pyrrolidinone and 5-(1-methylethoxy)-1-[3-(trifluoromethyl)phenylsulfonyl]-2-pyrrolidinone were selected for further evaluation because of their potent anti-amnesic and/or antihypoxic activity.

European Journal of Medicinal Chemistry published new progress about Amnesia. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Quality Control of 5335-40-0.

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

Wu, Xishan; Shen, Hui; Zhang, Yan; Wang, Chao; Li, Qiu; Zhang, Cheng; Zhuang, Xiaoxi; Li, Chenchang; Shi, Yudan; Xing, Yanli; Xiang, Qiuping; Xu, Jinxin; Wu, Donghai; Liu, Jinsong; Xu, Yong published the artcile< Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist>, Formula: C7H7ClO4S2, the main research area is benzimidazole derivative XY123 ROR gamma inverse agonist.

Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. Herein, we report our effort on the discovery, optimization, and evaluation of benzothiazole and benzimidazole derivatives as novel inverse agonists of RORγ. The representative compound 27h (designated as XY123) (I) potently inhibited the RORγ transcription activity with a half-maximal inhibitory concentration (IC50) value of 64 nM and showed excellent selectivity against other nuclear receptors. 27H also potently suppressed cell proliferation, colony formation, and the expression of androgen receptor (AR)-regulated genes in AR-pos. prostate cancer cell lines. In addition, 27h demonstrated good metabolic stability and a pharmacokinetic property with reasonable oral bioavailability (32.41%) and moderate half-life (t1/2 = 4.98 h). Significantly, oral administration of compound 27h achieved complete and long-lasting tumor regression in the 22Rv1 xenograft tumor model in mice. Compound 27h may serve as a new valuable lead compound for further development of drugs for the treatment of prostate cancer.

Journal of Medicinal Chemistry published new progress about Androgen receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Formula: C7H7ClO4S2.

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

Wu, Xishan; Shen, Hui; Zhang, Yan; Wang, Chao; Li, Qiu; Zhang, Cheng; Zhuang, Xiaoxi; Li, Chenchang; Shi, Yudan; Xing, Yanli; Xiang, Qiuping; Xu, Jinxin; Wu, Donghai; Liu, Jinsong; Xu, Yong published the artcile< Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist>, Formula: C7H7ClO4S2, the main research area is benzimidazole derivative XY123 ROR gamma inverse agonist.

Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. Herein, we report our effort on the discovery, optimization, and evaluation of benzothiazole and benzimidazole derivatives as novel inverse agonists of RORγ. The representative compound 27h (designated as XY123) (I) potently inhibited the RORγ transcription activity with a half-maximal inhibitory concentration (IC50) value of 64 nM and showed excellent selectivity against other nuclear receptors. 27H also potently suppressed cell proliferation, colony formation, and the expression of androgen receptor (AR)-regulated genes in AR-pos. prostate cancer cell lines. In addition, 27h demonstrated good metabolic stability and a pharmacokinetic property with reasonable oral bioavailability (32.41%) and moderate half-life (t1/2 = 4.98 h). Significantly, oral administration of compound 27h achieved complete and long-lasting tumor regression in the 22Rv1 xenograft tumor model in mice. Compound 27h may serve as a new valuable lead compound for further development of drugs for the treatment of prostate cancer.

Journal of Medicinal Chemistry published new progress about Androgen receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Formula: C7H7ClO4S2.

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

Melngaile, Renate; Sperga, Arturs; Baldridge, Kim K.; Veliks, Janis published the artcile< Diastereoselective Monofluorocyclopropanation Using Fluoromethylsulfonium Salts>, Formula: C7H7ClO4S2, the main research area is diastereoselective monofluorocyclopropanation vinyl sulfone sulfonamide; monofluorocyclopropanation fluoromethylsulfonium salt.

Diarylfluoromethylsulfonium salts, alternatives to freons or advanced fluorinated building blocks, are bench stable and easy-to-use sources of direct fluoromethylene (:CHF) transfer to alkenes. These salts enabled development of a trans-selective monofluorinated Johnson-Corey-Chaykovsky reaction with vinyl sulfones or vinyl sulfonamides to access synthetically challenging monofluorocyclopropane scaffolds. The described method offers rapid access to monofluorinated cyclopropane building blocks with further functionalization opportunities to deliver more complex synthetic targets diastereoselectively.

Organic Letters published new progress about Arenesulfonium compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Formula: C7H7ClO4S2.

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

Tang, Sheng; Li, Yu-Huan; Cheng, Xin-Yue; Li, Ying-Hong; Wang, Hui-Qiang; Kong, Lan-Ying; Zhang, Xin; Jiang, Jian-Dong; Song, Dan-Qing published the artcile< SAR evolution and discovery of benzenesulfonyl matrinanes as a novel class of potential coxsakievirus inhibitors>, Formula: C7H7ClO4S2, the main research area is benzenesulfonyl matrinane coxsakievirus inhibitor structure activity relationship; coxsackieviruse; druggability; matrinane; matrinic acid; structure–activity relationship.

Materials & methods: Fifty-one novel 12N-substituted matrinic acid derivatives were synthesized and evaluated for their anti-coxsackievirus B3 activities. Results: Structure-activity relationship studies revealed that the 11-side chain could be determinant for the selectivity index by adjusting overall lipophilicity, and 11-butane was the best one for both potency and druggability. The optimized 35d showed the broad-spectrum anti-coxsackieviruse effects, an excellent pharmacokinetics and a good safety profile. More importantly, it displayed a potential effect for the pleconaril-resistant coxsackievirus B3 as well. Its mode of action is targeting on the viral transcription and translation stage, a different mechanism from that of pleconaril. Conclusion: Thus, we considered that 35d is a promising anti-enteroviral candidate for the treatment of various diseases infected with coxsackieviruses.

Future Medicinal Chemistry published new progress about Antiviral agents. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Formula: C7H7ClO4S2.

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

Luo, Yong; Ding, Hao; Zhen, Jing-Song; Du, Xian; Xu, Xiao-Hong; Yuan, Han; Li, Yi-Hui; Qi, Wan-Ying; Liu, Bing-Zhe; Lu, Shi-Man; Xue, Can; Ding, Qiuping published the artcile< Catalyst-free arylation of sulfonamides via visible light-mediated deamination>, Synthetic Route of 5335-40-0, the main research area is diaryl sulfone preparation photochem; sulfonamide aryl boronic acid arylation deamination visible light.

A novel arylation of sulfonamides RSO2N(R1)C(O)R2 (R = 4-methylphenyl, naphthalen-2-yl, 2,3-dihydro-1-benzofuran-6-yl, etc.; R1 = Ph, Me, Bn, etc.; R2 = Ph, Me, Bn, n-pentyl, 4-cyanophenyl) with boronic acids R3B(OH)2 [R3 = 4-(methoxycarbonyl)phenyl, 4-methylnaphthalen-1-yl, 1-benzofuran-2-yl, etc.] to afford numerous diaryl sulfones RS(O)2R3 via a visible light-mediated N-S bond cleavage, rather than the typical transition-metal-catalyzed C(O)-N bond activation, is described. This methodol., which represents the first catalyst-free protocol for the sulfonylation of boronic acids, is characterized by its simple reaction conditions, good functional group tolerance and high efficiency. Several successful examples for the late-stage functionalization of diverse sulfonamides indicate the high potential utility of this method in pharmaceutical science and organic synthesis.

Chemical Science published new progress about Arylboronic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Synthetic Route of 5335-40-0.

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

Porter, John; Lumb, Simon; Franklin, Richard J.; Gascon-Simorte, Jose M.; Calmiano, Mark; Le Riche, Kelly; Lallemand, Benedicte; Keyaerts, Jean; Edwards, Helen; Maloney, Alison; Delgado, Jean; King, Lloyd; Foley, Anne; Lecomte, Fabien; Reuberson, James; Meier, Christoph; Batchelor, Mark published the artcile< Discovery of 4-azaindoles as novel inhibitors of c-Met kinase>, Reference of 5335-40-0, the main research area is azaindole preparation cMet tyrosine kinase inhibitor.

A series of 4-azaindole inhibitors of c-Met kinase, e.g. I (R1 = H, NH2, CO2H, 1-piperazinyl, etc.; R2 = PhSO2, 2-O2NC6H4SO2, benzofurazan-4-ylsulfonyl, etc.), is described. The postulated binding mode was confirmed by an X-ray crystal structure of complex of I (R1 = CONH2; R2 = 2-O2NC6H4SO2) with c-Met kinase and series optimization was performed on the basis of this structure. Future directions for series development are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about Enzyme inhibitors. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Reference of 5335-40-0.

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

Zhao, Feng; Tan, Qi; Wang, Dahan; Deng, Guo-Jun published the artcile< Metal- and solvent-free direct C-H thiolation of aromatic compounds with sulfonyl chlorides>, Electric Literature of 5335-40-0, the main research area is arene aryl sulfonyl chloride thiolation; sulfide diaryl preparation.

A simple, efficient and green method for the direct thiolation of aromatic compounds using com. available sulfonyl chlorides as the sulfur source was developed under metal- and solvent-free conditions. The C-S bond was constructed via direct C-H functionalization of diverse aromatic compounds under an oxygen atm. In this process, various diaryl sulfides were synthesized in moderate to excellent yields. This protocol shows a broad substrate scope and good functional group tolerance. Moreover, a gram-scale experiment was also conducted to prove the prospect of this method for the scale-up synthesis of diaryl sulfides. Mechanistic studies indicate that this procedure probably undergoes a radical pathway.

Green Chemistry published new progress about Aromatic compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Electric Literature of 5335-40-0.

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

Byun, Youngjoo; Vogel, Susan R.; Phipps, Andrew J.; Carnrot, Cecilia; Eriksson, Staffan; Tiwari, Rohit; Tjarks, Werner published the artcile< Synthesis and Biological Evaluation of Inhibitors of Thymidine Monophosphate Kinase from Bacillus anthracis>, Application of C7H7ClO4S2, the main research area is thymidine phosphate analog preparation inhibitor Bacillus thymidine monophosphate kinase.

Nineteen lipophilic thymidine phosphate-mimicking compounds were designed and synthesized as potential inhibitors of thymidine monophosphate kinase of Bacillus anthracis, a Gram-pos. bacterium that causes anthrax. These thymidine analogs were substituted at the 5′-position with sulfonamide-, amide-, (thio)urea-, or triazole groups, which served as lipophilic surrogates for phosphate. Three of the tested compounds produced inhibition of B. anthracis growth and/or thymidine monophosphate activity. Addnl. studies will be necessary to elucidate the potential of this type of B. anthracis thymidine monophosphate inhibitors as novel antibiotics in the treatment of anthrax.

Nucleosides, Nucleotides & Nucleic Acids published new progress about Anthrax (disease). 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Application of C7H7ClO4S2.

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

Chen, Jianfang; Zhou, Haibin; Aguilar, Angelo; Liu, Liu; Bai, Longchuan; McEachern, Donna; Yang, Chao-Yie; Meagher, Jennifer L.; Stuckey, Jeanne A.; Wang, Shaomeng published the artcile< Structure-Based Discovery of BM-957 as a Potent Small-Molecule Inhibitor of Bcl-2 and Bcl-xL Capable of Achieving Complete Tumor Regression>, COA of Formula: C7H7ClO4S2, the main research area is pyrrole carboxylic acid preparation Bcl2 BclxL inhibitor SAR.

Bcl-2 and Bcl-xL antiapoptotic proteins are attractive cancer therapeutic targets. We have previously reported the design of 4,5-diphenyl-1H-pyrrole-3-carboxylic acids as a class of potent Bcl-2/Bcl-xL inhibitors. In the present study, we report our structure-based optimization for this class of compounds based upon the crystal structure of Bcl-xL complexed with a potent lead compound Our efforts accumulated into the design of compound 30 (BM-957, I), which binds to Bcl-2 and Bcl-xL with Ki < 1 nM and has low nanomolar IC50 values in cell growth inhibition in cancer cell lines. Significantly, compound 30 achieves rapid, complete, and durable tumor regression in the H146 small-cell lung cancer xenograft model at a well-tolerated dose schedule. Journal of Medicinal Chemistry published new progress about Antitumor agents. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, COA of Formula: C7H7ClO4S2.

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