Marmara Pharmaceutical Journal 2010 , Vol 14 , Issue 1
Synthesis and evaluation of antiviral, antitubercular and anticancer activities of some novel thioureas derived from 4-aminobenzohydrazide hydrazones
Pelin Çıkla1, Ş. Güniz Küçükgüzel1, İlkay Küçükgüzel1, Sevim Rollas1, Erik De Clercq2, Christophe Pannecouque2, Graciela Andrei2, Robert Snoeck2, Fikrettin Şahin3, Ömer Faruk Bayrak3
1Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, İstanbul, Türkiye
2Katholieke Universiteit Leuven, Rega Institute for Medical Research, Leuven, Belçika
3Yeditepe University, Faculty of Engineering and Architecture, Genetics and Bioengineering Department, İstanbul, Türkiye
DOI : 10.12991/201014460 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. Keywords : Hydrazones, Thioureas, Antiviral activity, Anticancer activity, Mycobacterium tuberculosis H37Rv