1. Antimicrobial and Hypoglycemic Activities of Novel N-Mannich Bases Derived from 5-(1-Adamantyl)-4-substituted-1,2,4-triazoline-3-thiones
- Author
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Ali A. El-Emam, Hanan M. Hassan, Ebtehal S. Al-Abdullah, Hanaa M. Al-Tuwaijri, El-Sayed E. Habib, and Mogedda E. Haiba
- Subjects
Blood Glucose ,Male ,Stereochemistry ,Administration, Oral ,Microbial Sensitivity Tests ,1,2,4-triazoles ,Median lethal dose ,Catalysis ,Article ,Diabetes Mellitus, Experimental ,Inorganic Chemistry ,Lethal Dose 50 ,Mannich Bases ,lcsh:Chemistry ,Anti-Infective Agents ,medicine ,Animals ,Hypoglycemic Agents ,Gliclazide ,Physical and Theoretical Chemistry ,Candida albicans ,Molecular Biology ,lcsh:QH301-705.5 ,Spectroscopy ,N-Mannich bases ,antimicrobial activity ,biology ,Molecular Structure ,Chemistry ,Organic Chemistry ,General Medicine ,Pathogenic fungus ,biology.organism_classification ,Antimicrobial ,In vitro ,Computer Science Applications ,Rats ,lcsh:Biology (General) ,lcsh:QD1-999 ,hypoglycemic activity ,adamantane derivatives ,Antibacterial activity ,Bacteria ,medicine.drug - Abstract
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%).
- Published
- 2014