Design, synthesis, and biological profile of novel N-(5-aryl-1,3,4-thiadiazol-2-yl) hydrazinecarboxamides

Abstract

KEYWORDSNew series of arylthiadiazole hydrazinecarboxamides (5a-e) have been synthesized by hydrazinolysis of carbamates (4a-e) and spectrally characterized. The new candidates have been screened for their anticonvulsant and immunomodulatory activities. Compound 5e was the most potent anticonvulsant candidate as it showed 100% protection against both maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) screens without neurotoxicity at 100 mg/kg (0.318 mmol/kg). With respect to immunomodulation, compounds 5a and 5d revealed immunostimulatory activity while compounds 5b, 5c, and 5e had immunosuppressive responses based on ELISA detection of IgM and IgG levels, counting the total mesenteric lymph nodes lymphocytes, and histo-pathological examinations.

Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives

“…Subcutaneous (sc) injection of aqueous solution of PTZ at a dose of 85 mg/kg was administered in the loose fold of skin at the back of the mouse neck. This dose (called convulsive dose 97 (CD97)), causes seizures in more than 97% of animals [ 37 ]. The test is carried out by giving scPTZ, 45 min after intraperitoneal injection (i.p.)…”

Synthesis and properties of m‐ferrocenylbenzoylthiadiazole derivatives

“…2‐Amino‐5‐aryl‐1,3,4‐thiazoles and 3‐ferrocenylbenzoic acid were synthesized according to the literature . Other reagents and starting materials were purchased from commercial sources.…”