Nontoxic Metal–Cyclam Complexes, a New Class of Compounds with Potency against Drug-Resistant <i>Mycobacterium tuberculosis</i>

Tuberculosis (TB) accounted for 1.5 million deaths in 2014, and new classes of anti-TB drugs are required. We report a class of functionalized 1,8-disubstituted cyclam derivatives that display low micromolar activity against pathogenic mycobacteria. These compounds inhibit intracellular growth of <i>Mycobacterium tuberculosis</i>, are nontoxic to human cell lines, and are active against multidrug-resistant <i>M. tuberculosis</i> strains, indicating a distinct mode of action. These compounds warrant further appraisal as novel agents to control TB in humans

Serpulanines A to C, N‑Oxidized Tyrosine Derivatives Isolated from the Sri Lankan Fungus <i>Serpula</i> sp.: Structure Elucidation, Synthesis, and Histone Deacetylase Inhibition

Serpulanines A (<b>1</b>), B (<b>2</b>), and C (<b>3</b>) have been isolated from extracts of the rare Sri Lankan macrofungus <i>Serpula</i> sp. The structures of <b>1</b>, <b>2</b>, and <b>3</b> were elucidated by a combination of spectroscopic and single-crystal X-ray diffraction analyses. Serpulanines A (<b>1</b>) and B (<b>2</b>) both contain the rare (<i>E</i>)-2-hydroxyimino hydroxamic acid functional group array. A proposed biogenesis for serpulanine B (<b>2</b>) suggests that its (<i>E</i>)-2-hydroxyimino hydroxamic acid moiety arises from a diketopiperazine precursor. Synthetic serpulanine A (<b>1</b>) inhibited class I/II histone deacetylases in murine metastatic lung carcinoma cells with an IC₅₀ of 7 μM

Additional file 4: Figure S2. of Disease progression in idiopathic pulmonary fibrosis with mild physiological impairment: analysis from the Australian IPF registry

Locally Weighted Scatterplot Smoothing curves for FVC% predicted. a. Mild physiological impairment (FVC ≥ 80%). b. Moderate-severe physiological impairment (FVC < 80%). c. Summary of LOWESS curve means. (ZIP 212 kb

Additional file 3: Figure S1. of Disease progression in idiopathic pulmonary fibrosis with mild physiological impairment: analysis from the Australian IPF registry

Exploratory analysis of varying thresholds. (PNG 100 kb

Additional file 2: Table S2. of Disease progression in idiopathic pulmonary fibrosis with mild physiological impairment: analysis from the Australian IPF registry

Baseline characteristics of patients excluded from analysis. (DOC 35 kb

Additional file 1: Table S1. of Disease progression in idiopathic pulmonary fibrosis with mild physiological impairment: analysis from the Australian IPF registry

GAP stage calculation. (DOC 30 kb