In order to prepare new antiepileptic drugs with a broader clinical application and lower toxic side effects, we have employed esterification and condensation reactions (we call it Niche Chemistry) to reduce the use of valproic acid as the target molecule. In combination with the study of a broad-spectrum of novel anticonvulsants, we have synthesized two valeric acid derivative compounds [(4-acetamidophenyl 2-propylvalerate (1), and (E)-5-(4-((2-propylpentanoyl)oxy)styryl)-1,3-phenylene bis(2-propylvalerate) (2) by an esterification reaction. The maximum shock seizure test for products 1 and 2 has been successfully carried out, and their cytotoxic activity and survival effects have also been carefully investigated.
As part of our research program into pharmacologically valuable compounds and chelating agents for transition metal ions, novel 8‐cyclo‐1,5,3,7‐diazadiphosphocines (5–16) were successfully synthesized in good yields via [4 + 2] cycloaddition reaction between 8‐cyclo‐1,5,3,7‐diazadiphosphocines (4a‐c) with dienophiles (dimethyl acetylenedicarboxylate [DMAD], diethyl acetylenedicarboxylate [DEAD], diethyl diazene‐1,2‐dicarboxylate [DEDAD], and diisopropyl diazene‐1,2‐dicarboxylate [DIPDAD]). The core precursor scaffolds (4a‐c) were prepared via a one‐pot reaction between heteroaromatic amine analogs (1a‐c), paraformaldehyde and hypophosphorous acid in the presence of 6 M HCl. The biological activity of all synthesized 8‐cyclo‐1,5,3,7‐diazadiphosphocines (4a‐c, and 5–16) was evaluated against several cancer cell lines.
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