ABSTRACT
Novel continuous-flow cascade reactions are developed for producing 1,4-diaryl-disubstituted dipolar γ-carbolines 2 that contain a carboxylate group and their two pentacyclic precursors 6, 7 from hemiindigos 1. The nucleophilic and pro-electrophilic chemistry described is new to the hemiindigos 1, and it led to the discovery of antimycobacterial scaffold characteristic of rimino-type pentacycles 6, 7 and potent drug clofazimine. The new scaffold like clofazimine appears to be useful in developing lead agents active against drug-resistant/dormant TB.
ABSTRACT
We studied high-resolution (1)H nuclear magnetic resonance spectra of the serum and serum albumin from patients with the first episode of schizophrenia and healthy individuals. A relative increase in signal intensities of CH(2) protons in serum LDL and VLDL in schizophrenia was demonstrated. Higher intensities of CH(2) and CH(3) protons of non-esterified fatty acids were found in (1)H nuclear magnetic resonance spectra of serum albumin. These data attest to an essential role of changes in lipid metabolism and changed ligand load of albumin in schizophrenia.
Subject(s)
Protons , Schizophrenia/diagnosis , Serum Albumin/chemistry , Adolescent , Adult , Female , Humans , Lipid Metabolism , Lipoproteins, LDL/chemistry , Lipoproteins, LDL/metabolism , Lipoproteins, VLDL/chemistry , Lipoproteins, VLDL/metabolism , Male , Nuclear Magnetic Resonance, Biomolecular , Protein Conformation , Schizophrenia/metabolism , Serum Albumin/metabolismABSTRACT
Ethyl 4,4-difluoro-4-phenoxyacetoacetate was obtained and studied as a precursor to new heterocyclic compounds. 6-Hydroxypyrimidine, 1,3-dihydro-1,5- benzodiazepin-2-one, quinolin-2-one and 6-hydroxypyrazolo[3,4-b]pyridine derivatives containing phenoxydifluoromethyl groups were synthesized. These results make it possible to introduce aryloxydifluoromethyl substituents for the design of biologically active heterocycles.
