title: New hydroxamic acid derivatives of fluoroquinolones: synthesis and evaluation of antibacterial and anticancer properties.
abstract: A series of new hydroxamic acid derivatives (6a-f) at C-3 position of fluoroquinolones were designed and synthesized through multistep synthesis. The design concept involved replacement of the 3-carboxylic acid in fluoquinolones with hydroxamic acid as an acid mimicking group. The synthetic work employed in this work provides a good example for the synthesis of pure hydroxamic acid based fluoroquinolones. The synthesized compounds were characterized by (1)H-NMR, electrospray ionization (ESI)-MS and IR. The new compounds were tested for their in vitro antimicrobial and anti-proliferative activity. Out of the six derivatives, compound 6e exhibited moderate antibacterial activity by inhibiting the growth of Escherichia coli and Klebsiella pneumoniae (MIC: 4.00-8.00 µg/mL). Compounds 6b and 6f displayed good growth inhibition against A549 Lung adenocarcinoma and HCT-116 Colon carcinoma cell lines.
authors.affiliation: Anthem Biosciences Pvt. Ltd.
authors.forename: Gavara Govinda
authors.initials: GG
authors.lastname: Rajulu
authors.forename: Halehatty Seephya
authors.initials: HS
authors.lastname: Bhojya Naik
authors.forename: Abhilash
authors.initials: A
authors.lastname: Viswanadhan
authors.forename: Jayaraman
authors.initials: J
authors.lastname: Thiruvengadam
authors.forename: Kondodiyil
authors.initials: K
authors.lastname: Rajesh
authors.forename: Sambasivam
authors.initials: S
authors.lastname: Ganesh
authors.forename: Hiriyan
authors.initials: H
authors.lastname: Jagadheshan
authors.forename: Poonimangadu Koppolu
authors.initials: PK
authors.lastname: Kesavan
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D004927:Escherichia coli Infections / Q000188:drug therapy; D024841:Fluoroquinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007710:Klebsiella Infections / Q000188:drug therapy; D007711:Klebsiella pneumoniae / Q000187:drug effects / Q000254:growth & development; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D024841:Fluoroquinolones; D006877:Hydroxamic Acids