In Vitro Antimicrobial Activities of 6-Substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstitutedbenzal/acetophenone) Hydrazone Derivatives

被引:2
作者
Abiha, Gul Bayram [1 ]
Bahar, Leyla [1 ]
Utku, Semra [1 ]
机构
[1] Mersin Univ, Mersin, Turkey
来源
REVISTA ROMANA DE MEDICINA DE LABORATOR | 2018年 / 26卷 / 02期
关键词
antimicrobial; chemotherapeutic; microdilution; 3(2H)-pyridazinone; RESISTANCE; ANTIFUNGAL; ANTIBACTERIAL; INFECTIONS; CANDIDA; SUSCEPTIBILITY; PYRIDAZINONE; EPIDEMIOLOGY;
D O I
10.2478/rrlm-2018-0017
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
Aim: In vitro antibacterial activity of 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstitutedbenzal/acetophenone) hydrazone derivatives were tested in common species causing hospital-acquired infections. Material and Method: Antimicrobial activities of the compounds were performed by determining minimum inhibitory concentration (MIC) value against four Gram-positive, five Gram-negative and four Candida species fungi. Modified serial microdilution method was carried out. Reference strains of American Type Culture Collection (ATCC) were used. Results: In general, eleven compounds exhibited considerable activity. Comparatively, compound 3 exhibited strong activity against Enterobacter hormaechei and 5, 11 were the most active against Acinetobacter baumannii at 31.25 mu g/mL. Compounds 1,2,3,4,8 and 10 were found to be as active as positive control ampicillin trihidrate against Stenotrophomonas maltophilia. On the other hand, compounds 1,2,3,4,7,8,9,10 and 11 showed strong antifungal activitiy as much as fluconazole against Candida tropicalis. Compound 1 was mostly active against Candida albicans, Candida glabrata, Candida parapsilosis and Candida tropicalis. It was also revealed that the antifungal activity of compounds 1, 6, 7, 8 and 9 were higher than the others. Compound 1 and 8 exhibited the best activity against Candida glabrata and Candida parapsilosis respectively. Conclusions: All tested compounds showed better activity against Gram-negative bacteria and yeast than Gram-positive bacteria. These compounds may be considered as alternative antimicrobial agents in the treatment of multiple drug resistant Gram-negative, Gram-positive bacteria and fungal pathogens. Especially, we suggested that Compound 1 and 8 might be a promising candidate of new antifungal agents.
引用
收藏
页码:231 / 241
页数:11
相关论文
共 30 条
  • [1] Antibacterial and antifungal activities of new pyrazolo[3,4-d]pyridazin derivatives
    Akbas, E
    Berber, I
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2005, 40 (04) : 401 - 405
  • [2] Epidemiology of antimicrobial resistance in bloodstream infections
    Akova, Murat
    [J]. VIRULENCE, 2016, 7 (03) : 252 - 266
  • [3] Update on antifungal resistance in Aspergillus and Candida
    Arendrup, M. C.
    [J]. CLINICAL MICROBIOLOGY AND INFECTION, 2014, 20 : 42 - 48
  • [4] Asif M, 2014, MINI-REV MED CHEM, V14, P1093
  • [5] Pyridazin-3(2H)-ones: the versatile pharmacophore of medicinal significance
    Bansal, Ranju
    Thota, Sridhar
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (06) : 2539 - 2552
  • [6] Antibiotic Exposure as a Risk Factor for Fluconazole-Resistant Candida Bloodstream Infection
    Ben-Ami, Ronen
    Olshtain-Pops, Keren
    Krieger, Michal
    Oren, Ilana
    Bishara, Jihad
    Dan, Michael
    Wiener-Well, Yonit
    Weinberger, Miriam
    Zimhony, Oren
    Chowers, Michal
    Weber, Gabriel
    Potasman, Israel
    Chazan, Bibiana
    Kassis, Imad
    Shalit, Itamar
    Block, Colin
    Keller, Nathan
    Kontoyiannis, Dimitrios P.
    Giladi, Michael
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2012, 56 (05) : 2518 - 2523
  • [7] Bernabe KJ, 2017, INT J ANTIMICROB AG, V17, P30274
  • [8] Clinical Laboratory Standards Institute, 2012, M02A11 CLSI, P40
  • [9] Synthesis and analgesic and anti-inflammatory activities 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(p-substituted/nonsubstituted benzal)hydrazone derivatives
    Gokce, Mehtap
    Utku, Semra
    Kupeli, Esra
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (09) : 3760 - 3764
  • [10] Approaches towards the synthesis of a novel class of 2-amino-5-arylazonicotinate, pyridazinone and pyrido[2,3-d]pyrimidine derivatives as potent antimicrobial agents
    Ibrahim, Hamada Mohamed
    Behbehani, Haider
    Elnagdi, Mohamed H.
    [J]. CHEMISTRY CENTRAL JOURNAL, 2013, 7 : 1 - 16