| Yazarlar |
Hasan Tunel
|
|
Mustafa Er
Türkiye |
|
Hakan Alıcı
Zonguldak Bülent Ecevit Üniversitesi, Türkiye |
|
Abdurrahman Onaran
Akdeniz Üniversitesi, Türkiye |
Tuncay KARAKURT
Kırşehir Ahi Evran Üniversitesi, Türkiye |
|
Hakan Tahtacı
Karabük Üniversitesi, Türkiye |
| Özet |
| In this study, thioether-bridged imidazo[2,1-b][1,3,4]thiadiazole derivatives that contained both imidazole and 1,3,4-thiadiazole (compounds 7a-7i and 8a-8i) were synthesized from the reactions of 2-amino-1,3,4-thiadiazole with phenacyl bromide (6a-6i) (at yields of 59% to 74%). The structure of the synthesized compounds was characterized using H-1 NMR, C-13 NMR, Fourier-transform infrared spectroscopy, elemental analysis, mass spectroscopy, and X-ray diffraction analysis. Mycelial growth, mycelial growth inhibition, minimum inhibitory concentration, minimum fungicidal concentration, and lethal dose values against various plant pathogenic fungi were determined for all of the target compounds synthesized in the study. The test results showed that most of the compounds had moderate to good antifungal activity. In addition, the absorption, distribution, metabolism, excretion (ADME) parameters of the compounds were calculated, and it was observed that all of the compounds met the drug-likeness rules in general. Finally, using docking simulations, it was found that compounds 7h, 7i, 8h, and 8i showed high affinity to PDB ID:5TZ1, which is an CYP51 antifungal target structure. |
| Anahtar Kelimeler |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | JOURNAL OF HETEROCYCLIC CHEMISTRY |
| Dergi ISSN | 0022-152X |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Makale Dili | Türkçe |
| Basım Tarihi | 06-2021 |
| Cilt No | 58 |
| Sayı | 6 |
| Sayfalar | 1321 / 1343 |
| Doi Numarası | 10.1002/jhet.4260 |
| Makale Linki | http://dx.doi.org/10.1002/jhet.4260 |
| Atıf Sayıları | |
| WoS | 9 |
| SCOPUS | 11 |
| Google Scholar | 13 |
