Abstract
One major disease of the pupae and the adult bee is the so-called Varroosis that is owing to the bee parasite Varroa destructor. It is an ectoparasite of bees, causing significant losses in the bee population needed for honey production as well as for pollination in agriculture. Costic acid is a sesquiterpene-carboxylic acid present in the plant Dittrichia viscosa. Recent studies by our group have shown that costic acid acts as acaricide against V. destructor. Oxalic acid is also an acaricide commonly used against varroa mites. In spite of its structural simplicity—it is the simplest bicarboxlic acid—it is equipotent to costic acid which consists of a trans-decalin system with three chiral centres. The basic goal of this project was to design and synthesize a hybrid entity, incorporating aspects of both oxalic acid and costic acid that would be more active than the parent compounds. This approach introduces a useful strategy for the preparation of congeners of bioactive compounds and proposes a structural framework for a new series of acaricidal agents.
Highlights
A major disease of the pupae and the adult European bee is Varroosis that is owing to the bee parasite Varroa destructor [1,2]
The compound has been isolated by our group, assayed for its acaricidal activity and found to be active against the bee parasite V. destructor
The fact that α-costic acid, which is the double bond isomer of costic acid acts against varroa, supported the idea that the carbon framework of this bicyclic system might be essential for activity
Summary
A major disease of the pupae and the adult European bee is Varroosis that is owing to the bee parasite Varroa destructor [1,2]. Varroa is an ectoparasite of bees causing significant losses in the bee population that is needed for honey production and for pollinating [3] an estimated $8–$10 billion worth of crops (for a recent commentary on the issue of pollinators, see [4]). Oxalic acid is a natural product that to date is considered one of the most efficient acaricidal agents used against royalsocietypublishing.org/journal/rsos R. Soc. Open Sci. 7: 200612 O OH COOH RR R. H costic acid oxalic acid proposed synthetic analogue. The basic idea on the preparation of the synthetic congener
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