Progress in Rhinovirus Chemotherapy

Failure of a 3-Substituted Triazinoindole in the Prevention of Experimental Human Rhinovirus Infection

“…These compounds have no direct viricidal activity against A2 influ enza viruses, and neither do the triazinoindoles against rhinoviruses. 3-Substituted triazinoindole compounds inhibit a stage in viral synthesis and prevent the spread of infection [2]. This in vitro drug efficacy against rhinovirus was not demonstrated in the present clinical trials.…”

“…Antiviral com pounds for chemoprophylactic or therapeutic control of this infection have been sought. A group of 3-substituted triazinoindoles, analogues of isatin-/J-thiosemicarbazone, have been reported to exert broad spectrum antiviral activity in vitro [5,6] and are active against a large number of rhinovirus serotypes [7], One of these compounds showed a suggestive activity against experimental rhinovirus infection in chimpanzees [2].…”

Multistep organic synthesis leading to the formation of triazinothiazoloquinoxalines involving cost effective rea-gents

“…It was recrystalllized from ethenol as white crystalline mass m.p.>300°C[>300°C] [18] yield 80% (3).Thiazolo [5], [4-b] quinoxalin -2 -amine (3) -A mixture of 2,3 -dichloroquinoxaline (20mmol) and thiourea (20mmol) in absolute ethanol (100ml) was heated under reflex for 2hr. The reaction mixture on cooling and neutralization with anhydrous potassium carbonate solution yielded the free base which on crystallization from dimethyl formamide (DMF) furnished light yellow crystalline mass m.p.>300°C[>300°C] [19] yield 65% (4).General procedure for the synthesis of N-arylidenethiazolo [5], [4-b] quinoxalin-2-amines (4a-e). -Thiazolo [5], [4-b] quinoxalin -2 -amines (10 mmol) and an aromatic aldehydes (10mmol) in DMSO (100ml) were heated under reflux for 2h.…”

Antiviral Activity of N-Phenyl-N′-arylthiourea Derivatives against some Rhinoviruses

“…Of all substances studied only some triazi-noindoles were active in vivo, in rhinovirus infections in primates [3,15] but not in humans [21].…”

“…Several compounds have been selected recently as inhibitors of the in vitro multiplication of rhinoviruses, namely guanidine [20], HBB and other benzimidazoles [9,18,20], a thiosemicarbazone derivative [8], 3-substituted triazinoindoles [3,8,10,11,14,15,21], some pyrimidine analogues [12,13,19], 4'-hydroxy-5,6,7,8-tetramethoxyflavone [4], and aromatic sulfonic acids [2]. Of all substances studied only some triazi-noindoles were active in vivo, in rhinovirus infections in primates [3,15] but not in humans [21].…”