Late Stage Lead Diversification (LSLD) Coupled with Quantitative NMR Spectroscopy to Identify New SAR Vectors at Nanomole Scale Synthesis: Application to Loratadine a Human Histamine H1 Receptor Inverse Agonist.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00483
Abstract: An experimental approach is described for late stage lead diversification (LSLD) of frontrunner drug candidates using nanomole scale amounts of lead compounds for SAR development. The process utilizes C-H bond activation methods to explore chemical… read more here.
Keywords: late stage; diversification lsld; lead diversification; stage lead ... See more keywords
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00116
Abstract: In this report, we describe a method whereby lead molecules can be converted into several new analogues each using liver microsomes. Less than one micromole of substrate is incubated with liver microsomes (mouse, rat, hamster,… read more here.
Keywords: lead diversification; phosphodiesterase; using liver; spectroscopy ... See more keywords