title: Synthesis and biological evaluation of pyrazoline derivatives bearing an indole moiety as new antimicrobial agents.
abstract: 1-(p-Methylphenyl)-3,5-diaryl-2-pyrazoline derivatives (2a-f) were synthesized via the treatment of 1-(1H-indol-3-yl)-3-aryl-2-propen-1-ones (1a-f) with p-methylphenylhydrazine hydrochloride in hot acetic acid. The structures of these compounds were elucidated by IR, ¹H NMR, and mass spectral data and elemental analysis. These compounds were investigated for their antimicrobial activity. Brine-Shrimp lethality assay was carried out to determine the toxicity of the compounds. Compound 2e, which is the pyrazoline derivative bearing the 2,5-dichlorophenyl moiety, can be identified as the most promising agent against Klebsiella pneumoniae (ATCC 13883) and Candida glabrata (ATCC 36583) due to its inhibitory effects on K. pneumoniae and C. glabrata with a MIC value of 100 µg/mL as a non-toxic agent (LC₅₀ > 1000 µg/mL).
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskişehir, Turkey. ahmeto@anadolu.edu.tr
authors.forename: Ahmet
authors.initials: A
authors.lastname: Özdemir
authors.forename: Mehlika Dilek
authors.initials: MD
authors.lastname: Altintop
authors.forename: Zafer Asim
authors.initials: ZA
authors.lastname: Kaplancıklı
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.forename: Hülya
authors.initials: H
authors.lastname: Karaca
authors.forename: Yağmur
authors.initials: Y
authors.lastname: Tunalı
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D041221:Candida glabrata / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007711:Klebsiella pneumoniae / Q000187:drug effects; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018675:Toxicity Tests / Q000379:methods
chemical_list: D000890:Anti-Infective Agents; D007211:Indoles; D011720:Pyrazoles