کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582604 | 981060 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents
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کلمات کلیدی
CXCR4CXC chemokine receptor type 4CCR5NNRTINRTIMultinuclear activation of a galactosidase indicatoranti-hiv agents - عوامل ضد هویNucleoside reverse transcriptase inhibitors - مهار کننده های ترانس کپسول معکوس نوکلئوزیدNon-Nucleoside Reverse Transcriptase Inhibitors - مهار کننده های ترانسپرتالس معکوس غیر هسته ایMAGI - مگی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents](/preview/png/10582604.png)
چکیده انگلیسی
3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimido[1,2-c][1,3]benzothiazin-6-imine were investigated for the development of more potent anti-HIV agents. Several different derivatives containing a 9-aryl group were designed and synthesized using Suzuki-Miyaura cross-coupling and Ullmann coupling reactions. Modification of the m-methoxyphenyl or benzo[d][1,3]dioxol-5-yl group resulted in improved anti-HIV activity. In addition, the 2,4-diazaspiro[5.5]undec-2-ene-fused benzo[e][1,3]thiazine derivatives were designed and tested for their anti-HIV activities. The most potent 9-(benzo[d][1,3]dioxol-5-yl) derivative was two-threefold more effective against several strains of HIV-1 and HIV-2 than the parent compound, PD 404182.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 21, 1 November 2012, Pages 6434-6441
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 21, 1 November 2012, Pages 6434-6441
نویسندگان
Tsukasa Mizuhara, Shinya Oishi, Hiroaki Ohno, Kazuya Shimura, Masao Matsuoka, Nobutaka Fujii,