Picornaviruses, particularly human rhinoviruses cause approximately one half of all cases of respiratory tract infections (common colds). No effective anti-rhinoviruses therapy is currently available although during the past decade some antiviral active compounds are reported like disoxaril and pirodavir. (1,2) The published information about the structure/activity relationships of HRV indicates that the most active compounds have general formula 1, wherein the group designed as Het can be a wide range of heterocycles and the central flexible group R and the phenyl ring substituents can be variable. The published information about the structure/activity relationships of HRV indicates that the most active compounds have general formula 1, wherein the group designed as Het can be a wide range of heterocycles and the central flexible group R and the phenyl ring substituents can be variable. The cytotoxicity of these compounds was evaluated by measuring the effect produced on cell morphology and cell growth in vitro. The antiviral activity was studied on Human Rhinoviruses 14 (group A) and 39 (group B). The results indicate that compounds 8 (Ar = p-COCH3-C6H4), 9 (Ar = 3,4-methylendioxy-C6H3) and 10 (n = 1,R = p-COCH3) were highly active against HRV14, whilst 7 (Ar = p-CN-C6H4), 8 and 10 were able to inhibit HRV39 at non-toxic doses.
Synthesis of New Compounds with Promising Antiviral Properties against Group A and B Human Rhinoviruses
BERNARD, ANGELA MARIA;CABIDDU, MARIA GRAZIA;POMPEI, RAFFAELLO
2013-01-01
Abstract
Picornaviruses, particularly human rhinoviruses cause approximately one half of all cases of respiratory tract infections (common colds). No effective anti-rhinoviruses therapy is currently available although during the past decade some antiviral active compounds are reported like disoxaril and pirodavir. (1,2) The published information about the structure/activity relationships of HRV indicates that the most active compounds have general formula 1, wherein the group designed as Het can be a wide range of heterocycles and the central flexible group R and the phenyl ring substituents can be variable. The published information about the structure/activity relationships of HRV indicates that the most active compounds have general formula 1, wherein the group designed as Het can be a wide range of heterocycles and the central flexible group R and the phenyl ring substituents can be variable. The cytotoxicity of these compounds was evaluated by measuring the effect produced on cell morphology and cell growth in vitro. The antiviral activity was studied on Human Rhinoviruses 14 (group A) and 39 (group B). The results indicate that compounds 8 (Ar = p-COCH3-C6H4), 9 (Ar = 3,4-methylendioxy-C6H3) and 10 (n = 1,R = p-COCH3) were highly active against HRV14, whilst 7 (Ar = p-CN-C6H4), 8 and 10 were able to inhibit HRV39 at non-toxic doses.
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