title: Synthesis of new compounds with promising antiviral properties against group A and B Human Rhinoviruses.
abstract: The human common cold, which is a benign disease caused by the Rhinoviruses, generally receives palliative symptomatic treatments, since no specific therapy against any of these viruses currently exists. In this work, some original synthetic compounds were produced and tested, in order to find non-toxic substances with an improved protection index (PI) for infected cells, as compared to reference drugs such as Pirodavir. We designed a series of novel molecules with a double oxygen in the central hydrocarbon chain and some modifications of the lateral methylisoxazole and propoxybenzoate moieties of lead compound 6602 (ethyl 4-{3-[2-(3-methyl-1,2-isoxazol-5-yl)ethoxy]propoxy}benzoate). It was found that most of these substances were actually less toxic than Pirodavir; in addition, the new molecule indicated as 8c was more than 30 times less toxic than Pirodavir, about twice as active on the group A strain of Rhinovirus HRV14, and even four times more effective on the group B strain HRV39, as compared to Pirodavir's PI.
authors: Dipartimento di Scienze Chimiche e Geologiche, Università di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554, Bivio per Sestu, I-09042 Monserrato (CA), Italy.
authors: Angela M
authors: AM
authors: Bernard
authors: Dipartimento di Scienze Chimiche e Geologiche, Università di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554, Bivio per Sestu, I-09042 Monserrato (CA), Italy. Electronic address: mgcabidd@unica.it.
authors: Maria G
authors: MG
authors: Cabiddu
authors: Dipartimento di Scienze Chimiche e Geologiche, Università di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554, Bivio per Sestu, I-09042 Monserrato (CA), Italy.
authors: Stefania
authors: S
authors: De Montis
authors: Dipartimento di Scienze Chimiche e Geologiche, Università di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554, Bivio per Sestu, I-09042 Monserrato (CA), Italy.
authors: Roberto
authors: R
authors: Mura
authors: Dipartimento di Scienze Biomediche, Sezione di Microbiologia e Virologia, Università di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554, Bivio per Sestu, I-09042 Monserrato (CA), Italy. Electronic address: rpompei@unica.it.
authors: Raffaello
authors: R
authors: Pompei
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D019817:Benzoic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D011724:Pyridazines / Q000737:chemistry* / Q000494:pharmacology*; D012229:Rhinovirus / Q000187:drug effects*; D012703:Serotyping; D013329:Structure-Activity Relationship
chemical_list: C000600871:1-(4-(3-((2-ethoxy-1,3-benzoxazol-6-yl)oxy)propoxy)phenyl)ethanone; D000998:Antiviral Agents; D001583:Benzoxazoles; D010880:Piperidines; D011724:Pyridazines; D019817:Benzoic Acid; C074589:pirodavir
keywords: Antivirals; Cell receptors; Rhinoviruses