title: Antimicrobial and hypoglycemic activities of novel N-Mannich bases derived from 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thiones.
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%).
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. ealabdullah@ksu.edu.sa.
authors.forename: Ebtehal S
authors.initials: ES
authors.lastname: Al-Abdullah
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. haltuwajri@ksu.edu.sa.
authors.forename: Hanaa M
authors.initials: HM
authors.lastname: Al-Tuwaijri
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia. hananhafila@hotmail.com.
authors.forename: Hanan M
authors.initials: HM
authors.lastname: Hassan
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. mogedda.haiba@yahoo.com.
authors.forename: Mogedda E
authors.initials: ME
authors.lastname: Haiba
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Medinah 11344, Saudi Arabia. sayedhabib@hotmail.co.jp.
authors.forename: Elsayed E
authors.initials: EE
authors.lastname: Habib
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. aelemam@ksu.edu.sa.
authors.forename: Ali A
authors.initials: AA
authors.lastname: El-Emam
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D001786:Blood Glucose / Q000187:drug effects; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D007928:Lethal Dose 50; D008297:Male; D008352:Mannich Bases / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D051381:Rats
chemical_list: D000890:Anti-Infective Agents; D001786:Blood Glucose; D007004:Hypoglycemic Agents; D008352:Mannich Bases