Anitha Huliyurdurga Channigarayappa1, Sreenivasa Swamy1*, Mohan R Nadigar2, Vivek Chandramohan3, Shivaraja Govindaiaha1
1Department of Studies and Research in Chemistry, Tumkur University, Tumkur-572103, Karnataka, INDIA
2Department of PG Studies in Chemistry, Shridevi PG Centre. Sira Road, Tumkur-572106, Karnataka, INDIA.
3Department of Biotechnology, Siddaganga Institute of Technology, Tumkur-572103, Karnataka, INDIA
*Corresponding Author
Dr. S. Sreenivasa
Associate Professor and Coordinator
Department of Studies and Research in Chemistry,
Tumkur University, Tumkur -572103, Karnataka (state), India
Cell: +91 96202 30672 (P), +91 94482 33725 (R)
Abstract
Background: Piperazine derivatives are the most privileged structural motifs in the field of nitrogen heterocyclic chemistry. They occur in several natural and synthetic bioactive compounds and are widely used in medicine. Objective: Piperazine with sulfonyl moiety place an important role in showing diverse biological activities. The objective of present study was consisting of synthesis, characterization and biological evaluation of some sulfonyl piperazine derivatives for antimicrobial, anthelmintic and inflammatory activity. Methods: In present studies we describe synthesis of a new substituted sulfonyl piperazine derivatives (8a-j), by coupling 1-[(4-methylphenyl)sulfonyl]piperazine a key intermediate with different substituted benzyl bromide. Synthesized compounds were characterized by using 1H NMR, 13C NMR, IR spectroscopic and CHN elemental analysis and were screened for in vitro antimicrobial action against different bacterial strains and fungal cultures using micro dilution assay and disc diffusion method, anthelmintic activity using test model Pheretima posthuma. Some of the promising molecules were tested for their anti-inflammatory activity by carrageenan induced paw edema against albino wistar rats and hypothetical binding mode are also studied by molecular modeling study. Results: Compounds 8a, 8b, 8c, 8e and 8f showed good antimicrobial activity, compounds 8b, 8c and 8e displayed anthelmintic activity comparable to standard and compounds 8a, 8b and 8f showed demonstrated significant anti-inflammatory activity. Conclusion: Synthesized piperazine sulfonamides in good yield, biologically activity and future pharmacological studies can be done on these structural specific synthesised molecules and QSAR studies.
Keywords: N-Boc Piperazine, Sulfonamides, Antimicrobial, Anthelmintic, Anti-inflammatory
