Efficient Synthesis of Acyclic and Cyclic Pyrazoles for Evaluation as Antiviral nsp2 Protease Inhibitors

Pyrazole (E)-vinyl sulfone 3 was identified as a potential covalent CHIKV nsp2 protease inhibitor from a high throughput screen in the READDI Antiviral Drug Discovery Center at UNC.1 Initial re-synthesis of the hit compound yielded a mixture of acyclic (3) and cyclic sulfones (4) (Scheme 1), which were identified by 1D and 2D NMR, but Read More …

AViDD Filters: Compound Filtering SOP for Hit to Lead

High throughput screening (HTS) is a powerful technique for identifying potential drug candidates from large libraries of compounds. However, many compounds that show activity in HTS are false positives or may not be suitable for further development. Therefore, it is important to apply various filters to eliminate compounds that have undesirable properties, such as poor Read More …

PLCζ1: a promising target for non-hormonal contraceptives

The Structural Genomics Consortium (SGC) has been funded by the Bill & Melinda Gates Foundation to research Women’s and Children’s Health, focusing on the advancement of drug discovery in reproductive biology and disease, child development, and childhood diseases. The SGC plans to generate protein reagents and chemical probes for several potential drug targets for new, Read More …

PATL2: A Potential Contraceptive Target August 2023 Update

PATL2: A Potential Contraceptive Target A promising protein target for NHCs is Protein Associated with Topoisomerase II Homolog 2 (PATL2), a highly conserved, oocyte-specific mRNA-binding protein that represses translation1. For consanguineous families, the inheritance pattern for PATL2 is recessive; thus, infertility is often caused by homozygous mutations in the gene2. Although some mutations in PATL2 Read More …