Author/Authors :
Çikla, Pelin Marmara University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, Turkey , Küçükgüzel, S. Güniz Marmara University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, Turkey , Küçükgüzel, Ilkay Marmara University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, Turkey , Rollas, Sevim Marmara University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry, Turkey , De Clercq, Erik Katholieke Universiteit Leuven - Rega Institute for Medical Research, Belgium , Pannecouque, Christophe Katholieke Universiteit Leuven - Rega Institute for Medical Research, Belgium , Andrei, Graciela Katholieke Universiteit Leuven - Rega Institute for Medical Research, Belgium , Snoeck, Robert Katholieke Universiteit Katholieke Universiteit - Rega Institute for Medical Research, Belgium , Sahin, Fikrettin Yeditepe University - Faculty of Engineering and Architecture - Department of Genetics and Bioengineering, Turkey , Bayrak, Ömer Faruk Yeditepe University - Faculty of Engineering and Architecture - Department of Genetics and Bioengineering, Turkey
Abstract :
A series of novel 1-[4-[[2-[(4-substituted phenyl)methylene]hydrazino]carbonyl]p henyl]-3-substituted thiourea derivatives have been synthesized by the addition of substituted aryl isothiocyanates to 4-amino-N’-[(4-substituted phenyl) methylene] benzohydrazide, which was prepared by condensation of 4-aminobenzoic acid hydrazide with 4-fluorobenzaldehyde or 4-(trifluoromethyl)benzaldeyde. All synthesized compounds were evaluated in vitro against HIV-1 (IIIB) and HIV-2 (ROD) strains in MT-4 cells, as well as other selected viruses such as HSV-1, HSV-2, Coxsackie virus B4, Sindbis virus, human cytomegalovirus, and varicella-zoster virus using HeLa, Vero, or HEL cell cultures. Antimycobacterial activity against Mycobacterium tuberculosis H37 Rv was also evaluated. The anticancer activity and cytotoxicity screening of the synthesized compounds were determined on A 549 and L 929 cell lines.
NaturalLanguageKeyword :
Hydrazones , Thioureas , Antiviral activity , Anticancer activity , Mycobacterium tuberculosis H37Rv