Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives
Yıl: 2019 Cilt: 6 Sayı: 2 Sayfa Aralığı: 424 - 432 Metin Dili: İngilizce DOI: 10.35193/bseufbd.601344 İndeks Tarihi: 15-09-2020
Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives
Öz: In this study, 8 new compounds having 2-((5-substituted-1,3,4-thiadazol-2-yl)amino)-2-oxoethyl-4-substituepiperazine-1-carbodithioate structures were synthesized, antimicrobial and anticholinesterase activitieswere evaluated. The structures of synthesized compounds were proved by 1H NMR, 13C NMR and mass spectra.The synthesized compounds were tested for antibacterial activity against eight bacteria strains and antifungalactivity against four fungus strains. When the antibacterial activities of the compounds were examined, it wasfound that the compounds 3c, 3d, 3g and 3h were effective against E. faecalis (ATCC 29212) and E. faecalis(ATCC 51922) with MIC value of 25 μg/mL. It was determined that the carbon chain at the para position ofpiperazine increased the activity but where as the addition of benzyl group to the para position (3a, 3b, 3e, 3f)did not affect the activity. Furthermore, the acetylcholinesterase activity of the synthesized compounds wasexamined but none of the compounds showed AChE inhibitory activity as much as standard drug Donepezil.
Anahtar Kelime: Yeni 1,3,4-Tiyadiazol-Piperazin Türevlerinin Sentezi, İn Vitro Antikolinesteraz ve Antimikrobiyal Değerlendirilmesi
Öz: Bu çalışmada 2-((5-substitüe-1,3,4-tiyadiazol-2-il)amino)-2-oksoetil-4-substitüepiperazin-1-karboditiyat yapısında 8 yeni bileşiğin sentezi yapılarak, antimikrobiyal ve antikolinesteraz aktiviteleri incelenmiştir. Sentezlenen bileşiklerin yapıları IR, 1H NMR, 13C NMR ve kütle spektrumları kullanılarak kanıtlanmıştır. Sentezlenen bileşikler, sekiz bakteri suşuna karşı antibakteriyel aktivite ve dört mantar suşuna karşı antifungal aktivite açısından test edilmiştir. Bileşiklerin antibakteriyel aktiviteleri incelendiğinde 3c, 3d, 3g ve 3h kodlu bileşiklerin 25 μg/mL MİK değeri ile E. fecalis (ATCC 29212) ve E. fecalis (ATCC 51922) karşı etkili oldukları bulunmuştur. Piperazinin para konumunda bulunan karbon zincirinin aktiviteyi arttırdığı (3c, 3d, 3g, 3h), ancak para konumuna benzil grubunun eklenmesinin (3a, 3b, 3e, 3f) aktiviteyi etkilemediği belirlenmiştir. Ayrıca, sentezlenen bileşiklerin asetilkolinesteraz aktivitesi incelenmiş ancak bileşiklerden hiçbiri standart ilaç Donepezil kadar AChE inhibe edici aktivite göstermemiştir.
Anahtar Kelime: Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
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| APA | SAGLIK B, ACAR ÇEVİK U (2019). Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. , 424 - 432. 10.35193/bseufbd.601344 |
| Chicago | SAGLIK BEGÜM NURPELIN,ACAR ÇEVİK ULVİYE Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. (2019): 424 - 432. 10.35193/bseufbd.601344 |
| MLA | SAGLIK BEGÜM NURPELIN,ACAR ÇEVİK ULVİYE Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. , 2019, ss.424 - 432. 10.35193/bseufbd.601344 |
| AMA | SAGLIK B,ACAR ÇEVİK U Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. . 2019; 424 - 432. 10.35193/bseufbd.601344 |
| Vancouver | SAGLIK B,ACAR ÇEVİK U Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. . 2019; 424 - 432. 10.35193/bseufbd.601344 |
| IEEE | SAGLIK B,ACAR ÇEVİK U "Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives." , ss.424 - 432, 2019. 10.35193/bseufbd.601344 |
| ISNAD | SAGLIK, BEGÜM NURPELIN - ACAR ÇEVİK, ULVİYE. "Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives". (2019), 424-432. https://doi.org/10.35193/bseufbd.601344 |
| APA | SAGLIK B, ACAR ÇEVİK U (2019). Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi, 6(2), 424 - 432. 10.35193/bseufbd.601344 |
| Chicago | SAGLIK BEGÜM NURPELIN,ACAR ÇEVİK ULVİYE Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi 6, no.2 (2019): 424 - 432. 10.35193/bseufbd.601344 |
| MLA | SAGLIK BEGÜM NURPELIN,ACAR ÇEVİK ULVİYE Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi, vol.6, no.2, 2019, ss.424 - 432. 10.35193/bseufbd.601344 |
| AMA | SAGLIK B,ACAR ÇEVİK U Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi. 2019; 6(2): 424 - 432. 10.35193/bseufbd.601344 |
| Vancouver | SAGLIK B,ACAR ÇEVİK U Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives. Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi. 2019; 6(2): 424 - 432. 10.35193/bseufbd.601344 |
| IEEE | SAGLIK B,ACAR ÇEVİK U "Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives." Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi, 6, ss.424 - 432, 2019. 10.35193/bseufbd.601344 |
| ISNAD | SAGLIK, BEGÜM NURPELIN - ACAR ÇEVİK, ULVİYE. "Synthesis, In Vitro Anticholinesterase and Antimicrobial Evaluation of New 1,3,4-Thiadiazole-Piperazine Derivatives". Bilecik Şeyh Edebali Üniversitesi Fen Bilimleri Dergisi 6/2 (2019), 424-432. https://doi.org/10.35193/bseufbd.601344 |
