The combination of two separate pharmacological agents into a
single molecule is an emerging strategy within medicinal chemistry
and drug discovery.10 The work of Morphy and Rankovic11 and
Hopkins et al.12 has highlighted both the opportunities within this
paradigm, but also the trends towards increased molecular weight
and lipophilicity in multipharmacology ligands when compared to
known oral drugs.13 With these challenges in mind, a small set of
conjugated CQ–astemizole hybrids 5–8 was designed (Fig. 2), the
synthesis and biological evaluation of which are described in this
letter.