Synthesis, characterization, antimicrobial activity and structure-activity relationships of new aryldisulfonamides

Alyar S., KARACAN N.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.24, sa.4, ss.986-992, 2009 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 24 Sayı: 4
  • Basım Tarihi: 2009
  • Doi Numarası: 10.1080/14756360802561220
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.986-992
  • Anahtar Kelimeler: Antimicrobial activity, sulfonamides, structure-activity relationship, CARBONYLS M(CO)(6) M, METAL-CARBONYLS, PHOTOCHEMICAL-REACTIONS, ANTIBACTERIAL ACTIVITY, POTENTIAL ANTICANCER, RE(CO)(5)BR, MN(CO)(3)CP, MO, METHANESULFONYLHYDRAZONE, DERIVATIVES
  • Gazi Üniversitesi Adresli: Evet

Özet

A series of aromatic disulfonamide (1-8) derivatives and 4-methylbenzenesulfonyl hydrazide (9) were synthesized and characterized. All compounds were evaluated in vitro for their antimicrobial activity against Staphylococcus aureus ATCC 25953, Bacillus cereus ATCC 6633, Bacillus magaterium RSKK 5117, Escherichia coli ATCC 11230, Salmonella enterititis ATCC 13076 by microdilution and disc diffusion methods. Antimicrobial activity of the aromatic disulfonamides decreased as the length of the carbon chain increased. An analysis of the structure-activity relationship (SAR) along with computational studies showed that the most active compound (9) possessed low lipophilicity (AlogP=0.59) and high solubility (logS = -1.33).