A series of dispiro-cycloalkanones were synthesized using the ''Corey Chaykovsky'' reaction of a,a 0 -(E,E)-bis(benzylidene)-cycloalkanones/methanone in good yields. The compounds were evaluated for their in vitro antituberculosis activity against M. tuberculosis H37Rv and screened in silico. Some selected compounds were screened for mycobacterial NAD + -dependent DNA ligase inhibitory activity. Two of the compounds showed good in vitro antitubercular and NAD + -dependent DNA ligase inhibitory activity along with good correlation to in silico results.
Preclinical evaluation of drug-like molecules requires their oral administration to experimental animals using suitable vehicles. We studied the effect of oral dosing with corn oil, carboxymethyl cellulose, dimethyl sulfoxide, and polysorbate-80 on the progression of Mycobacterium tuberculosis infection in mice. Infection was monitored by physical (survival time and body weight) and bacteriological (viable counts in lungs) parameters. Compared with water, corn oil significantly improved both sets of parameters, whereas the other vehicles affected only physical parameters.
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