کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10585215 | 981364 | 2012 | 16 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Weight loss effects of quaternary salts of 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles; structure-activity relationships
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کلمات کلیدی
dimethylacetamideN-ethyl-N′-(3-dimethylaminopropyl)carbodiimide hydrochloridebenzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphatePyBOPAIBNNMP4-dimethylaminopyridineDMAPN-MethylpyrrolidoneDMAcamphorsulfonic acid - اسید کافئورولفونیکCSA - ایالات مؤتلفهٔ آمریکاintra-peritoneal - داخل صفاقیdiisopropylethylamine - دی ایزوپروپیلایتیلامینCbi - سیبیSAR study - مطالعه SARDIPEA - نخودWeight loss - کاهش وزن
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Weight loss effects of quaternary salts of 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles; structure-activity relationships Weight loss effects of quaternary salts of 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles; structure-activity relationships](/preview/png/10585215.png)
چکیده انگلیسی
Quaternary salt analogues based on the DNA minor groove binder and adenine N3 alkylating agent 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indole (aminoCBI) show remarkable effects on the body weight of mice (a long-term failure to gain weight relative to matched controls with no loss of appetite or perceptible deterioration in health) following administration of a single (non-toxic) dose between about 0.5-5 μmol/kg. The nature of the quaternizing group was not important, but a related hydroxyCBI analogue was much less effective. Compounds where the chloro group was replaced by a hydrogen or hydroxy group (thus abrogating DNA alkylating capability) showed no weight control activity. It is speculated, based on other studies, that the marked long-term weight control effect is due to inhibition of bile flow into the intestine and reduced absorption of triglycerides, together with accelerated cell death in spleen and white adipose tissues due to drug accumulation there. This class of compound may serve as interesting tools for further study of these phenomena.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 2, 15 January 2012, Pages 734-749
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 2, 15 January 2012, Pages 734-749
نویسندگان
Moana Tercel, Ralph J. Stevenson, Guo-Liang Lu, Stephen M. Stribbling, William R. Wilson, Michele A. Tatnell, Rebecca N. Marnane, Kathleen G. Mountjoy, William A. Denny,