Current Medicinal Chemistry - Volume 23, Issue 18, 2016

In this review we discuss drug design strategies directed to the development of potential anti-influenza A(H1N1) inhibitors of M2 ion channel, neuraminidase (NA), hemagglutinin (HA) and RNA-dependent RNA-polymerase complex (RdRp) major targets, following temporal chronology of their findings. Besides searching for new chemotypes, eventually active against new targets of influenza A (H1N1), the design of optimiz Read More

The development of reversibly binding radioligands for imaging brain proteins in vivo, such as enzymes, neurotransmitter transporters, receptors and ion channels, with positron emission tomography (PET) is keenly sought for biomedical studies of neuropsychiatric disorders and for drug discovery and development, but is recognized as being highly challenging at the medicinal chemistry level. This article aims to compile a Read More

The histamine H4 receptor has stood out since its discovery and identification in 2000 as an important target in the search for potential new drugs for the treatment of inflammatory and allergic diseases such as rhinitis, pruritus and asthma. Thus, in the last decade, both industry and academia have performed an intensive and productive search for new ligands of this newest subtype of histamine receptor. The most promising c Read More

Atherosclerosis is driven by inflammation, with a strong involvement of innate immunity, and involves an expansion of the arterial intima, a normally small area composed of several cell types including smooth muscle cells, lipids, monocytes, macrophages, dendritic cells, and extracellular matrix. Macrophages derived from recruited monocytes are predominant innate immune cells that play crucial roles in the Read More