Tuesday , 11 May 2021

Synthesis and Antimicrobial activity of 5[4(morpholin-4-yl) phenyl] 1,3,4 Oxadiazole 2-yl Sulphonyl acetohydrazide Derivatives

Author Details
M Somashekhar*1, Basavraj Sonnad4, Bharati Tare1, R V Heralagi2, Sachin Lokapure3
1Department Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore.
4Department Pharmacology, Krupanidhi College of Pharmacy, Bangalore.
2Department Pharmaceutical Chemistry, BLDEA’S College of Pharmacy, Bijapur. India
3Department Pharmaceutical Chemistry, Rajaram Bapu College of Pharmacy, Kasegaon, India.

We have chosen molecule having moieties possessing antimicrobial activity, one of which is hydrazide skeleton, which is reported to have antibacterial and antitubercular activity and other morpholine ring attached to 4th position of the benzene ring which possess the antibacterial, antimycobacterial and antifungal activity. Present work deals with the preparation of morpholie And 4-chloro-benzonitrile on reflux gives 4-(morpholine-4-yl)benzonitrile. This upon treating with sodium hydroxide gives 4-(morpholin-4-yl)benzoicacid. Then this upon treating with thionyl chloride gives 4-(morpholin-4-yl)benzoyl chloride. This on further treatement with hydrazine-hydrate gives 4-(morpholin-4-yl) benzohydrazide. Which is treated with Carbon di sulphide gives 5[4(morpholin-4-yl) phenyl ] 1,3,4 oxadiazole 2-thiol and it is treated with chloroacetyl chloride gives 5[4(morpholin-4-yl) phenyl ] 1,3,4 oxadiazole 2-yl sulphonylacetylchloride and then it is further treated with hydrazine hydrate gives 5[4(morpholin-4-yl) phenyl ] 1,3,4 oxadiazole 2-yl sulphonyl acetohydrazide and then it is treated with various substituted of aromatic aldehyde and to form morpholine derivatives. Hydrazides were synthesized so as to increase intracellular concentration and so as to try and decrease the resistant developed due to decrease intracellular concentration of the drug. These synthesized compounds were subjected to preliminary biological evaluation. The characterization of synthesized compounds was identified on the basis of IR, 1HNMR, Mass spectroscopy. The compounds have been evaluated for antimicrobial activity.
Keywords: Morpholine, Antimicrobial activity, Intracellular concentration


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