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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 14, No. 11, 2015, pp. 2047-2053
Bioline Code: pr15268
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 14, No. 11, 2015, pp. 2047-2053

 en Synthesis and Evaluation of some New 5-Substituted-1,3,4- oxadiazol-2yl-4-(morpholin-4yl Sulfonyl)benzyl Sulfides as Antibacterial Agent
Aziz-ur-Rehman; Gul, S.; Abbasi, M. A.; Nafeesa, K.; Akhtar, M. N.; Khan, K. M.; Ahmad, I. & Afzal, S.

Abstract

Purpose: To synthesise a new series of 5-substituted-1,3,4-Oxadiazol-2yl-4-(morpholin-4yl sulfonyl)benzyl sulfide and evaluate their antibacterial activity.
Methods: Different organic acids were converted consecutively into corresponding esters, hydrazides and 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-e). The targets, 6a-e were synthesized by stirring 4a-e with 4-(4-(bromomethyl)phenylsulfonyl) morpholine (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). All the structures were elucidated by modern spectroscopic techniques and screened against bacteria using standard procedure and ciprofloxacin drug as positive control.
Results: The yield of the synthesized compounds (4a-e and 6a-e) were moderate (65 - 90 %). Compounds 6a-e had antibacterial activity against Pseudomonas aeruginosa check for this species in other resources , Bacillis subtilis check for this species in other resources and Staphylococcus aureus check for this species in other resources while some had activity against the other bacteria used. One of the compounds, 6b, exhibited significant activity against all the bacterial strains, i.e., S. typhi check for this species in other resources (-), E. coli check for this species in other resources (-), K. pneumoniae check for this species in other resources (-), P. aeruginosa (-), B. subtilis (+) and S. aureus (+) with MIC (μM) values of 11.01 ± 0.31, 15.37 ± 3.33, 16.11 ± 1.14, 9.70 ± 1.96, 10.01 ± 2.70 and 9.15 ± 0.29, respectively. However, none of the compounds had any inhibitory activity against any bacteria as high as that of ciprofloxacin.
Conclusion: Five new compounds with antibacterial activities have been synthesized. Their potential as therapeutic agents is, however, yet to be evaluated.

Keywords
1,3,4-Oxadiazole; Benzyl sulfide; 4-(4-(bromomethyl)phenylsulfonyl)morpholine; Spectral analysis; Antibacterial activity

 
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