An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

The field of asthma has undergone a dramatic change in recent years. Advances in our
understanding of type 2 airway inflammation have driven the discovery of monoclonal …

Leukotrienes are potent immune-regulating lipid mediators with patho-genic roles in
inflammatory and allergic diseases, particularly asthma. These autacoids also contribute to …

Inflammation is a multifaceted biological process in which the conversion of arachidonic acid
to eicosanoids, including prostaglandins and leukotrienes (LTs), plays a crucial role. 5 …

Lipoxygenases (LOX) transform arachidonic acid (AA, C20: 4) and docosahexaenoic acid
(DHA, C22: 6) into bioactive lipid mediators (LMs) that comprise not only pro-inflammatory …

Atherosclerosis is one of the most important problems of modern medicine as it is the
leading cause of hospitalizations, disability, and mortality. The key role in the development …

The cytosolic metalloenzyme leukotriene A4 hydrolase (LTA4H) is the final and rate-limiting
enzyme in the biosynthesis of pro-inflammatory leukotriene B4 (LTB4). Preclinical studies …

Pyrazoles are ubiquitous structures in medicinal chemistry. We report the first regioselective
route to C3-hydroxyarylated pyrazoles obtained through reaction of pyrazole N-oxides with …

Herein, we disclose the unique physical properties of diethanolamine (DEA) boronic esters
that have facilitated the development of a simple and standard process for their synthesis …

Cysteinyl leukotrienes are proinflammatory mediators with a clinically established role in
asthma and a human genetic and preclinical role in cardiovascular pathology. Given that …