title: Semisynthesis and antimicrobial activity of novel guttiferone-A derivatives.
abstract: Six derivatives of guttiferone-A (LFQM-79, 80, 81, 82, 113 and 114) were synthesized and evaluated for their antimicrobial activity against the opportunistic or pathogenic fungi Candida albicans (ATCC 09548), Candida glabrata (ATCC 90030), Candida krusei (ATCC 6258), Candida parapsilosis (ATCC 69548), Candida tropicalis (ATCC 750), Cryptococcus neoformans (ATCC 90012), Trichophyton tonsurans, Microsporum gypseum and also against the opportunistic and pathogenic Gram-positive bacteria Staphylococcus aureus (ATCC 6538), Staphylococcus epidermidis (ATCC 12228), Bacillus cereus (ATCC 11778) and Gram-negative Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 9027), Salmonella typhimurium (ATCC 14028), Proteus mirabilis (ATCC 25933). The antimicrobial activities of derivatives were compared with guttiferone-A and they presented to be more potent than the original molecule and sometimes greater than standard drugs established in therapeutics. The current study showed that derivatives of guttiferone-A possess potent antimicrobial activity and are relatively non-cytotoxic, which reveal these new molecules as promising new drug prototype candidates, with innovative structural pattern.
authors.affiliation: Laboratory of Phytochemistry and Medicinal Chemistry, Institute of Chemistry, Federal University of Alfenas, 37130-000 Alfenas, MG, Brazil.
authors.forename: Kris S T
authors.initials: KS
authors.lastname: Dias
authors.forename: Jaqueline P
authors.initials: JP
authors.lastname: Januário
authors.forename: Jéssica Lopes
authors.initials: JL
authors.lastname: D' Dego
authors.forename: Amanda L T
authors.initials: AL
authors.lastname: Dias
authors.forename: Marcelo H
authors.initials: MH
authors.lastname: dos Santos
authors.forename: Ihosvany
authors.initials: I
authors.lastname: Camps
authors.forename: Luiz Felipe L
authors.initials: LF
authors.lastname: Coelho
authors.forename: Claudio
authors.initials: C
authors.lastname: Viegas
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000254:growth & development; D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001577:Benzophenones; C558133:guttiferone A