Affiliations 

  • 1 1Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001 India
  • 2 2Collaborative Drug Discovery Research Group, Faculty of Pharmacy, Campus Puncak Alam, Universiti Teknologi MARA (UiTM), Bandar Puncak Alam, 42300 Shan Alam, Selangor Malaysia
  • 3 3Brain Research Laboratory, Faculty of Pharmacy, Campus Puncak Alam, Universiti Teknologi MARA (UiTM), Bandar Puncak Alam, 42300 Shan Alam, Selangor Malaysia
  • 4 4Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Minderbroedersstraat 10, 3000 Louvain, Belgium
Monatsh Chem, 2013;144(6):825-849.
PMID: 32214480 DOI: 10.1007/s00706-012-0877-3

Abstract

ABSTRACT: A variety of N'-[4-[(substituted imino)methyl]benzylidene]-substituted benzohydrazides have been synthesized and evaluated for antimicrobial and anticancer potential. Results from testing of antimicrobial activity indicated the most potent antimicrobial agents had pMIC am = 1.51. The synthesized compounds were bacteriostatic and fungistatic in action. Results from evaluation of antiviral activity indicated that none of the synthesized hydrazide derivatives inhibited viral replication at sub-toxic concentrations. Results from anti-HIV screening against HIV-2 strain ROD indicated that one compound was more potent (IC 50 ≥ 1 μg/cm3) than the standard drug nevirapine (IC 50 ≥ 4 μg/cm3) and another was equipotent (IC 50 ≥ 4 μg/cm3). The most effective anticancer agent against both HCT116 and MCF7 cancer cell lines had IC 50 = 19 and 18 μg/cm3, respectively. QSAR analysis indicated the importance of Wiener index (W) and energy of the lowest unoccupied molecular orbital (LUMO) in describing the antimicrobial activity of the synthesized compounds.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.