Design and synthesis of an indol derivative as antibacterial agent against .

Several indole derivatives with antibacterial activity have been prepared using different protocols; however, some require special reagents and conditions. The aim of this study involved the synthesis of some indole derivatives using estrone and OTBS-estrone as chemical tools. The synthesis of the indole derivatives involves reactions such as follows: (1) synthesis of two indol derivatives ( or ) by reaction of estrone or OTBS-estrone with phenylhydrazine in medium acid; (2) reaction of or with 6-cloro-1-hexyne in medium basic to form two hexynyl-indol ( or ); (3) preparation of indol-propargylic alcohol derivatives ( or ) by reaction of benzaldehyde with or in medium basic; (4) synthesis of indol-aldehydes ( or ) via oxidation of or with DMSO; (5) synthesis of indeno-indol-carbaldehyde ( or ) via alkynylation/cyclization of or with hexyne in presence of copper(II); (6) preparation indeno-indol-carbaldehyde complex ( or ) via alkynylation/cyclization of or with 1-(hex-5-yn-1-yl)-2-phenyl-1-imidazole. The antibacterial effect exerted by the indol-steroid derivatives against and bacteria was evaluated using dilution method and the minimum inhibitory concentration (MIC). The results showed that only the compound inhibit the growth bacterial of . In conclusion, these data indicate that antibacterial activity of can be due mainly to functional groups involved in the chemical structure in comparison with the compounds studied.