Arylpiperazine derivatives of isotiazolopyridines of Mannich base type 1a-h exhibited differentiated analgesic activity in pharmacological screening [1].

To explain the observed discrepancy of biological effects within series 1a-h, we studied structure/analgesic activity relationship with a view of determining which geometry and portion of the side chain in molecules are important in an analgesia. In our SAR study we found that the conformation of arylpiperazine substituent and steric as well as substituent effects in its arylpiperazine part may contribute to the pharmacological activity of compounds 1a-h. Basic structural and conformational information were obtained from X-ray investigations and molecular modeling studies [2].

[1]. Malinka W., Karczmarzyk Z., Sieklucka-Dziuba M., Sadowski M., Kleinrok Z., Il Farmaco 2001, 56, 905.

[2]. Karczmarzyk Z., Malinka W., J. Chem. Crystallogr. 2006, in preparation.

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