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Start Over Author "Ren, Feng" Journal journal of medicinal chemistry
10 results on '"Ren, Feng"'

6. Positional Isomeric Effects on the Optical Properties, Multivalent Glycosidase Inhibition Effect, and Hypoglycemic Effect of Perylene Bisimide–deoxynojirimycin Conjugates

Author

Ke-Rang Wang, Hong-Xin Zhang, Xiao-Liu Li, Ren-Feng Li, Li-Yue Xu, Hui-Yan Zhang, Si-Bing Chen, Zhi-Ran Cao, Jian-Xing Yang, Jing Liu, and Guo-Min Ai

Subjects
Blood Glucose, Glycoside Hydrolases, Stereochemistry, Binding energy, Molecular Conformation, Administration, Oral, Conjugated system, Imides, Mice, chemistry.chemical_compound, Isomerism, Drug Discovery, Mole, Animals, Hypoglycemic Agents, Glycoside hydrolase, Perylene, Inhibitory effect, Glucosamine, Binding Sites, Chemistry, Hydrogen bond, Hydrogen Bonding, Molecular Docking Simulation, Kinetics, Thermodynamics, Molecular Medicine, Protein Binding, Conjugate
Abstract

Although multivalent glycosidase inhibitors have shown enhanced glycosidase inhibition activities, further applications and research directions need to be developed in the future. In this paper, two positional isomeric perylene bisimide derivatives (PBI-4DNJ-1 and PBI-4DNJ-2) with 1-deoxynojirimycin conjugated were synthesized. Furthermore, PBI-4DNJ-1 and PBI-4DNJ-2 showed positional isomeric effects on the optical properties, self-assembly behaviors, glycosidase inhibition activities, and hypoglycemic effects. Importantly, PBI-4DNJ-1 exhibited potent hypoglycemic effects in mice with 41.33 ± 2.84 and 37.45 ± 3.94% decreases in blood glucose at 15 and 30 min, respectively. The molecular docking results showed that the active fragment of PBI-4DNJ-1 has the highest binding energy (9.649 kcal/mol) and the highest total hydrogen bond energy (62.83 kJ/mol), which were related to the positional isomeric effect on the hypoglycemic effect in mice. This work introduced a new means to develop antihyperglycemic agents in the field of multivalent glycomimetics.

Published
2021

7. Positional Isomeric Effects on the Optical Properties, Multivalent Glycosidase Inhibition Effect, and Hypoglycemic Effect of Perylene Bisimide–deoxynojirimycin Conjugates

Author

Li, Ren-Feng, primary, Yang, Jian-Xing, additional, Liu, Jing, additional, Ai, Guo-Min, additional, Zhang, Hui-Yan, additional, Xu, Li-Yue, additional, Chen, Si-Bing, additional, Zhang, Hong-Xin, additional, Li, Xiao-Liu, additional, Cao, Zhi-Ran, additional, and Wang, Ke-Rang, additional

Published
2021
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8. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists

Author

Lu, Hongfu, primary, Yang, Ting, additional, Xu, Zhongmiao, additional, Lin, Xichen, additional, Ding, Qian, additional, Zhang, Yueting, additional, Cai, Xin, additional, Dong, Kelly, additional, Gong, Sophie, additional, Zhang, Wei, additional, Patel, Metul, additional, Copley, Royston C. B., additional, Xiang, Jianing, additional, Guan, Xiaoming, additional, Wren, Paul, additional, and Ren, Feng, additional

Published
2018
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9. Discovery of Novel 1,2,4-Thiadiazole Derivatives as Potent, Orally Active Agonists of Sphingosine 1-Phosphate Receptor Subtype 1 (S1P1)

Author

Ren, Feng, primary, Deng, Guanghui, additional, Wang, Hailong, additional, Luan, Linbo, additional, Meng, Qinghua, additional, Xu, Qiongfeng, additional, Xu, Heng, additional, Xu, Xuesong, additional, Zhang, Haibo, additional, Zhao, Baowei, additional, Li, Chengyong, additional, Guo, Taylor B., additional, Yang, Jiansong, additional, Zhang, Wei, additional, Zhao, Yonggang, additional, Jia, Qiantao, additional, Lu, Hongtao, additional, Xiang, Jia-Ning, additional, Elliott, John D., additional, and Lin, Xichen, additional

Published
2012
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10. Discovery of Novel 1,2,4-ThiadiazoleDerivatives asPotent, Orally Active Agonists of Sphingosine 1-Phosphate ReceptorSubtype 1 (S1P1).

Author

Ren, Feng, Deng, Guanghui, Wang, Hailong, Luan, Linbo, Meng, Qinghua, Xu, Qiongfeng, Xu, Heng, Xu, Xuesong, Zhang, Haibo, Zhao, Baowei, Li, Chengyong, Guo, Taylor B., Yang, Jiansong, Zhang, Wei, Zhao, Yonggang, Jia, Qiantao, Lu, Hongtao, Xiang, Jia-Ning, Elliott, John D., and Lin, Xichen

Subjects
*PHARMACEUTICAL research, *THIADIAZOLES, *SPHINGOSINE-1-phosphate, *DRUG synergism, *STRUCTURE-activity relationships, *LYMPHOPENIA, *PHARMACOKINETICS, *LABORATORY rodents
Abstract

A novel series of 1,2,4-thiadiazole compounds was discoveredasselective S1P1agonists. The extensive structure–activityrelationship studies for these analogues were reported. Among them, 17gwas identified to show high in vitro potency with reasonablefree unbound fraction in plasma (Fu>0.5%), good brain penetration (BBR > 0.5), and desirable pharmacokineticproperties in mouse and rat. Oral administration of 1 mg/kg 17gresulted in significant peripheral lymphocytes reductionat 4 h after dose and rapid lymphocytes recovery at 24 h. 17gshowed a transient lymphopenia profile in the repeated dose studyin mouse. In addition, 17galso demonstrated efficacycomparable to that of FTY720 (1) in the mouse EAE modelof MS. [ABSTRACT FROM AUTHOR]

Published
2012
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