Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 5-Chloropicolinaldehyde, is researched, Molecular C6H4ClNO, CAS is 31181-89-2, about In vivo potent BM635 analogue with improved drug-like properties.SDS of cas: 31181-89-2.
Herein an efficient method was reported for the design, synthesis, biol. evaluation, pharmacokinetic anal. as well as in vivo TB mouse efficacy studies of novel (2-methyl-1H-pyrrol-3-yl)methanamines I [R = Me, 4-i-PrC6H4, 4-F3CC6H4, etc.; R1 = i-Pr, cyclohexyl, 4-FC6H4, etc.; R2 = 4-morpholinyl, 3-hydroxy-1-piperidyl, 3-methoxy-1-piperidyl] from 2-methyl-1H-pyrroles, formaldehyde and amines under Mannich reaction conditions. These BM635 analogs I showed improved physicochem. properties and excellent antimycobacterial activity. This hit-to-lead campaign led to the identification of a new compound I [R = 4-i-PrC6H4, R1 = i-Pr, R2 = 4-morpholinyl] that showed excellent activity (MIC = 0.15 μM; SI = 133) against drug-sensitive Mycobacterium tuberculosis strains as well as efficacy in a murine model of TB infection.
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Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate