[Quantitative structure-activity analysis of thiobenzamides].
It is very difficult to meet all prerequisites for the optimization of the tuberculostatic action of thiobenzamides. On the one hand, a strongly polarized C=S bond of the thiocarbamido group is necessary, and on the other hand, the value of the Hammett constant must be positive (to prevent hepatotoxicity). The conjugated system can be extended to reduce the excitation energy of the eta-eta electronic transition. However, the lipophilicity should not be overincreased (to avoid the risk of increased antimitotic activity and acute toxicity). Of the culture media, the Sauton system seems to be best suited since it is the most simple. However, the culture medium according to Sula comes closest to in vivo conditions as it contains proteins and is devoid of surfactants.
D000577:Amides / Q000494:pharmacology*; D000818:Animals; D000995:Antitubercular Agents; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008433:Mathematics; D051381:Rats; D013329:Structure-Activity Relationship; D013854:Thioamides / Q000494:pharmacology* / Q000633:toxicity
D000577:Amides; D000995:Antitubercular Agents; D013854:Thioamides
Quantitative Struktur-Wirkungs-Analyse der Thiobenzamide.