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Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and their Antibacterial and Antiacetylcholinesterase Activity

Author(s):

B. Ramalingeswara Rao*, Mohana Rao Katiki, Kommula Dileep, C. Ganesh Kumar, G. Narender Reddy, Jagadeesh Babu Nanubolu and M. S. R. Murty   Pages 1 - 12 ( 12 )

Abstract:


Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

Keywords:

2-Aminobenzothiazole, Piperazine sulfonamides, Antibacterial activity, Antifungal activity, AChE inhibitory activity

Affiliation:

Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007, Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007, Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007, Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007, Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007, Centre for X-ray Crystallography, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500007, Medicinal Chemistry and Pharmacology Division, Discovery Laboratory, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad-500007



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