Publications by authors named "D S Kalinin"
This study presents a novel series of -acylated 1,2,4-triazol-5-amines and 1-pyrazol-5-amines, featuring a pyrazin-2-yl moiety, developed as covalent inhibitors of thrombin. These compounds demonstrated potent inhibitory activity, with derivatives and achieving IC values as low as 0.7 and 0.
View Article and Find Full Text PDFThe P2X4 receptor (P2X4R), a ligand-gated ion channel activated by ATP, plays a critical role in neuroinflammation, chronic pain, and cancer progression, making it a promising therapeutic target. In this study, we explored the design and synthesis of piperazine-based P2X4R antagonists, building on the structural framework of paroxetine. A series of over 35 compounds were synthesized to investigate structure-activity relationships (SARs) in a Ca²⁺-flux assay for P2X4R antagonistic activity.
View Article and Find Full Text PDFHead and neck paragangliomas (HNPGLs) are rare neoplasms that, along with pheochromocytomas and extra-adrenal paragangliomas, are associated with inherited mutations in at least 12 susceptibility genes in approximately 40% of cases. However, due to the rarity of HNPGLs, only a series of small-scale studies and individual cases have reported mutations in additional genes that may be involved in tumorigenesis. Consequently, numerous disease-causing mutations and genes responsible for the pathogenesis of HNPGLs remain poorly investigated.
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- - The filamentous fungus produces meroterpenoid secondary metabolites, including compounds that can be transformed into isoindolinones using primary amines, revealing their potential for semi-synthetic modification.
- - This study focuses on the reaction of acetoxystachybotrydial acetate with l-tryptophan and tryptamine, discovering rare isomeric structures and investigating their unique behaviors through various analytical techniques.
- - The compounds were assessed for biological activities, including cytotoxicity and metabolism, where one isomer demonstrated lower cytotoxicity, faster metabolism, and higher activity compared to the original substance, highlighting the potential for further research and application.
In recent years, there has been an increase in the incidence of gastroesophageal reflux disease (GERD) in the elderly not only in our country, but also worldwide. In this regard, the issues of early diagnosis and development of an individualized approach to the treatment of this disease are of particular relevance. When addressing these issues, it is necessary to take into account a number of features in patients of older age groups, which include polymorbidity and polypharmacotherapy in combination with anatomical, physiological and functional age-related changes.
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