| 3-(5-Dimethylamino-1-naphthalenesulphonyl)-2-(3-pyridyl)thiazolidine (YHI-1) selectively inhibits human immunodeficiency virus type 1. | |
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MedLine Citation:
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PMID: 9875395 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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3-(5-Dimethylamino-1-naphthalenesulphonyl)-2-(3-pyridyl)thiazolidi ne (YHI-1), a synthetic analogue of D-cysteinolic acid isolated from sardines (Sardinops melanostictus), was found to be a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) replication in various cell cultures. YHI-1 inhibited HIV-1IIIB replication with a 50% effective concentration (EC50) of 3.35, 10.23 and 4.61 microM in MT-4 cells, peripheral blood mononuclear cells and MAGI-CCR5 cells, respectively. However, no antiviral activity was observed with non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains, such as nevirapine-resistant HIV-1HE/NEV and MKC-442-resistant HIV-1IIIB-R, or with HIV-2ROD or SIVMAC. YHI-1 failed to inhibit reverse transcriptase (RT) activity in vitro with different template-primer systems. Time-of-addition experiments, the failure to inhibit NNRTI-resistant strains and the failure to show in vitro activity against RT suggest that a metabolite of YHI-1 inside the cell acts like an NNRTI. Thus, YHI-1 seems to belong to a new class of HIV-1 inhibitor and is a good candidate for further development. |
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Authors:
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M Premanathan; R Arakaki; S Ramanan; S Jinno; M Baba; S Yamashita; H Nakashima |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Antiviral chemistry & chemotherapy Volume: 9 ISSN: 0956-3202 ISO Abbreviation: Antivir. Chem. Chemother. Publication Date: 1998 Sep |
Date Detail:
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Created Date: 1999-02-12 Completed Date: 1999-02-12 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9009212 Medline TA: Antivir Chem Chemother Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 423-30 Citation Subset: IM; X |
Affiliation:
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Department of Microbiology and Immunology, Kagoshima University Dental School, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-HIV Agents / pharmacology* Antiviral Agents / chemistry, pharmacology Cell Line Cysteine / analogs & derivatives, pharmacology Drug Resistance / genetics Fishes HIV Core Protein p24 / metabolism HIV Protease / metabolism HIV-1 / drug effects*, genetics Humans Molecular Structure Naphthalenes / pharmacology* Nevirapine / pharmacology Reverse Transcriptase Inhibitors / pharmacology Thiazoles / chemistry*, pharmacology* Thiazolidines Virus Replication / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Anti-HIV Agents; 0/Antiviral Agents; 0/HIV Core Protein p24; 0/Naphthalenes; 0/Reverse Transcriptase Inhibitors; 0/Thiazoles; 0/Thiazolidines; 0/YHI-1; 129618-40-2/Nevirapine; 16421-58-2/cysteinolic acid; 52-90-4/Cysteine; EC 3.4.23.-/HIV Protease |
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