دورية أكاديمية
Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB 1 R) Receptor with Reduced Lipophilicity.
العنوان: | Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CB |
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المؤلفون: | Iyer MR; Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Cinar R; Section on Fibrotic Disorders, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Wood CM; Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Zawatsky CN; Section on Fibrotic Disorders, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Coffey NJ; Laboratory of Physiologic Studies, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Kim KA; Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Liu Z; Section on Fibrotic Disorders, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Katz A; Laboratory of Physiologic Studies, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Abdalla J; Laboratory of Physiologic Studies, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, Maryland 20852, United States., Hassan SA; Bioinformatics and Computational Biosciences Branch, National Institute of Allergy and Infectious Diseases, NIH, Bethesda, Maryland 20892, United States., Lee YS; Bioinformatics and Computational Biosciences Branch, National Institute of Allergy and Infectious Diseases, NIH, Bethesda, Maryland 20892, United States. |
المصدر: | Journal of medicinal chemistry [J Med Chem] 2022 Feb 10; Vol. 65 (3), pp. 2374-2387. Date of Electronic Publication: 2022 Jan 27. |
نوع المنشور: | Journal Article; Research Support, N.I.H., Intramural |
اللغة: | English |
بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
أسماء مطبوعة: | Publication: Washington Dc : American Chemical Society Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- |
مواضيع طبية MeSH: | Anti-Obesity Agents/*therapeutic use , Cannabinoid Receptor Antagonists/*therapeutic use , Obesity/*drug therapy , Pyrazoles/*therapeutic use , Receptor, Cannabinoid, CB1/*metabolism, Animals ; Anti-Obesity Agents/chemical synthesis ; Anti-Obesity Agents/metabolism ; Body Weight/drug effects ; Brain/metabolism ; Cannabinoid Receptor Antagonists/chemical synthesis ; Cannabinoid Receptor Antagonists/metabolism ; Diet, High-Fat ; Drug Inverse Agonism ; Hydrophobic and Hydrophilic Interactions ; Male ; Mice, Inbred C57BL ; Molecular Structure ; Pyrazoles/chemical synthesis ; Pyrazoles/metabolism ; Stereoisomerism ; Structure-Activity Relationship ; Mice |
مستخلص: | In the present report, we describe the synthesis and structure-activity relationships of novel "four-arm" dihydropyrazoline compounds designed as peripherally restricted antagonists of cannabinoid-1 receptor (CB |
المشرفين على المادة: | 0 (Anti-Obesity Agents) 0 (Cannabinoid Receptor Antagonists) 0 (Pyrazoles) 0 (Receptor, Cannabinoid, CB1) |
تواريخ الأحداث: | Date Created: 20220127 Date Completed: 20220218 Latest Revision: 20240226 |
رمز التحديث: | 20240226 |
DOI: | 10.1021/acs.jmedchem.1c01836 |
PMID: | 35084860 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1520-4804 |
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DOI: | 10.1021/acs.jmedchem.1c01836 |