Synthesis And Mesomorphic Properties Of Fluoro And Isothiocyanato Biphenyl Tolane Liquid Crystals

Four series of high birefringence biphenyl tolane liquid crystals having a terminal isothiocyanato or fluoro group were synthesized; their mesomorphic properties were studied by optical polarizing microscopy and DSC. These biphenyl tolane compounds exhibit reasonably low melting points and high birefringence of 0.37-0.49. By using these compounds a eutectic mixture was formulated exhibiting a wide nematic range, high figure-of-merit and low viscosity

Super High Birefringence Isothiocyanato Biphenyl-Bistolane Liquid Crystals

We have designed, synthesized, and evaluated the physical properties of some high birefringence (Δn) isothiocyanato biphenyl-bistolane liquid crystals. These compounds exhibit Δn ∼ 0.7-0.8 at room temperature and wavelength λ= 633 nm. Laterally substituted short alkyl chains and fluorine atom eliminate smectic phase and lower the melting temperature. The moderate melting temperature and very high clearing temperature make those compounds attractive for eutectic mixture formulation. A eutectic mixture based on those compounds was formulated and its physical properties evaluated. The simulated absorption spectra agree reasonably well with the measured results

Pharmacokinetics of the Anti-Human Immunodeficiency Virus Agent 1-(β-d-Dioxolane)Thymine in Rhesus Monkeys▿ †

β-d-Dioxolane-thymine (D-DOT) has potent and selective in vitro activity against several clinically important resistant human immunodeficiency virus (HIV) mutants and is in advanced preclinical development. Therefore, the single-dose intravenous and oral pharmacokinetics of D-DOT were studied with three rhesus monkeys. The pharmacokinetic profiles of D-DOT in serum and urine were adequately described by a two-compartment open pharmacokinetic model. D-DOT was rapidly and almost completely absorbed (absorption rate constant = 2.7 h−1; fraction of oral dose absorbed = 0.82 to 1.06). The average serum beta half-life was 2.16 h. The average central and steady-state volumes of distributions were 0.52 and 1.02 liter/kg of body weight, respectively, and the average systemic and renal clearance values were 0.36 liter/h/kg and 0.18 liter/h/kg. Four or eight percent of administered D-DOT was eliminated in the urine as glucuronide within 8 h after intravenous or oral administration, respectively. D-DOT reached levels in the cerebrospinal fluid in excess of 10 to 20 times the median effective concentration for wild-type HIV and resistant mutants. The potent antiretroviral activity of D-DOT against a lamivudine- and zidovudine-resistant HIV-1 mutant, together with an excellent pharmacokinetic profile for rhesus monkeys, suggest that further development is warranted