G. Trapani et al., SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME YL-2-ACYLALKYLIDENE-2,3-DIHYDRO-1,3-BENZOTHIAZOLES, Arzneimittel-Forschung, 44-2(8), 1994, pp. 969-971
Several N-alkenyl-2-acylalkylidene-2,3-dihydro-1,3- benzothiazoles (4)
were synthesized and tested for in vitro antibacterial activity again
st different Gram-positive and Gram-negative bacteria. Compounds 4 wer
e also tested for antifungal activity against Saccharomyces cerevisiae
. The findings clearly showed that all the compounds 4 were devoid of
antifungal activity, whereas errs the compounds 4i-m,o-r were effectiv
e against the bacterial strains used. Compounds 4k,m,p,q proved to be
the most active antibacterial agents showing in some cases minimum inh
ibitory concentrations (MIC) lower than chloramphenicol and gentamicin
, used as reference compounds. In the case of two representative bacte
rial strains (Gram-positive and Gram-negative, respectively), a parabo
lic relationship was found between the antibacterial activity of compo
unds 4i-m,o-r expressed as log1/MIC and the molecular lipophilicity me
asured as R(M) values.