Botulinum neurotoxins (BoNTs) are among the most deadly poisons known, though ironically, they also are of great therapeutic utility. A number of research programs have been initiated to discover small molecule inhibitor...
Synthesis of a strict structural analogue of albaconazole in which the quinazolinone ring is fused by a thiazole moiety led to the discovery of a new triazole with broad-spectrum antifungal activity. Compound I exhibited...
High-throughput screening and subsequent hit optimization identified 1-piperidinyl-benzimidazoles, exemplified by compound 1, as TRPV4 inhibitors. Lead optimization identified potent TRPV4 blocker 19, which has good targ...
The indenopyrazole framework was investigated as a new class of HIP-la inhibitors. Indenopyrazole 21 was found to most strongly inhibit the hypoxia-induced HIF-1 alpha transcriptional activity (IC50 = 0.014 mu M) among a...
Oligodeoxynucleotides (ODNs) containing a CpG or certain synthetic dinucleotides, referred to as immune-stimulatory dinucleotides, induce Toll-like receptor 9 (TLR9)mediated immune responses. Chemical modifications such ...
Two homogeneous high-throughput assays, AlphaScreen and fluorescence polarization, were established to quantify inhibitor selectivity between different protein-protein complexes. As a first case study, they have been suc...