First, we synthesized three model amides 73-75 (see SI p. S65-S66; Figure ) to see the impact of the replacement of the hydrogen atom (73) with the methoxy (74) and the methyl sulfone (75) groups at the lipophilicity. We used two parameters: calculated (clogP) and experimental (logP) lipophilicities. According to both parameters, clogP and logP, replacement of the hydrogen atom (73) with the methoxy group (74) had a small effect at the lipophilicity. At the same time, an analogous replacement with the MeSO2-substituent (75) led to a dramatic decrease of lipophilicity by ca. 1.2 logP units.