title: Characterization and biological studies of bis- and tera-acetyl derivatives of hydrocarbon-bridged diamines-I.
abstract: A systematic study of the pharmaceutically important, double ended, chelating agents of the types CH(3)CONH(CH(2))nNHCOCH(3) and (CH(3)CO)(2)N(CH(2))n N(COCH(3))(2), where n= 2, 3, 4, 5 and 6, prepared by the bis- and tetra-acetylation of the corresponding diamino-polymethylenes, have been carried out. Bis- and tertra-acetyl derivatives have been characterized by their elemental analysis and the FTIR spectra, Mass spectra and H-NMR spectra of these compounds have been reported to establish their structures. In the present work, FTIR spectra have been found an excellent means for distinguishing the bis-acetyl derivatives from their tetra-acetyl counterparts. The structures of these bis- and tetra-acetyl compounds have further been established by their H-NMR and Mass Spectra. The selective pharmacological screening of the derivatives was carried out according to the standard procedures. The compounds were screened for their antibacterial and antifungal activities and it was found that majority of these compounds did not possess any remarkable activity. Only the compound BA1,2-DAE, showed significant antifungal activity against Microsporum canis (80%).
authors.affiliation: Department of Pharmacy, University of Balochistan, Quetta, Pakistan. naheed_haque@hotmail.com
authors.forename: Naheed
authors.initials: N
authors.lastname: Haque
authors.forename: Izhar
authors.initials: I
authors.lastname: Hussain
mesh_terms: D000107:Acetylation; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology; D002614:Chelating Agents / Q000737:chemistry* / Q000494:pharmacology*; D003959:Diamines / Q000737:chemistry* / Q000494:pharmacology*; D006838:Hydrocarbons / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D008864:Microsporum / Q000187:drug effects / Q000254:growth & development; D015394:Molecular Structure; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D002614:Chelating Agents; D003959:Diamines; D006838:Hydrocarbons