Synthesis of a Series of Diaminoindoles

[Image: see text] A selection of 3,4-diaminoindoles were required for a recent drug discovery project. To this end, a 10-step synthesis was developed from 4-nitroindole. This synthesis was subsequently adapted and used to synthesize 3,5-; 3,6-; and 3,7-diaminoindoles from the corresponding 5-, 6-, or 7-nitroindole. These novel intermediates feature orthogonal protecting groups that allow them to be further diversified. This is the first reported synthesis of these types of compounds

Human monocyte heat shock protein 72 responses to acute hypoxic exercise after 3 days of exercise heat acclimation

The aim of this study was to determine whether short-term heat acclimation (STHA) could confer increased cellular tolerance to acute hypoxic exercise in humans as determined via monocyte HSP72 (mHSP72) expression. Sixteen males were separated into two matched groups. The STHA group completed 3 days of exercise heat acclimation; 60 minutes cycling at 50% V˙O2peak in 40°C 20% relative humidity (RH). The control group (CON) completed 3 days of exercise training in 20°C, 40% RH. Each group completed a hypoxic stress test (HST) one week before and 48 hours following the final day of CON or STHA. Percentage changes in HSP72 concentrations were similar between STHA and CON following HST1 (P=0.97). STHA induced an increase in basal HSP72 (P=0.03) with no change observed in CON (P=0.218). Basal mHSP72 remained elevated before HST2 for the STHA group (P0.05). Percent change in mHSP72 was lower after HST2 in STHA compared to CON (P=0.02). The mHSP72 response to hypoxic exercise was attenuated following 3 days of heat acclimation. This is indicative of improved tolerance and ability to cope with the hypoxic insult, potentially mediated in part by increased basal reserves of HSP72

Properties of charmonium in lattice QCD with 2+1 flavors of improved staggered sea quarks

We use the dynamical gluon configurations provided by the MILC collaboration in a study of the charmonium spectrum and psi leptonic width. We examine sea quark effects on mass splitting and on the leptonic decay matrix element for light masses as low as m_s/5, while keeping the strange quark mass fixed and the lattice spacing nearly constant.Comment: Lattice2003(heavy

The impact of submaximal exercise during heat and/or hypoxia on the cardiovascular and monocyte HSP72 responses to subsequent (post 24 h) exercise in hypoxia

Background: The aims of this study were to describe the cellular stress response to prolonged endurance exercise in acute heat, hypoxia and the combination of heat and hypoxia and to determine whether prior acute exposure to these stressors improved cellular tolerance to a subsequent exercise bout in hypoxia 24 h later. Methods: Twelve males (age 22 ± 4 years, height 1.77 ± 0.05 m, mass 79 ± 12.9 kg, VO2 max 3.57 ± 0.7 L · min-1) completed four trials (30-min rest, 90-min cycling at 50% normoxic VO2 max) in normothermic normoxia (NORM; 18°C, FIO2 = 0.21), heat (HEAT; 40°C, 20% RH), hypoxia (HYP; FIO2 = 0.14) or a combination of heat and hypoxia (COM; 40°C, 20% RH, FIO2 = 0.14) separated by at least 7 days. Twenty-four hours after each trial, participants completed a hypoxic stress test (HST; 15-min rest, 60-min cycling at 50% normoxic VO2 max, FIO2 = 0.14). Monocyte heat shock protein 72 (mHSP72) was assessed immediately before and after each exercise bout. Results: mHSP72 increased post exercise in NORM (107% ± 5.5%, p > 0.05), HYP (126% ± 16%, p

D_s spectrum and leptonic decays with Fermilab heavy quarks and improved staggered light quarks

We present preliminary results for the D_s meson spectrum and decay constants in unquenched lattice QCD. Simulations are carried out with 2+1 dynamical quarks using gauge configurations generated by the MILC collaboration. We use the ``asqtad'' a^2 improved staggered action for the light quarks, and the clover heavy quark action with the Fermilab interpretation. We compare our spectrum results with the newly discovered 0+ and 1+ states in the D_s system.Comment: 3pp. Presented at 21st International Symposium on Lattice Field Theory (LATTICE 2003), Tsukuba, Ibaraki, Japan, 15-19 Jul 200