Antiurolithiatic Potential of a Series of Phthalimide Derivatives on Calcium Oxalate Crystals.
Daniele Regina Sonza, Laura Von Borell du Vernay França, Rita de Cássia Vilhena da Silva, Anelize Dada, Mariana Zanovello, Thaise Boeing, Priscila de Souza, Rogério Correa
Abstract
Open AccessUrolithiasis, primarily caused by calcium oxalate crystals, represents a major health concern due to high recurrence rates and limitations of current treatments in dissolving existing stones. This study investigated the antiurolithiatic potential of 15 phthalimide derivatives against calcium oxalate monohydrate (COM) and dihydrate (COD) crystals. The compounds were synthesized via condensation of phthalic anhydride with nitrogenous bases and evaluated using urine samples from rats with sodium oxalate-induced crystallization. All derivatives reduced COM crystal formation at one or more concentrations, though only LD-F 03 inhibited COD crystals. Notably, LD-F 10 decreased COM by 89%, whereas LD-F 11 achieved 92% COM inhibition. These results demonstrate the structural versatility of phthalimides and the need to optimize molecular design for selective activity. Overall, phthalimide derivatives show promising antiurolithiatic effects, warranting further studies on pharmacokinetics, safety, and potential combination with current therapies to reduce recurrence and surgical interventions.