DESIGN, SYNTHESIS AND ANTIFUNGAL EVALUATION OF NOVEL SUBSTITUTED 1, 3, 4-OXADIAZOLES, AND 1, 3, 4-THIADIAZOLES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 9
Abstract
Objective: The purpose of this research is to evaluate the antifungal activity of synthesized conjugates of thiophene with 1, 3, 4-oxadiazoles and 1, 3, 4-thiadiazoles using in vitro methods.Methods: The series of (IVa-e) and (Va-e) compounds were synthesized from thiosemicarbazide (IIIa-e) series by treating with iodine-sodium hydroxide mixture and by phosphoric acid cyclization respectively. Thiosemicarbazides (IIIa-e) were prepared by the reaction of 2–amino-4, 5, 6, 7-tetrahydro-benzo[b]thiophene-3-carbohydrazide (II) with substituted isothiocyanates. Carbohydrazide (II) was synthesized by the reaction of hydrazine hydrate with ethyl 2–amino-4, 5, 6, 7-tetrahydrobenzeno[b]thiophene-3-carboxylate (I), which was prepared by one pot synthesis method. Finally, the synthesized compound series was characterized by physicochemical and spectral data (IR, NMR and Mass) and evaluated for in vitro antifungal activity against Candida albicans and Aspergillus niger using disc diffusion method. The percentage inhibition was calculated with reference to the standard drug.Results: The structures of the synthesized conjugates of thiophene with 1, 3, 4-oxadiazoles and 1, 3, 4–thiadiazoles were confirmed by IR, NMR, and Mass spectroscopic techniques. The results of bioassay were indicated that some synthesized compounds IVd, IVe, Vd, and Ve exhibited moderate antifungal activities against Candida albicans and Aspergillus niger; whereas compounds IVb, IVc, Vb, and Vc showed prominent antifungal activities when compared to standard drug, Fluconazole. Conclusion: Present study demonstrates the synthesis of conjugates of thiophene with 1, 3, 4-oxadiazoles and 1, 3, 4–thiadiazoles. These compounds were evaluated for in vitro antifungal activity against Candida albicans and Aspergillus niger using disc diffusion method. The compounds IVd, IVe, Vd, and Ve exhibited moderate antifungal activities, whereas compounds IVb, IVc, Vb, and Vc showed prominent antifungal activities. Â
Authors and Affiliations
Prabhat K Upadhyay, Pradeep Mishra
Keywords
Related Articles
- EP ID EP578483
- DOI -
- Views 65
- Downloads 0
EVALUATION OF ANTIFUNGAL ACTIVITY OF ORIGANUM VULGARE AND ROSMARINUS OFFICINALIS ESSENTIAL OIL BEFORE AND AFTER INCLUSION IN β-CYCLODEXTRINE
Objective: The aim of this study is to evaluate and compare the antifungal activity of essential oil of Origanum vulgare and Rosmarinus officinalis collected in north region of Albania, and how is it modified by microenc...
SYNTHESIS OF NOVEL TAMARIND 8-HYDROXYQUINOLINE-5-SULFONIC ACID (THQSA) RESIN AND THEIR APPLICATION IN INDUSTRIAL EFFLUENT TREATMENT
Objective: An investigation was undertaken regarding the adsorption of different heavy metal ions from industrial effluent using novel tamarind 8-hydroxyquinoline-5-sulfonic acid (THQSA) resin.Methods: THQSA resin was sy...
PHARMACOGNOSTIC STUDY OF CALLISTEMON CITRINUS L. BARK
Objective: Pharmacognostic study of Callistemon citrinus L. barkMethods: The bark of Callistemon citrinus L. was shade dried and powdered mechanically. The powdered material was used for further Pharmacognostic study. Th...
2.4 GHZ HETERODYNE RECEIVER FOR HEALTHCARE APPLICATION
The objective of this research was to design a basic 2.4 GHz heterodyne receiver for healthcare on a 130um CMOS process. The ultimate goal for the wireless industry is to minimize the trade-offs between performance and c...
UTILITY OF CERTAIN σ AND π-ACCEPTORS FOR THE SPECTROPHOTOMETRIC DETERMINATION OF VORICONAZOL ANTIFUGAL DRUG IN PHARMACEUTICAL FORMULATION
Objective: Studies were carried out, for the first time, to investigate the charge-transfer reactions of voriconazole antifungal drug (VOR) as n-electron donor with the σ-acceptor iodine (I2) and various π-acceptors: 7...