Examination of antibacterial properties of three thiazolidine-4-carboxylic acid derivatives against Pseudomonas, Acinetobacter, Staphylococcus aureus, and Escherichia coli
Abstract
Treatment of multi-drug resistant bacteria is a growing problem for global public health. We need new drugs to keep up with resistant. It is known that Thiazolidine-4-carboxylic acids (TCA) are able to inhibit bacterial growth by mimicking various essential functions of naturally occurring amino acids. Therefore, we aimed to synthesis three TCA derivatives, two of them are novel, and investigated their antibacterial activities on multi-drug resistant (MDR) bacteria. Compounds (1a-c) were synthesized from L-Cysteine hydrochloride and dihydroxybenzaldehyde derivatives and their in vitro activities against multi-drug resistant bacteria were assayed by the Kirby-Bauer method according to CLSI criteria. 1a-c exhibited significant antibacterial effect against Gram-positive bacteria such as S. aureus and Gram-negative bacteria such as Pseudomanas, Acinetobacter, and Escherichia coli superior to current antibiotics. Here, new potential antibacterial agents, which can be easily synthesized in high yield under mild condition, have been reported. But it is clear that further research and in-vitro activity tests of these three compounds should be performed.
Keywords
Kaynakça
- 1. Sriramurthy V, Barcan GA, Kwon O. Bisphosphine-catalyzed mixed double-Michael reactions: Asymmetric synthesis of oxazolidines, thiazolidines, and pyrrolidines. J Am Chem Soc 2007; 129:12928-12929.
- 2. Song ZC, Ma GY, Lv PC, Li HQ, Xiao ZP, Zhu HL. Synthesis, structure and structure-activity relationship analysis of 3-tert-butoxycarbonyl-2-arylthiazolidine-4-carboxylic acid derivatives as potential antibacterial agents. Eur J Med Chem 2009; 44:3903-3908.
- 3. Moallem SA, Imenshahidi M, Shahini N, Javan AR, Karimi M, Alibolandi M et al. Synthesis, anti-inflammatory and anti-nociceptive activities and cytotoxic effect of novel thiazolidin-4-ones derivatives as selective cyclooxygenase (COX-2) inhibitors. Iran J of Basic Med Sci 2013; 16:1238-1244.
- 4. Hutt MP, Antibacterial thiazolidine or thiomorpholine substituted quinolones. US Patent 4,473,568 A, 25 Sep. 1984.
- 5. Onen-Bayram FE, Durmaz I, Scherman D, Herscovici J, Cetin-Atalay R, A novel thiazolidine compound induces caspase-9 dependent apoptosis in cancer cells. Bioorg Med Chem 2012; 20:5094-5102. 6. Li W, Lu Y, Wang Z, Dalton JT, Miller DD, Synthesis and antiproliferative activity of thiazolidine analogs for melanoma. Bioorg Med Chem Lett 2007; 17:4113-4117. 7. Aiello F, Brizzi A, De Grazia O, Garofalo A, Grande F, Sinicropi, MS et al. An approach to the stereo-controlled synthesis of polycyclic derivatives of l-4-thiazolidinecarboxylic acid active against HIV-1 integrase. Eur J Med Chem 2006; 41:914-917.
- 8. Ha YM, Park YJ, Lee JY, Park D, Choi YJ, Lee EK et al. Design, synthesis and biological evaluation of 2-(substituted phenyl) thiazolidine-4-carboxylic acid derivatives as novel tyrosinase inhibitors. Biochimie 2012; 94:533-540.
- 9. Unger L, DeMoss RD. Action of a proline analogue, l-thiazolidine-4-carboxylic acid, in Escherichia coli. J Bacteriol 1966; 91:1556–1563.
- 10. Anderson RJ, Groundwater PW, Todd A, Worsley AJ. Antibacterial Agents: Chemistry, Mode of Action, Mechanisms of Resistance and Clinical Applications, John Wiley and Sons; 2012.
Ayrıntılar
Birincil Dil
İngilizce
Konular
Sağlık Kurumları Yönetimi
Bölüm
Araştırma Makalesi
Yayımlanma Tarihi
31 Aralık 2017
Gönderilme Tarihi
30 Haziran 2017
Kabul Tarihi
8 Eylül 2017
Yayımlandığı Sayı
Yıl 2017 Cilt: 2 Sayı: 4