PMID- 15457681
OWN - NLM
STAT- MEDLINE
DCOM- 20050818
LR  - 20170214
IS  - 0956-3202 (Print)
IS  - 0956-3202 (Linking)
VI  - 15
IP  - 4
DP  - 2004 Jul
TI  - Isothiazole derivatives as novel HIV replication inhibitors.
PG  - 201-5
AB  - A series of 3,4,5-trisubstituted isothiazoles has been screened against HIV-1 
      (IIIB) and HIV-2 (ROD) at sub-toxic concentrations in acutely infected MT-4 
      cells. Among the tested compounds, only 
      3-mercapto-5-phenyl-4-isothiazolecarbonitrile was found to inhibit the 
      replication of HIV-1 (IIIB) and HIV-2 (ROD) at 50% effective concentrations 
      (EC50) of 7.8 and 9.7 microg/ml, respectively. The presence of a thioalkyl chain 
      or dialkylamino function in the 3-position caused a loss of anti-HIV activity. 
      New 4-cyano-5-phenylisothiazoles with other substituents in the 3-position have 
      also been synthesized and studied as potential anti-HIV agents. Our results have 
      demonstrated that 5-phenyl-3-(4-cyano-5-phenylisothiazol-3-yl) 
      disulphanyl-4-isothiazolecarbonitrile and 
      S-(4-cyano-5-phenylisothiazol-3-yl)-O-ethyl thiocarbonate are effective against 
      both HIV-1 (IIIB) (EC50=13.6 and 15.2 microg/ml, respectively) and HIV-2 (ROD) 
      (EC50=17.4 and 13.4 microg/ml, respectively).
FAU - Cutri, Christian C C
AU  - Cutri CC
AD  - Department of Pharmaceutical Sciences, University of Catania, Catania, Italy.
FAU - Garozzo, Adriana
AU  - Garozzo A
FAU - Pannecouque, Christophe
AU  - Pannecouque C
FAU - Castro, Angelo
AU  - Castro A
FAU - Guerrera, Francesco
AU  - Guerrera F
FAU - De Clercq, Erik
AU  - De Clercq E
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Antivir Chem Chemother
JT  - Antiviral chemistry & chemotherapy
JID - 9009212
RN  - 0 
      (5-phenyl-3-(4-cyano-5-phenylisothiazol-3-yl)disulfanyl-4-isothiazolecarbonitrile)
RN  - 0 (Anti-HIV Agents)
RN  - 0 (Disulfides)
RN  - 0 (S-(4-cyano-5-phenylisothiazol-3-yl)-O-ethyl thiocarbonate)
RN  - 0 (Thiazoles)
SB  - IM
MH  - Anti-HIV Agents/chemical synthesis/*chemistry/*pharmacology
MH  - Cell Line
MH  - Disulfides
MH  - HIV-1/*drug effects/physiology
MH  - HIV-2/*drug effects/physiology
MH  - Humans
MH  - Molecular Structure
MH  - Thiazoles/chemical synthesis/*chemistry/*pharmacology
MH  - Virus Replication/*drug effects
EDAT- 2004/10/02 05:00
MHDA- 2005/08/19 09:00
CRDT- 2004/10/02 05:00
PHST- 2004/10/02 05:00 [pubmed]
PHST- 2005/08/19 09:00 [medline]
PHST- 2004/10/02 05:00 [entrez]
AID - 10.1177/095632020401500403 [doi]
PST - ppublish
SO  - Antivir Chem Chemother. 2004 Jul;15(4):201-5. doi: 10.1177/095632020401500403.