| 摘要 |
Fluorine-containing molecules include fluorine-18 labeled hydrogen ion indicator molecules and methods of making and using the same. Fluorine atoms incorporated into the indicator molecules provides novel structural modifications to the precursor molecules, shifting the absorbance maxima relative to their non-fluorinated precursor/cogeners. These molecules are useful for non-invasive in vivo measurement of blood volume, blood flow and pH in biological objects. Compounds are functionalized by a radioisotopically enriched fluorine-18 label and indicator molecule with structure derived from triarylmethane derived indicators, such as phenol red, cresol red, cresol purple, thymol blue, bromophenol red, naphthol blue, phenolphthalein, cresolphthalein, thymolphthalein, naphtholphthalein, gentian violet (methyl violet 10B), methyl violet 2B, methyl violet 6B, leucomalachite green (malachite green), brilliant green, pararosaniline, fuchsines, or salts thereof. During its radioactive decay, fluorine-18 produces high-energy positrons, which can be detected by positron emission tomography (PET) or single photon emission computer tomography (SPECT). |
| 主权项 |
1. A compound having a structure of Formula I, II, III, or IV, or a salt thereof:wherein
X1 and X2 are independently, at each occurrence, hydrogen or fluorine; R1, R2, R3, and R4, are independently, at each occurrence, hydrogen, optionally substituted C1-6 alkyl; optionally substituted C3-6 cycloalkyl, optionally substituted C2-6 alkenyl; optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroalkyl, optionally substituted heteroaryl, or halo; X3 and X4 are independently, at each occurrence, hydrogen, fluorine, bromine, chlorine, iodine, optionally substituted C1-6 alkyl; optionally substituted C3-6 cycloalkyl, optionally substituted C2-6 alkenyl; optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroalkyl, or optionally substituted heteroaryl; provided at least one of X1, X2, X3, and X4 is fluorine; wherein where present, the fluorine is either present at its natural abundance of isotopes at each occurrence or is statistically enriched in the radioisotope 18F above its natural isotopic abundance relative to the 19F isotope at each occurrence. |
