Antimicrobial and Hypoglycemic Activities of Novel N-Mannich Bases Derived from 5-(1-Adamantyl)-4-substituted-1,2,4-triazoline-3-thiones

International Journal of Molecular Sciences

Ebtehal S. Al-Abdullah¹  Hanaa M. Al-Tuwaijri¹  Hanan M. Hassan²  Mogedda E. Haiba¹  Elsayed E. Habib³  Ali A. El-Emam¹ 

[1] Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; E-Mails:;Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia; E-Mail:;Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Medinah 11344, Saudi Arabia; E-Mail:

关键词: adamantane derivatives;    1;    2;    4-triazoles;    N-Mannich bases;    antimicrobial activity;    hypoglycemic activity;   

DOI  :  10.3390/ijms151222995

来源: mdpi

【 摘 要 】

The reaction of 5-(1-adamantyl)-4-ethyl or allyl-1,2,4-triazoline-3-thione with formaldehyde solution and various 1-substituted piperazines yielded the corresponding N-Mannich bases. The newly synthesized N-Mannich bases were tested for in vitro inhibitory activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Six compounds showed potent antibacterial activity against one or more of the tested microorganisms, while two compounds exhibited moderate activity against the tested Gram-positive bacteria. None of the newly synthesized compounds were proved to possess marked activity against Candida albicans. The oral hypoglycemic activity of six compounds was determined in streptozotocin (STZ)-induced diabetic rats. Four compounds produced significant strong dose-dependent reduction of serum glucose levels, compared to gliclazide at 10 mg/kg dose level (potency ratio > 75%).

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.