N ′-[4-[(Substituted imino)methyl]benzylidene]-substituted benzohydrazides: synthesis, antimicrobial, antiviral, and anticancer evaluation, and QSAR studies
Identifieur interne : 001352 ( Main/Exploration ); précédent : 001351; suivant : 001353N ′-[4-[(Substituted imino)methyl]benzylidene]-substituted benzohydrazides: synthesis, antimicrobial, antiviral, and anticancer evaluation, and QSAR studies
Auteurs : Pradeep Kumar [Inde] ; Balasubramanian Narasimhan [Inde] ; Kalavathy Ramasamy [Malaisie] ; Vasudevan Mani [Malaisie] ; Rakesh Kumar Mishra [Malaisie] ; Abu Bakar Abdul Majeed [Malaisie] ; Erik De Clercq [Belgique]Source :
- Monatshefte für Chemie - Chemical Monthly [ 0026-9247 ] ; 2013-06-01.
English descriptors
- KwdEn :
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. Graphical Abstract:
Url:
- https://api.istex.fr/ark:/67375/VQC-8Q1BSZQT-C/fulltext.pdf
- http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7087754
DOI: 10.1007/s00706-012-0877-3
Affiliations:
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<front><div type="abstract" xml:lang="en">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. Graphical Abstract:</div>
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