A study of 3-substituted benzylidene-1,3-dihydro-indoline derivatives as antimicrobial and antiviral agents.
3-Substituted benzylidene-1,3-dihydro-indoline derivatives were tested for their in vitro antibacterial activity against the Gram-negative bacteria Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, and the Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus, and for their their in vitro antifungal activity against Candida krusei and Candida albicans. The minimum inhibitory concentration (MIC) values were determined by the 2-fold serial dilution technique in Mueller Hinton broth and Sabouraud dextrose agar using antibacterial and antifungal assays, respectively. For comparison of the antimicrobial activity, rifampicin, ampicillin trihydrate, gentamicin sulfate, and ofloxacin were used as reference antibacterial agents, and fluconazole and amphotericin B were employed as reference antifungal agents. The most active compound 10 showed notable inhibition against Bacillus subtilis, Staphylococcus aureus, and Candida krusei. Compounds 1 and 6 were found slightly effective against Klebsiella pneumoniae and Escherichia coli. In addition, compounds 13 and 14 showed inhibition against Bacillus subtilis and Staphylococcus aureus. Indole derivatives were also tested in vitro for replication of the HepAD38 cell line and compared with lamivudine (3TC, L-2',3'-dideoxy-3'-thiacytidine). The IC50 values of the compounds were found to be >1000 microM against HBV except for compound 13 which exhibited activity with an IC50 value of 500 microM.
Olgen
Süreyya
S
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey. olgen@pharmacy.ankara.edu.tr
Ozkan
Semiha
S
D000890:Anti-Infective Agents / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology*; D001597:Benzylidene Compounds / Q000737:chemistry / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects; D020008:Delavirdine / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D007211:Indoles / Q000494:pharmacology*; D019259:Lamivudine / Q000494:pharmacology; D008826:Microbial Sensitivity Tests
D000890:Anti-Infective Agents; D000998:Antiviral Agents; D001597:Benzylidene Compounds; D007211:Indoles; D019259:Lamivudine; C057812:indoline; D020008:Delavirdine