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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and In Vitro Antimicrobial Activity of Medicinally Important Novel N-alkyl, N-aryl and Urea Derivatives of 1-benzhydryl Piperizine: A Structure-Activity Relationship Study

Author(s): Channapillekoppal Siddegowda Ananda Kumar, Karunakara Murthy, Marlinganadoddi Panchegowda Sadashiva, Mallappanahally Kambappa Vinaya, Naraganahalli Ramegowda Thimmegowda, Salekoppal Boregowda Benaka Prasad, Siddappa Chandrappa and Kanchugarakoppal Subbegowda Rangappa

Volume 6, Issue 2, 2009

Page: [146 - 154] Pages: 9

DOI: 10.2174/157018009787582570

Price: $65


Novel 1-benzhydryl piperazine derivatives 7(a-k) and 8(a-i) were synthesised in order to determine their antimicrobial activity and possible structure-activity relationships to improve the efficacy. Their chemical structures were confirmed by 1H NMR, IR and elemental analysis. All the compounds were screened for their in vitro antibacterial activity against Bacillus subtilis, Escherichia coli and Staphylococcus aureus by using Streptomycin as positive control and antifungal activity against Aspergillus niger, Cephalosporium acremonium and Fusarium moniliforme by using Nystatin as positive control. Among the synthesized novel compounds 7h, 7k, 8g, 8h and 8i showed potent antimicrobial activities compared to the standard drugs. The SAR studies reveals that, both linkage and substituents on phenyl ring are responsible for the antimicrobial activity for these class of agents.

Keywords: 1-benzhydryl piperazine derivatives, alkyl halides, aryl halides, isocyanates, minimum inhibitory concentration, antimicrobials

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