The role of anionic, imidic and amidic forms in structure-activity relationships. Conjugation and bacteriostatic activity in sulphonamides.

The electronic structures of anionic, imidic and amidic forms of sulphonamides were investigated and compared by means of I.R., Raman and U.V. spectroscopy. Indices reflecting the electronic situation of the common moiety p-H2N-C6H4-SO2 was a whole, although not necessarily related, physically, to any event taking place in the biological processes, were found to correlate with the in vitro bacteriostatic activity of the specific individual forms. The influence of N1-substituents both on the SO2 electronic features and on the coupling between the para amino group and the phenyl ring was discussed. It resulted that the most active chemical species, in this class of compounds, are characterized, electronically, by the most electron-rich common moiety and, in particular, by the most negative oxygens in the SO2 group and the most available (less engaged) lone-pair in the rho-amino group. These conclusions give a new settlement both to the problem of resonance and to the relation between resonance effects and bacteriostatic activity in this class of compounds.     

Fixed-interval punishment of running in hamsters

Four hamsters received brief electric shocks contingent upon running in a wheel. The fixed interval between shocks was varied systematically from 0 to 60 sec. Time spent running was directly related to the length of the fixed interval, while running speed remained roughly constant. Running depended on the fixed interval between shocks in the same way as bar-pressing maintained by food reinforcement, despite the fact that running was not established with nor maintained by explicit reinforcement.