Shantaram Gajanan Khanage1, Popat Baban Mohite1, Ramdas Bhanudas Pandhare2, S Appala Raju3. 1. Department of Pharmaceutical Chemistry and PG studies, M.E.S. College of Pharmacy, Sonai, Ahmednagar, Maharashtra, India-414105. 2. Department of Pharmacology, M.E.S. College of Pharmacy, Sonai, Tq-Newasa, Dist.-Ahmednagar, Maharashtra, India-414105. 3. Department of Pharmaceutical chemistry, H.K.E.'S College of Pharmacy, Sedam road, Gulbarga, Karnataka, India-585105.
Abstract
PURPOSE: An efficient technique has been developed for microwave assisted synthesis of 1-[5-(substituted aryl)-1H-pyrazol-3-yl]-3,5-diphenyl-1H-1,2,4-triazole as antinociceptive and antimicrobial agents. METHODS: The desired compounds (S1-S10) were synthesized by the microwave irradiation via cyclization of formerly synthesized chalcones of 3,5-diphenyl-1H-1,2,4-triazole and hydrazine hydrate in mild acidic condition. All newly synthesized compounds were subjected to study their antinociceptive and antimicrobial activity. The analgesic potential of compounds was tested by acetic acid induced writhing response and hot plate method. The MIC values for antimicrobial activity were premeditated by liquid broth method. RESULTS: The compounds S1, S2, S4, S6 and S10 were found to be excellent peripherally acting analgesic agents when tested on mice by acetic acid induced writhing method and compounds S3, S6 and S1 at dose level of 100 mg/kg were exhibited superior centrally acting antinociceptive activity when tested by Eddy's hot plate method. In antimicrobial activity compound S10 found to be broad spectrum antibacterial agent at MIC value of 15.62 µg/ml and compound S6 was exhibited antifungal potential at 15.62 µg/mL on both fungal strains. CONCLUSION: Some novel pyrazoles clubbed with 1,2,4-triazole derivatives were synthesized and evaluated as possible antimicrobial, centrally and peripherally acting analgesics.
PURPOSE: An efficient technique has been developed for microwave assisted synthesis of 1-[5-(substituted aryl)-1H-pyrazol-3-yl]-3,5-diphenyl-1H-1,2,4-triazole as antinociceptive and antimicrobial agents. METHODS: The desired compounds (S1-S10) were synthesized by the microwave irradiation via cyclization of formerly synthesized chalcones of 3,5-diphenyl-1H-1,2,4-triazole and hydrazine hydrate in mild acidic condition. All newly synthesized compounds were subjected to study their antinociceptive and antimicrobial activity. The analgesic potential of compounds was tested by acetic acid induced writhing response and hot plate method. The MIC values for antimicrobial activity were premeditated by liquid broth method. RESULTS: The compounds S1, S2, S4, S6 and S10 were found to be excellent peripherally acting analgesic agents when tested on mice by acetic acid induced writhing method and compounds S3, S6 and S1 at dose level of 100 mg/kg were exhibited superior centrally acting antinociceptive activity when tested by Eddy's hot plate method. In antimicrobial activity compound S10 found to be broad spectrum antibacterial agent at MIC value of 15.62 µg/ml and compound S6 was exhibited antifungal potential at 15.62 µg/mL on both fungal strains. CONCLUSION: Some novel pyrazoles clubbed with 1,2,4-triazole derivatives were synthesized and evaluated as possible antimicrobial, centrally and peripherally acting analgesics.
Entities:
Keywords:
Antimicrobial; Antinociceptive; Chalcones; Hot plate method; MIC; Microwave
Authors: Nur Izzati Ismail; Lee Ming-Tatt; Nordin Lajis; Muhammad Nadeem Akhtar; Ahmad Akira; Enoch Kumar Perimal; Daud Ahmad Israf; Mohd Roslan Sulaiman Journal: Molecules Date: 2016-08-22 Impact factor: 4.411