Current Topics in Medicinal Chemistry - Volume 21, Issue 24, 2021

Drug development is a very time, capital, and labor-intensive process. It was anticipated that bringing a novel chemical entity to market would take over a billion dollars and around 14 years [1]. In addition, drug development is characterized by a very high attrition rate both in preclinical and clinical studies. It was reported that only 40% of drug candidates with the most drug-like properties could make their way into clinical tri Read More

Prodrug design is an effective method proven to improve the drug-like properties of a molecule, and it has been widely used in the drug development of various diseases. Due to the complexity of the central nervous system (CNS), the development of CNS drugs has high requirements related to the pharmaceutical, pharmacokinetic, and pharmacodynamic properties of the molecules. Prodrug design has now been wide Read More

Amino acids derived prodrugs emerged as an attractive approach to improve oral delivery of drugs with low solubility and permeability. Conjugation of amino acids with parent drug molecules resulted in several-fold increases in water solubility. Acceptability of the amino acids derived prodrug approach increases day by day to fulfill the different characteristics needed to get the desired pharmacological or therapeutic activity. D Read More

Cancer is the second leading cause of human death after cardiovascular disease, and the most used drugs in clinics are cytotoxic agents. However, these drugs have some inherent disadvantages, such as the risk of toxicity, low selectivity, poor solubility, and so on. To overcome these shortcomings, a variety of drug delivery strategies based on prodrugs have been developed. The application of drug delivery systems ca Read More

Uncaging chemistry catalyzed by transition metals is developed from deprotection reactions and metal-organic catalytic reactions. Also, it has the characteristics of high efficiency, simplicity and rapidity in the living biological system. In the past decade, metal encapsulation systems (such as nanoparticles) and metal complexes have been developed to reveal the reactivity of transition metals (including palladium, ruthenium, a Read More

Biofilms are among the most important causes of nosocomial and recurrent infections as biofilms confer antibiotic resistance to pathogenic bacteria and protect them from the host’s immune system. Thus, it is imperative to investigate effective therapeutic agents to counteract biofilms. As an important signaling molecule, Nitric Oxide (NO) plays a crucial role in various biological and pathological processes. NO could disp Read More

Hydrogen sulfide (H2S), as one of the endogenous gasotransmitters, has shown great potential in treating cardiovascular diseases (CVDs). H2S plays a protective role in CVDs by removing reactive oxygen species (ROS), promoting vasodilation, inhibiting myocardial hypertrophy, preventing thrombosis, and protecting mitochondria. However, there still exist some problems for H2S as drugs such as challenging delivery, uncon Read More