Endocrine disrupting chemicals (EDCs) are of great concern given their potential influence
on the endocrine system. In silico methods for the evaluation of EDCs have been widely …

This chapter will discuss the recent literature of macrocycles and drug-like property space
moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this …

Synthetic glucocorticoids (GC) are essential for the treatment of a broad range of
inflammatory diseases. However, their use is limited by target related adverse effects on, eg …

The clinical success of linezolid for treating Gram-positive infections paired with the high
conservation of bacterial ribosomes predicts that if oxazolidinones were engineered to …

The mechanism-based risk for hyperkalemia has limited the use of mineralocorticoid
receptor antagonists (MRAs) like eplerenone in cardio-renal diseases. Here, we describe …

Macrocyclic compounds are of growing interest as a new class of therapeutics, especially as
inhibitors binding to protein–protein interfaces. As molecular modeling is a well-established …

A novel series of morpholine-based nonsteroidal mineralocorticoid receptor antagonists is
reported. Starting from a pyrrolidine HTS hit 9 that possessed modest potency but excellect …

A one-pot synthesis of functionalized N-trifluoromethyl pyrazoles from readily available di-
Boc trifluoromethylhydrazine and dialdehydes, diketones, carbonylnitriles, and …

Macrocycles are interesting molecules with unique features due to their conformationally
constrained yet flexible ring structure. This characteristic poses a difficult challenge for …

Dianionic cyano-aci-nitroacetate affords 3-cyanoisoxazol (in) es upon heating with a range
of dipolarophiles in the presence of hydrochloric acid. In this reaction, nitroacetonitrile is …