Influence of Phytase Supplementation at Increasing Doses from 0 to 1500 FTU/kg on Growth Performance, Nutrient Digestibility, and Bone Status in Grower-Finisher Pigs Fed Phosphorus-Deficient Diets.

The objective of the current study is to assess the effects of the inclusion of 6-n phytase to a phosphorous-deficient diet on the growth performance (feed intake, average daily gain, and feed conversion ratio), apparent digestibility of calcium and phosphorus, and bone characteristics of grower-finisher pigs. The experimental diets included a phosphorus-deficient diet containing 0 (negative control), 250, 500, 1000, or 1500 FTU/kg of 6-phytase, and a diet formulated to meet the phosphorus nutrient requirements of pigs (positive control). Pigs were fed the experimental diets from the time they were ~35 kg body weight until they reached slaughter weight of ~110 kg.

Lymphatic transport and lymph node targeting of methotrexate-conjugated PEGylated dendrimers are enhanced by reducing the length of the drug linker or masking interactions with the injection site.

Drug conjugation to dendrimer-based delivery systems has been shown to enhance delivery to the lymphatic system after subcutaneous administration. Dendrimer interaction with components of the interstitium at the injection site, however, may prevent drainage from the injection site. The current study sought to vary the length of a linker employed to conjugate methotrexate (MTX) to a PEGylated dendrimer, in an attempt to reduce MTX interaction with interstitial binding sites and enhance lymphatic drainage.

The discovery of 1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 1.

Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. Compound 1a (9b-(4-chlorophenyl)-1-(4-fluorobenzoyl)-1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-one) was identified as an inhibitor of A and B strains of RSV targeting the fusion glycoprotein. SAR was developed by systematic exploration of the phenyl (R(1)) and benzoyl (R(2)) groups.

An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.

Respiratory infections caused by human rhinovirus are responsible for severe exacerbations of underlying clinical conditions such as asthma in addition to their economic cost in terms of lost working days due to illness. While several antiviral compounds for treating rhinoviral infections have been discovered, none have succeeded, to date, in reaching approval for clinical use. We have developed a potent, orally available rhinovirus inhibitor 6 that has progressed through early clinical trials.

gem-Dihalocyclopropanes as building blocks in natural-product synthesis: enantioselective total syntheses of ent-erythramine and 3-epi-erythramine.

ent-Erythramine ((-)-1), the enantiomer of the alkaloid erythramine, was prepared in 15 steps from known compounds. The first of three pivotal bond-forming steps in the synthesis was a Suzuki-Miyaura cross-coupling reaction of the starting materials to give a bis-silyl ether. The second involved silver(I)-induced electrocyclic ring opening of the gem-dichlorocyclopropane formed in the next step and trapping of the ensuing pi-allyl cation by the tethered nitrogen atom to give, following cleavage of the allyloxycarbonyl protecting group, an approximately 5:6 mixture of the chromatographically separable diastereoisomeric spirocyclic products.