10.1007/s11172-007-0154-5
The research presents a convenient method for synthesizing derivatives of 6H-pyrazolo[1,5-c]pyrimidine-7-thione and 7-aminopyrazolo[1,5-c]pyrimidine from difluoroboron chelate complexes of aroylacetones, amide acetals, and thiosemicarbazide or aminoguanidine. The study builds on previous work involving the synthesis of 5-aroylmethylpyrazoles and their hydrazones from difluoroboron chelate complexes of aroylacetones, amide acetals, and hydrazines. The key chemicals involved in this research include aroylacetones, difluoroboron chelates, amide acetals, thiosemicarbazide, and aminoguanidine. The reactions involve the formation of intermediate chelate complexes, which then undergo cyclization to produce the desired pyrazolo[1,5-c]pyrimidine derivatives. The synthesized compounds are characterized by various spectroscopic techniques, including 1H NMR, 13C NMR, 11B NMR, IR, and mass spectrometry. The study highlights the regioselectivity of the reactions and the potential biological activities of the synthesized pyrazolo[1,5-c]pyrimidines.
10.1016/j.bmc.2009.02.018
The research focuses on the development and evaluation of N-Terminal 2,3-diaminopropionic acid (Dap) peptides as efficient methylglyoxal (MG) scavengers to inhibit advanced glycation endproduct (AGE) formation. The purpose of this study was to address the issue of non-enzymatic glycation of proteins, which leads to the formation of AGEs that are associated with various age-related diseases and complications, including diabetes. The researchers synthesized N-terminal Dap peptides and assessed their ability to prevent protein modifications by MG, a highly reactive α-dicarbonyl compound. The peptides demonstrated a high scavenging potency, as evaluated through various assays including RP-HPLC, SDS–PAGE, and cell viability studies, and were compared to known AGE inhibitors such as aminoguanidine, pyridoxamine, metformin, and carnosine. The study concluded that N-terminal Dap containing dipeptides effectively inhibit the formation of AGEs and may provide a therapeutic potential for decelerating and treating AGE-related diseases. Chemicals used in the process included Dap and various amino acids to synthesize the peptides, as well as MG and other α-dicarbonyl compounds for the assessment of scavenging activity.
