Current Topics in Medicinal Chemistry - Volume 25, Issue 12, 2025

Transient receptor potential vanilloid (TRPV) channels are a member of the TRP superfamily, which consists of six proteins and is expressed in many neuronal and non-neuronal cells. Among them, TRPV1-4 are non-selective cation channels that are highly sensitive to temperature changes, while TRPV5-6 are channels that are highly selective to Ca²⁺. These cation channels have attracted great interest academically, especially from a pharmacological perspective. TRPV channels play a vital role in many physiological processes and can be regulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. The regulation of their activities can lead to a variety of diseases and disorders, such as neurodegenerative diseases, pain, cancer, and skin diseases. In fact, several TRPV1 and TRPV3 modulators have been developed for clinical use. Therefore, the development of TRPV channel modulators has important clinical significance and value. Herein, we focused on and summarized the latest research progress of endogenous and exogenous ligands of six TRPV channels and their pharmacological effects on related diseases.

The development of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs), such as Roxadustat (ROX), Enarodustat (ENA), Desidustat (DES), Vadadustat (VAD), Molidustat (MOL), and Daprodustat (DAP), has significant effects on anemia in chronic kidney disease. This review presents comprehensive information about the synthesis, pharmacology, and analysis of HIF-PHIs across several matrices. The literature has presented several approaches for quantifying HIF-PHIs in diverse sample matrices. Furthermore, HIF-PHIs exhibit similar modes of action, demonstrating distinct pharmacokinetic parameters. The pharmacological insights encompass their half-life, mechanism of action, absorption, distribution, metabolism, excretion, and therapeutic uses. Research indicates that most studies concentrate on hyphenated methodologies for drug estimation in various biological fluids. Consequently, this study assesses the biological efficacy of HIF-PHIs and elucidates the analytical methodologies currently employed for measurement across various matrices.

Ongoing research and development efforts are currently focused on creating COVID-19 vaccines using a variety of platforms. Among these, mRNA technology stands out as a cutting-edge method for vaccine development. There is a growing public awareness of mRNA and its potential in vaccine development. Despite being relatively recent, extensive scientific research has been dedicated to vaccines for a considerable period. mRNA vaccines are created by synthesizing the spike protein from a DNA template. This review delves into the various aspects of these vaccines and thoroughly explores the intricacies of COVID-19 vaccinations. It is essential to choose a reliable, efficient, and widely accessible vaccine to combat COVID-19. However, due to the possibility of virus mutations, developing a dependable and safe vaccine is crucial to prepare for future outbreaks of SARS-CoV-2 variants. Meanwhile, concerns remain regarding the potential risks associated with these vaccines.

Phenyl amino pyrimidine attracts researchers due to its versatile scaffold and medicinal significance. This significant moiety present in the Imatinib contributed to medicinal chemistry. In this manuscript, we reviewed various derivatives of Imatinib containing 2-phenylamino-pyrimidine, which has a variety of roles, especially in the anti-cancer category. This manuscript aims to prepare a scientific report that underscores the novel Imatinib derivatives in the field of chemistry for various activities such as anti-cancer, anti-microbial, and miscellaneous focused on cardiovascular, anti-platelets, and anti-parasitic, etc. Finally, this manuscript may attract researchers for new structure design, and the development of novel phenyl amino pyrimidine scaffolds that are more active and less harmful. We propose a compilation and analysis of around 100 Imatinib derivatives having main chromatophores, such as phenylaminopyrimidine. A large number of researchers are interested in Imatnib-based analogs as they have wide biological potential in the largely developing chemical world of the heterocyclic moiety. The phenylamino pyrimidine moiety became an important moiety for researchers to discover combinational libraries and implement the efforts in search of the lead entities. Phenylaminopyrimidine has been manifesting to be an effective moiety in the current respective disease scenario. It has been discovered that phenylaminopyrimidine and its derivatives have an extensive spectrum of pharmacological potential with numerous applications in academic interest, in the pharmaceutical industry, medicinal chemistry, etc. Imatinib containing phenylaminopyrimidine and its novel synthetic derivatives are a prominent heterocyclic compound class with intriguing use in medicinal chemistry. Thus, in brief, attention should be given to other chemical approaches for synthesizing novel compounds containing phenylaminopyrimidine moiety, hence potentiating their efficacy.