Structural characterization of 5-fluorouracil & piperazine new solid forms and evaluation of their antitumor activity

Pharmaceutical cocrystals: A review of preparations, physicochemical properties and applications

“… Therapeutic category API Coformer Ref. Anticancer Tegafur Syringic acid 179 5-Fluorouracil l -Phenylalanine 180 Cinnamic acid 181 Piperazine 182 Gentisic acid 176 3,4-Dihydroxybenzoic acid 176 4-Aminopyridine 176 Hydroquinone 183 Quinoxaline 3-Thiosemicarbano-butan-2-one-oxime 189 Benzotriazole p -Hydroxybenzoic acid 190 Temozolomide Oxalic acid 191 Quercetin Pyrazole 192 Imidazolidinone 192 Baclofen 192 Metformin Dichloroacetate 193 Dabrafenib Ethylenediamine hydrate 194 Berberine Chloride Myricetin 195 Betulinic acid Ascorbic acid 196 Antibacterial Nitrofurantoin Trimethoprim 197 Ciprofloxacin Carvacrol 198 Thymol 198 Sulfathiazole Amantadine hydroch...…”

“…Therefore, massive doses are required to maintain the therapeutic window of FU, with the resulting risk of side effects of drug resistance. Recently, several 5-fluorouracil cocrystals with the enhanced anticancer bioactivity have been successfully prepared with coformers, such as l -phenylalanine 180 , cinnamic acid 181 , piperazine 182 , gentisic acid 176 , 3,4-dihydroxybenzoic acid 176 , 4-aminopyridine 176 and hydroquinone 183 . For instance, the cocrystal of 5-fluorouracil‒ l -phenylalanine (FU‒PHE) exhibited greater anticancer activity in comparison with the individual components ( Fig.…”

Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim

“…According to previous research, co-crystals are a new solid form designed using the principles of crystal engineering and supramolecular chemistry, which can significantly improve the physicochemical properties and bioavailability of drugs and are suitable for non-dissociated and weakly dissociated drugs. − Therefore, co-crystallization is an effective way to improve drug molecules’ physicochemical properties; it can improve the physicochemical properties of active pharmaceutical ingredients (API), increase their bioavailability, and even extend the life of API without affecting their original biological activity. − For 5-fluorouracil, after the formation of co-crystals between 5-fluorouracil and bipyridine, nicotinamide, piperazine, hydroquinone, etc., its anticancer activity, solubility, drug selectivity, and membrane permeability were all obtained in different degrees of improvement. − For trimethoprim, the physicochemical properties improved after the formation of the co-crystals; it has been reported that the solubility and antibacterial activity of nitrofurantoin and trimethoprim are significantly enhanced after the formation of co-crystals. , …”

Research progress of piperazine and morpholine derivatives in the discovery of agricultural chemicals

“…In addition, the two nitrogen atoms of piperazine are basic, which improves water solubility [3] and may increase its conductivity in plants. The biological activities of piperazine derivatives have been widely reported in medicine, such as antitumor [4], antibacterial [5,6], anti-inflammatory [7], antioxidant [8], anti-tuberculosis [9], and other activities [10,11]. In the research and development of pesticides, the effective grafting of active groups can significantly improve the biological activity, which is the key to discovering highly active agrochemical candidates [12][13][14][15][16].…”