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    
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.
M Premanathan; R Arakaki; S Ramanan; S Jinno; M Baba; S Yamashita; H Nakashima
Related Documents :
21925045 - Empiric antimicrobial therapy and infectious diarrhea. do we need local guidelines?
18753355 - Molecular typing of treponema pallidum clinical strains from lisbon, portugal.
9258355 - Synthesis and in vitro activity of long-chain 5'-o-[(alkoxycarbonyl)phosphinyl]-3'-azid...
18426335 - Molecular epidemiology and divergence of hiv type 1 protease codon 35 inserted strains ...
16879935 - Comparative evaluation of molecular assays for the identification of intestinal spiroch...
14574105 - Genetic determination of ploidy level in xanthophyllomyces dendrorhous.
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    
Department of Microbiology and Immunology, Kagoshima University Dental School, Japan.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Anti-HIV Agents / pharmacology*
Antiviral Agents / chemistry,  pharmacology
Cell Line
Cysteine / analogs & derivatives,  pharmacology
Drug Resistance / genetics
HIV Core Protein p24 / metabolism
HIV Protease / metabolism
HIV-1 / drug effects*,  genetics
Molecular Structure
Naphthalenes / pharmacology*
Nevirapine / pharmacology
Reverse Transcriptase Inhibitors / pharmacology
Thiazoles / chemistry*,  pharmacology*
Virus Replication / drug effects
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

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhib...
Next Document:  Synthesis, structure and in vitro anti-human immunodeficiency virus activity of novel 3-methyl-1H,3H...