Syntheses and in vitro biological screening of 1-aryl-10 H-[1,2,4]triazolo[3′,4′:3,4][1,2,4]triazino[5,6- b]indoles.

Autor: Upadhyay, Kuldip, Manvar, Atul, Loddo, Roberta, Colla, Paolo, Virsodiya, Vijay, Trivedi, Jalpa, Chaniyara, Ravi, Shah, Anamik
Zdroj: Medicinal Chemistry Research; Aug2013, Vol. 22 Issue 8, p3675-3686, 12p
Abstrakt: Structurally diverse 1-aryl-10 H-[1,2,4]triazolo[3′,4′:3,4][1,2,4]triazino[5,6- b]indoles 4a- v were synthesized by regiospecific heterocyclizations. The designed molecular diversity was evaluated in vitro in parallel cell-based assays for cytotoxicity of viruses multiplication supporting cell lines and antiviral activity against viruses representative of two of three genera of the Flaviviridae family. The compound library was also tested against Retrovirus (HIV-1), two Picornaviruses (CVB-2 and Sb-1), and Paramyxoviridae (VSV) representative. Among double-stranded RNA (dsRNA) viruses, Reoviridae representative (Reo-1) was tested. Two representatives of DNA virus families were also included-HSV-1 ( Herpesviridae) and VV ( Poxviridae). The compounds 4m and 4o were found cytotoxic, having CC values ranging from 4 to 30 μM. Moreover, compound 4v has exhibited significant activity (EC = 3 μM) against BVDV. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index