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Published on: May 9, 2025
Isothiazole derivatives as antiviral agents
Adriana Garozzo1, Christian C C Cutri, Christophe Pannecouque
1Department of Microbiological and Gynaecological Sciences, University of Catania, 95124 Catania, Italy. agar@unict.it
Antiviral Chemistry & Chemotherapy
|December 1, 2007
Summary
New isothiazole derivatives show potent antiviral activity against a range of viruses, including HIV and picornaviruses like poliovirus and rhinovirus. These compounds exhibit high selectivity indexes, indicating their potential as effective antiviral agents.
Area of Science:
- Medicinal Chemistry
- Virology
- Organic Synthesis
Background:
- Previous research identified isothiazole derivatives with activity against HIV-1 and HIV-2.
- Isothiazole compounds have demonstrated a broad spectrum of action against picornaviruses.
Purpose of the Study:
- To evaluate the antiviral activity of novel isothiazole derivatives against a panel of RNA and DNA viruses.
- To synthesize and assess a new isothiazole derivative based on previously effective compounds.
Main Methods:
- Synthesis of isothiazole derivatives, including S-[4-cyano-5-(4-OBn-phenyl)isothiazol-3-yl]-O-ethyl thiocarbonate.
- Antiviral screening against human immunodeficiency virus (HIV-1, HIV-2), poliovirus 1, Echovirus 9, rhinoviruses, Coxsackie B1, measles virus, adenovirus type 2, and herpes simplex virus type 1.
Main Results:
- Compounds showed high selectivity indexes against poliovirus 1 (SI: 223-828) and Echovirus 9 (SI: 200-334).
- The novel derivative S-[4-cyano-5-(4-OBn-phenyl)isothiazol-3-yl]-O-ethyl thiocarbonate was active against rhinoviruses (2, 39, 86, 89), Coxsackie B1, and measles virus.
- Activity was also observed against HIV-1 and HIV-2.
Conclusions:
- The newly synthesized isothiazole derivative exhibits broad-spectrum antiviral activity.
- These compounds represent promising candidates for the development of novel antiviral therapies.
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