Document Detail


3-(5-Dimethylamino-1-naphthalenesulphonyl)-2-(3-pyridyl)thiazolidine (YHI-1) selectively inhibits human immunodeficiency virus type 1.
MedLine Citation:
PMID:  9875395     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
M Premanathan; R Arakaki; S Ramanan; S Jinno; M Baba; S Yamashita; H Nakashima
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Antiviral chemistry & chemotherapy     Volume:  9     ISSN:  0956-3202     ISO Abbreviation:  Antivir. Chem. Chemother.     Publication Date:  1998 Sep 
Date Detail:
Created Date:  1999-02-12     Completed Date:  1999-02-12     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9009212     Medline TA:  Antivir Chem Chemother     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  423-30     Citation Subset:  IM; X    
Affiliation:
Department of Microbiology and Immunology, Kagoshima University Dental School, Japan.
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MeSH Terms
Descriptor/Qualifier:
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:
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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