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Value of intermediates in drug design – example of novel L-ascorbic acid derivatives

In our search of new hybrids of L-ascorbic acid and diverse pharmacophoric scaffolds as potential anticancer agents, novel conjugates of 1, 2, 3- triazole and L-ascorbic acid are synthesized using Cu(I) catalyzed click reaction (CuAAC) [1, 2]. Herein considered dibenzylated compounds are obtained as intermediates in the synthesis of target derivatives of vitamin C. The library of compounds with reasonable ADME/Tox profile is designed in a way to span physicochemical space by varying a substituent at position R1 of 1, 2, 3- triazole ring and by elimination of C5-OH group and introduction of C4=C5 double bond (Fig. 1).

ascorbic acid ; ADMET ; antiproliferative ; PCA

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