The proprotein convertases are believed to be responsible for the proteolytic maturation of a large number of peptide hormone precursors. Although potent furin inhibitors have been identified, thus far, no small-molecule prohormone convertase 1/3 or prohormone convertase 2 (PC2) inhibitors have been described. After screening 38 small-molecule positional scanning libraries against recombinant m...

Muurola-4,10(14)-dien-3-one (1), 10-O-acetyl-15-oxo-alpha-cadinol (2), 15-hydroxy-alpha-cadinol (3), 4alpha-hydroxy-5beta-ethoxy-epi-cubenol (4), and 4alpha-hydroxy-5beta-acetoxy-epi-cubenol (5), five new bicyclic sesquiterpenes, have been isolated from the heartwood of Chamaecyparis obtusa var. formosana along with the known compounds epi-cubenol, T-cadinol, T-muurolol, delta-cadinol, and alph...

A variety of novel bicyclic and tricyclic pyrimidine derivatives was obtained via reaction of 6-amino-2-thioxo-1H-pyrimidine-4-one (1) with a different reagents. The antimicrobial and anti-inflammatory activities of some of the synthesized compounds were tested.

2,4:3,5-di-O-methylene-D-glucitol (Glux-diol) was used for the synthesis of poly(butylene 10 succinate) (PBS) copolyesters by melt polycondensation. Glux-diol possess a rigid bicyclic 11 asymmetric structure made of two fused 1,3-dioxane rings and two hydroxyl functions at the end 12 positions. Copolyesters were prepared over the whole range of compositions with molecular 13 weights varying fro...

1-Azabicyclo [1.1.0] butane (ABB) bearing the highly strained bicyclic structure, which is synthetically useful for the preparation of 3-substituted azetidines, was obtained by the cyclization of 2,3-dibromopropylamine hydrobromide derived from inexpensive allylamine only with organolithium compounds and lithium amides. When other bases were employed, such as potassium, sodium, and magnesium sp...

Density Functional Theory (DFT) calculations at the B3LYP/6-31+G∗ level have been performed on 5-thiabicyclo[2.1.1]hex-2-ene S-oxide derivatives. The geometrical and electronic properties of the compounds have been analyzed in order to explain the favored stability of the exo configuration. Isodesmic reactions at the Gaussian-G2 theory yielded the exo conformer as the most stable one. Moreover,...

A comprehensive product study, performed via the turbulent flow chemical ionization mass spectrometry (TF-CIMS) technique, of the primary OH-initiated oxidation of many of the atmospherically abundant aromatic compounds was performed. The bicyclic peroxy radical intermediate, a key proposed intermediate species in the Master Chemical Mechanism (MCM) for the atmospheric oxidation of aromatics, w...