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Synthesis, structure elucidation, biological activity, enzyme inhibition and molecular docking studies of new Schiff bases based on 5-nitroisatin-thiocarbohydrazone    
Yazarlar
Hasan Yakan
Ondokuz Mayıs Üniversitesi, Türkiye
Hiba-H.S. Omer
Osman Buruk
Şükriye Çakmak
Sinop Üniversitesi, Türkiye
Sarmad Marah
Aysel Veyisoğlu
Sinop Üniversitesi, Türkiye
Doç. Dr. Halit MUĞLU Doç. Dr. Halit MUĞLU
Kastamonu Üniversitesi, Türkiye
Tevfik Özen
Türkiye
Halil Kütük
Türkiye
Özet
New Schiff bases bearing 5-nitroisatin-thiocarbohydrazone (1-9) have been prepared. The chemical structures of these compounds have been clarified by spectroscopic methods (IR, 1H NMR, and 13C NMR), and elemental analysis. Besides, they have been tested for antimicrobial activity. The antimicrobial activities of the novel compounds have been evaluated using a twofold serial dilution method for Minimum Inhibitory Concentration (MIC) against three gram-positive bacteria, three gram-negative bacteria, and two fungal pathogens. The obtained data showed that compound 7 has excellent activity against gram-strain-positive and gram-strain-negative bacteria. Compound 7 showed better activity than amoxicillin, which is one of the standard drugs used against the E. faecalis pathogen, but showed the same activity as tetracycline. Synthesized compounds could be formed the basis for the development of better antibacterial agents. The total antioxidant activity of compounds 3 and 5 showed better antioxidant activity than standard BHT, while compounds 4, 8, 7, 2, and 6 showed better antioxidant activity than standard Trolox. The urease inhibitory effect of compound 7 was better than thiourea. Also, the structure-activity relationship study showed that the scores of molecular models revealed that the compounds with the highest number of binding with urease enzyme were compounds 3 and 7 with total bond numbers of 19 and 18, respectively.
Anahtar Kelimeler
Antimicrobial activity | Antioxidant activity | Enzyme inhibitor | Molecular docking | Schiff bases | Spectroscopic studies
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı Journal of Molecular Structure
Dergi ISSN 0022-2860
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili İngilizce
Basım Tarihi 04-2023
Cilt No 1277
Sayı 1
Sayfalar 1 / 14
Doi Numarası 10.1016/j.molstruc.2022.134799
Makale Linki http://dx.doi.org/10.1016/j.molstruc.2022.134799