2, 4-Dihidro-1,2,4-Triazol Aminometil Türevlerinin İn Vitro Antioksidan ve Antimikrobiyal Aktivitelerinin Değerlendirilmesi
Öz
Günümüzde ilaç olarak kullanılan çoğu bileşiğin ana yapısında özellikle triazol, tiyadiazol ve oksadiazol gibi beş üyeli heterosiklik halka yapısı bulunmaktadır. Triazol bileşiklerinin büyük bir kısmının kullanımı, toksisite riski, uygulama zorluğu, yüksek oranda ilaç direncinin ortaya çıkması gibi sebeplerle ve istenmeyen yan etkilerin gözlenmesi, aktivitesindeki yetersizlik ve farmakokinetik eksiklikleri nedenleriyle sınırlı kalmıştır. Beş üyeli halka içeren bu bileşiklerin sağlık sektöründe, farmasötik kimyada, başta antikanser aktivite olmak üzere antifungal, anti-HIV, antitümör, antibakteriyal, antiviral, antidepresan, iltihap önleyici (antiinflamatuvar), tüberküloza karşı etkili (antitüberküloz), ağrı kesici (analjezik), idrar söktürücü (diüretik) gibi çok kapsamlı aktif biyolojik spektrumları bulunmaktadır. Bu çalışma ile farklı triazol bileşiklerinin (M1-M10) bazı biyolojik aktiviteleri araştırılarak triazoller konusunda yapılmış çalışmalara katkı sağlanması ve ilaç olabilme potansiyellerinin ortaya konulması planlanmıştır. Bu amaçla farklı triazol türevlerinin in vitro antioksidan aktiviteleri indirgeme-yükseltgeme potansiyelleri ile antimikrobiyal aktiviteleri araştırılmıştır. Bu çalışma kapsamında kullandığımız test bileşiklerinin bazılarının yüksek biyolojik aktivite özellikleriyle daha sonraki yapılacak çalışmalarda yol gösterici olacağını, başta ilaç sektörü olmak üzere yeni biyoyararlı malzemelerin üretimi konularında katkı sağlayacağına inanmaktayız. Ayrıca bu konunun literatüre kazandırılması ile de bu disiplinde çalışan bilim insanlarına yeni fikirler vereceğini düşünmekteyiz.
Anahtar Kelimeler
Triazol antioksidan aktivite antimikrobiyal aktivite metal şelatlama
Kaynakça
- 1. Kharb, R., Sharma, P.C., Yar, M.S., 2011. Pharmacological significance of triazole scaffold, J. Enzyme Inhib. Med. Chem., 26(1), 1-21. 2. Maccarrone, M., Ullrich, V., 2004, “Redox regulation in disease and ageing”, Cell Death and Differentiation, 11: 949–951. 3. Xiang, L., Chao, Li., Sheng, T., Qiuye, W., Honggang, H., Qingjie, Z. ve Yan, Z., 2016. Synthesis, In Vitro Biological Evaluation, and Molecular Docking of New Triazoles as Potent Antifungal Agents, Pharm. Chem. Life Sci., 349: 42 –49. 4. Sirassu, N., Ranjith, T. K., Nukala, S. K., Shaik, Y. ve Nagavelli, V. N., 2014. Synthesis and antibacterial activity of (1-aryl-1, 2, 3-triazol-4-yl) methyl esters of morpholine-3- carboxylic acid, Med. Chem. Res., 23: 5321–5327. 5. Kelly, F. J., 1998, “Use of antioxidants in the prevention and treatment of disease”, J Int Fed Clin Chem., 10(1):21-3 6. Georgopapadakou N. H., 1998. “Antifungals: mechanism of action and resistance, established and novel drugs”, Current Opinion in Microbiology, 1, 547- 548. 7. Oyaizu, M., 1986. ‘‘Studies on products of browning reaction prepared from glucosamine.,’’ Jpn. Nutr. 44, 307–316. 8. T.C.P. Dinis, V.M.C. Madeira, L.M. Almeida, 1994. ‘‘Action of phenolic derivatives (acetaminophen, salicylate, and 5-aminosalicylate) as inhibitors of membrane lipid peroxidation and as peroxyl radical scavengers’’ Arch. Biochem. Biophys., 315: 161–169. 9. Eloff JN, 1998. A sensitive and quick microplate method to determine the minimal inhibitory concentration of plant extracts for bacteria. Planta Med, 64:711–713. 10. CLSI, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically, Approved Standard, 9th ed., CLSI document M07-A9. Clinical and Laboratory Standards Institute, 950 West Valley Road, Suite 2500, Wayne, Pennsylvania 19087, USA, 2012. 11. CLSI, Reference Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts, Approved Standard, 2nd ed., NCCLS document M27- A2. CLSI, 940 West Valley Road, Suite 1400, Wayne, Pennsylvania 19087- 1898, USA, 2002. 12. Niki, E., 1991, ‘‘Vitamin C as an Antioxidant,’’ World Rev.Nutr.Diet., 64:3- 30. 13. Kandepu, NM., 1999, ‘‘Mannich bases of chalcones and cyclohexanones as candidate cytotoxic agents,’’ Ottawa: University of Saskatchewan. 14. Kuete V. (2010). Potential of Cameroonian plants and derived products against microbial infections: a review. Planta Med. 76 1479–1491. 10.1055/s-0030-1250027 15. Awouafack, M.D., McGaw, L.J., Gottfried, S., Mbouangouere R., Tane, P., Spiteller, M. and Eloff, J.N. (2013) Antimicrobial Activity and Cytotoxicity of the Ethanol Extract, Fractions and Eight Compounds Isolated from Eriosema robustum (Faba-ceae). BMC Complementary and Alternative Medicine, 13, 289. https://doi.org/10.1186/1472-6882-13-289
Evaluation of In Vitro Antioxidant and Antimicrobial Activities of 2, 4-Dihydro-1,2,4- Triazole Aminomethyl Derivatives
Öz
The main structure of most compounds used today as drugs is in particular the five-membered heterocyclic ring structure such as triazole, thiadiazole and oxadiazole. The use of a large proportion of triazole compounds has been limited by reasons of toxicity, difficulty in application, observation of occasional and undesirable side effects such as high drug resistance, inadequacy of activity and pharmacokinetic deficiencies. These compounds containing five members of the ring can be used in the healthcare sector in pharmaceutical chemistry, especially antifungal, anti-HIV, antitumoral, antibacterial, antiviral, antiinflammatory, analgesic, and diuretics. In this study, it was planned to investigate some biological activities of different triazole compounds (M1-M10) and to contribute the triazoles to studies and to determine the drug potentials. For this purpose, the antioxidant activities of different triazole derivatives were investigated by their reduction-oxidation potentials and antimicrobial activities. We believe that some of the test compounds we use in this study will contribute to the future work with high biological activity properties and will contribute to the production of new bioactive materials, especially in the pharmaceutical sector. We also think that this will give new ideas to the scientists who work in this discipline with the introduction of the literature.
Anahtar Kelimeler
Triazole antioxidant activity antimicrobial activity metal chelating
Kaynakça
- 1. Kharb, R., Sharma, P.C., Yar, M.S., 2011. Pharmacological significance of triazole scaffold, J. Enzyme Inhib. Med. Chem., 26(1), 1-21. 2. Maccarrone, M., Ullrich, V., 2004, “Redox regulation in disease and ageing”, Cell Death and Differentiation, 11: 949–951. 3. Xiang, L., Chao, Li., Sheng, T., Qiuye, W., Honggang, H., Qingjie, Z. ve Yan, Z., 2016. Synthesis, In Vitro Biological Evaluation, and Molecular Docking of New Triazoles as Potent Antifungal Agents, Pharm. Chem. Life Sci., 349: 42 –49. 4. Sirassu, N., Ranjith, T. K., Nukala, S. K., Shaik, Y. ve Nagavelli, V. N., 2014. Synthesis and antibacterial activity of (1-aryl-1, 2, 3-triazol-4-yl) methyl esters of morpholine-3- carboxylic acid, Med. Chem. Res., 23: 5321–5327. 5. Kelly, F. J., 1998, “Use of antioxidants in the prevention and treatment of disease”, J Int Fed Clin Chem., 10(1):21-3 6. Georgopapadakou N. H., 1998. “Antifungals: mechanism of action and resistance, established and novel drugs”, Current Opinion in Microbiology, 1, 547- 548. 7. Oyaizu, M., 1986. ‘‘Studies on products of browning reaction prepared from glucosamine.,’’ Jpn. Nutr. 44, 307–316. 8. T.C.P. Dinis, V.M.C. Madeira, L.M. Almeida, 1994. ‘‘Action of phenolic derivatives (acetaminophen, salicylate, and 5-aminosalicylate) as inhibitors of membrane lipid peroxidation and as peroxyl radical scavengers’’ Arch. Biochem. Biophys., 315: 161–169. 9. Eloff JN, 1998. A sensitive and quick microplate method to determine the minimal inhibitory concentration of plant extracts for bacteria. Planta Med, 64:711–713. 10. CLSI, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically, Approved Standard, 9th ed., CLSI document M07-A9. Clinical and Laboratory Standards Institute, 950 West Valley Road, Suite 2500, Wayne, Pennsylvania 19087, USA, 2012. 11. CLSI, Reference Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts, Approved Standard, 2nd ed., NCCLS document M27- A2. CLSI, 940 West Valley Road, Suite 1400, Wayne, Pennsylvania 19087- 1898, USA, 2002. 12. Niki, E., 1991, ‘‘Vitamin C as an Antioxidant,’’ World Rev.Nutr.Diet., 64:3- 30. 13. Kandepu, NM., 1999, ‘‘Mannich bases of chalcones and cyclohexanones as candidate cytotoxic agents,’’ Ottawa: University of Saskatchewan. 14. Kuete V. (2010). Potential of Cameroonian plants and derived products against microbial infections: a review. Planta Med. 76 1479–1491. 10.1055/s-0030-1250027 15. Awouafack, M.D., McGaw, L.J., Gottfried, S., Mbouangouere R., Tane, P., Spiteller, M. and Eloff, J.N. (2013) Antimicrobial Activity and Cytotoxicity of the Ethanol Extract, Fractions and Eight Compounds Isolated from Eriosema robustum (Faba-ceae). BMC Complementary and Alternative Medicine, 13, 289. https://doi.org/10.1186/1472-6882-13-289
Ayrıntılar
| Birincil Dil | Türkçe |
|---|---|
| Konular | Klinik Tıp Bilimleri |
| Bölüm | Araştırma Makalesi |
| Yazarlar | |
| Yayımlanma Tarihi | 1 Ağustos 2018 |
| Yayımlandığı Sayı | Yıl 2018Cilt: 3 Sayı: 1 |
