Selective 5-HT2C agonists as potential antidepressants.

The antidepressants currently used need improvement, especially in terms of efficacy, relapse rate and onset of action. In this review the clinical and experimental data which support the rationale for 5-HT2C agonists in the treatment of depression are listed. Next, the results obtained with the non-selective 5-HT2C agonists on the market and in clinical development are described. Finally, the preclinical data on the more selective 5-HT2C agonists are summarized. These recent preclinical results reveal a greater potency and effect size compared to fluoxetine, good tolerability and no evidence of tolerance development. Selective 5-HT2C agonists might become innovative drugs for the treatment of depression, panic, obsessive-compulsive disorder (OCD), some forms of aggression and eating disorders.

Influence of N substitution on antimycobacterial activity of ciprofloxacin.

Ciprofloxacin analogs with various substitutions on the piperazine nitrogen were tested against several mycobacteria. In contrast to what has been found with other gram-positive and gram-negative bacteria, alkyl analogs such as N-isopropylciprofloxacin were shown to be significantly more active than ciprofloxacin. MICs of 0.125 microgram/ml against Mycobacterium tuberculosis were found.

The mycobacterial cell-wall as target for antimycobacterial drugs. I--Synthesis and activity of some diphenylalkylanalogues of mycolic acids.

Mycolic acids are 2-alkyl-3-hydroxyfatty acids and are essential parts of the peptidoglycan of mycobacteria. Potential antimetabolites were prepared by substituting a longchain alkylgroup by a diphenylmethylfunction. 3-Oxo esters and 3-hydroxy esters and acids were prepared. The 3-oxo esters showed a slight activity against M. tuberculosis and some atypical mycobacteria.