Date of Award
Master of Science (MS)
Haythem Ali Saadeh
Raed A. Al-Qawasmeh
This thesis describes the synthesis of novel derivatives of isoniazid and 1, 3, 4- oxadiazole piperazines and biological activities evaluation. The synthesis of the isoniazid derivatives (36a-Ɩ) was achieved by nucleophilic substitution of chloroacetylated isoniazid 34 with substituted piperazines (35a-Ɩ) produced isoniazidpiperazines (36a-Ɩ). On the other hand, cyclodehydration of chloroacetylated isoniazid 34 with POCl3 give the corresponding 1, 3, 4-oxadiazole 37 which upon treatment with substituted piperazines (35a-m) gave 1, 3, 4-oxadiazole-piperazines (38a-m). All newly synthesized compounds were purified and characterized using spectroscopic techniques including 1H-NMR, 13C-NMR, IR spectrometry and mass spectrometry.
The biological activity of the synthesized compounds has been studied. The anti-bacterial activity was evaluated against six gram positive and gram negative bacteria. Compound 38m showed high and comparable activity as ciprofloxacin drug, while the other derivatives showed moderate activity. All derivatives showed no antifungal activity. Anti-cancer viability assay against breast cancer for selected derivatives showed significant activity.
Kaddoura, Ranem Mohammad, "Synthesis and Characterization of Novel Derivatives of 1, 3, 4- 0xadiazole and Isoniazid" (2020). Chemistry Theses. 13.