European Journal of Chemistry

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

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Published: Sep 30, 2014
DOI: https://doi.org/10.5155/eurjchem.5.3.488-496.1073
Keywords:
ELISA, Thiadiazoles, Arylthiadiazole, Anticonvulsants, Immunomodulatory, Hydrazinecarboxamides
Section
Research Article
Issue
Vol. 5 No. 3 (2014): September 2014
Dates
Received 2014-04-10
Accepted 2014-04-29
Published 2014-09-30


Main Article Content

Mohammed Farrag El-Behairy
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Mohamed Nabil Aboul-Enein
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Aida Abdel-Sattar El-Azzouny
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Ola Ahmed Saleh
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Yousreya Aly Maklad
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Mona Elsayed Aboutabl
Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, 12311, Cairo, Egypt
Amany Sayed Maghraby
Therapeutic Chemistry Department, Pharmaceutical and Drug Industries Research Division, Immunology and Infectious Diseases Laboratory, Centre of Excellence for Advanced Sciences, National Research Centre, Dokki, 12311, Cairo, Egypt

Abstract

New 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.


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El-Behairy, M. F.; Aboul-Enein, M. N.; El-Azzouny, A. A.-S.; Saleh, O. A.; Maklad, Y. A.; Aboutabl, M. E.; Maghraby, A. S. Design, Synthesis, and Biological Profile of Novel N-(5-Aryl-1,3,4-Thiadiazol-2-Yl) Hydrazinecarboxamides. Eur. J. Chem. 2014, 5, 488-496.

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Supporting Agencies

National Research Centre (Project No, 10010302), Dokki, Cairo, Egypt
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