1. Arch Pharm (Weinheim). 2009 Oct;342(10):605-13.

Synthesis and biological evaluation of 2-mercapto-1,3-benzothiazole derivatives
with potential antimicrobial activity.

Franchini C, Muraglia M, Corbo F, Florio MA, Di Mola A, Rosato A, Matucci R, Nesi
M, van Bambeke F, Vitali C.

Department of Pharmaceutical Chemistry, University of Bari, Bari, Italy.

The enhancement of bacterial resistance of pathogens to currently available
antibiotics constitutes a serious public health threat. So, intensive efforts are
underway worldwide to develop new antimicrobial agents. To identify compounds
with a potent antimicrobial profile, we designed and synthesized low molecular
weight 2-mercaptobenzothiazole derivatives 2a-2l and 3a-3l. Both series were
screened for in-vitro antibacterial activity against the representative panel of 
Gram-positive and Gram-negative bacteria strains. The biological screening
identified compounds 2e and 2l as the most active ones showing an interesting
antibacterial activity with MIC values of 3.12 microg/mL against Staphylococcus
aureus and 25 microg/mL against Escherichia coli, respectively. The replacement
of the S-H by the S-Bn moiety resulted in considerable loss of the antibacterial 
action of the 3a-3l series. The antibiotic action of compounds 2e and 2l was also
investigated by testing their activity against some clinical isolates with
different antimicrobial resistance profile. Moreover, the involvement of the NorA
efflux pump in the antibacterial activity of our molecules was evaluated.
Finally, in this paper, we also describe the cytotoxic activity of the most
interesting compounds by MTS assay against HeLa and MRC-5 cell lines.

PMID: 19753564 [PubMed - indexed for MEDLINE]