Yıl: 2020 Cilt: 10 Sayı: 3 Sayfa Aralığı: 681 - 694 Metin Dili: İngilizce DOI: 10.17714/gumusfenbil.679313 İndeks Tarihi: 18-02-2021

Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives

Öz:
In this study, new thiophene Schiff bases with morpholine (1,2) were synthesized. The structures of the compoundswere confirmed by 1H-NMR, 13C-NMR and IR spectrometry and their antioxidant, antibacterial, antileishmanial andenzyme activities were tested. The antioxidant activities observed from compounds 1 and 2 were remarkably high.According to the results obtained in our study, the compounds did not have antileishmanial activity (MIC >20000µg/ml). It was determined that the synthesized compounds had different rates of antibacterial activity against ninedifferent standard bacterial isolates. Enzyme inhibition effect of the compounds 1 and 2 was unimportant level and thecompound exhibited low binding affinity against the enzyme in molecular docking studies. The compounds 1 and 2formed many 𝜋 interactions with active site residue, however, they do not inhibit the enzyme due to did not interactwith key residues of the enzymes. Our in silico and in vitro studies results were compatible with each other. As a result,the compounds 1 and 2 may be used as antioxidant and antimicrobial drugs, If they can be investigated as drugcandidates.
Anahtar Kelime:

Yeni Schiff Bazlı Bileşiklerin Sentezi, Biyolojik Aktivite ve Moleküler Docking Çalışmaları

Öz:
Bu çalışmada, morfolinli (1,2) yeni tiyofen Schiff bazları sentezlenmiştir. Bileşiklerin yapıları, 1H-NMR, 13C-NMR ve IR spektrometrisi ile doğrulanarak antioksidan, antibakteriyel, antileishmanial ve enzim aktiviteleri test edilmiştir. Bileşik 1 ve 2'den gözlemlenen antioksidan aktiviteler dikkat çekici derecede yüksek olarak belirlenmiştir. Çalışmamızda elde edilen sonuçlara göre, bileşikler antileishmanial aktivite göstermemiştir (MIC> 20000 µg / ml). Sentezlenen bileşiklerin dokuz farklı standart bakteri izolatına karşı farklı antibakteriyel aktivite oranlarına sahip olduğu belirlenmiştir. Bileşik 1 ve 2'nin enzim inhibisyon etkisi önemsiz düzeyde olup ve bu bileşikler moleküler docking çalışmalarında enzimlere karşı düşük bağlanma afinitesi sergilemişlerdir. Bileşik 1 ve 2, aktif bölge kalıntısı ile birçok 𝜋 etkileşimi oluşturmuştur., Ancak, bu enzimlerin önemli kalıntıları ile etkileşime girmediği için enzimleri inhibe etmemişleridir. In siliko ve in vitro çalışma sonuçları birbiri ile uyumludur. Sonuç olarak bileşikler 1 ve 2, ilaç olarak araştırılırsa, antioksidan ve antimikrobiyal ilaçlar olarak kullanılabilir.
Anahtar Kelime:

Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
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APA Ünlüer D, ÜNVER Y, BEKTAŞ E, Direkel Ş, KARAMAN M, Karaman H (2020). Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. , 681 - 694. 10.17714/gumusfenbil.679313
Chicago Ünlüer Dilek,ÜNVER YASEMİN,BEKTAŞ Ersan,Direkel Şahin,KARAMAN Muhammet,Karaman Halide Sedef Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. (2020): 681 - 694. 10.17714/gumusfenbil.679313
MLA Ünlüer Dilek,ÜNVER YASEMİN,BEKTAŞ Ersan,Direkel Şahin,KARAMAN Muhammet,Karaman Halide Sedef Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. , 2020, ss.681 - 694. 10.17714/gumusfenbil.679313
AMA Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. . 2020; 681 - 694. 10.17714/gumusfenbil.679313
Vancouver Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. . 2020; 681 - 694. 10.17714/gumusfenbil.679313
IEEE Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H "Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives." , ss.681 - 694, 2020. 10.17714/gumusfenbil.679313
ISNAD Ünlüer, Dilek vd. "Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives". (2020), 681-694. https://doi.org/10.17714/gumusfenbil.679313
APA Ünlüer D, ÜNVER Y, BEKTAŞ E, Direkel Ş, KARAMAN M, Karaman H (2020). Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. Gümüşhane Üniversitesi Fen Bilimleri Dergisi, 10(3), 681 - 694. 10.17714/gumusfenbil.679313
Chicago Ünlüer Dilek,ÜNVER YASEMİN,BEKTAŞ Ersan,Direkel Şahin,KARAMAN Muhammet,Karaman Halide Sedef Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. Gümüşhane Üniversitesi Fen Bilimleri Dergisi 10, no.3 (2020): 681 - 694. 10.17714/gumusfenbil.679313
MLA Ünlüer Dilek,ÜNVER YASEMİN,BEKTAŞ Ersan,Direkel Şahin,KARAMAN Muhammet,Karaman Halide Sedef Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. Gümüşhane Üniversitesi Fen Bilimleri Dergisi, vol.10, no.3, 2020, ss.681 - 694. 10.17714/gumusfenbil.679313
AMA Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. Gümüşhane Üniversitesi Fen Bilimleri Dergisi. 2020; 10(3): 681 - 694. 10.17714/gumusfenbil.679313
Vancouver Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives. Gümüşhane Üniversitesi Fen Bilimleri Dergisi. 2020; 10(3): 681 - 694. 10.17714/gumusfenbil.679313
IEEE Ünlüer D,ÜNVER Y,BEKTAŞ E,Direkel Ş,KARAMAN M,Karaman H "Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives." Gümüşhane Üniversitesi Fen Bilimleri Dergisi, 10, ss.681 - 694, 2020. 10.17714/gumusfenbil.679313
ISNAD Ünlüer, Dilek vd. "Synthesis, Biological Activities and Molecular Docking Studies of New Schiff Bases Derivatives". Gümüşhane Üniversitesi Fen Bilimleri Dergisi 10/3 (2020), 681-694. https://doi.org/10.17714/gumusfenbil.679313