The Ugi four-component reaction (U-4CR) with N-hydroxyimides as a novel carboxylic acid isostere has been reported. This reaction provides straightforward access to α-hydrazino amides. A broad range of aldehydes, amines, isocyanides and N-hydroxyimides were employed to give products in moderate to high yields. This reaction displays N-N bond formation by cyclic imide migration in the Ugi reacti...

Sterols which have been identified in a transplantable preputial gland tumor are lanosterol, 24,25-dihydrolanosterol, 4cr-methylAs-cholestenol, A’-cholestenol, 7-dehydrocholesterol, and cholesterol (preceding paper (2)). Arranged in the above sequence, they suggest a possible pathway for the conversion of lanosterol to cholesterol. The studies presented in this report of acetate incorporation i...

A convenient base-mediated two-step synthesis of cotinine analogs and a one-pot base-free synthesis of iso-cotinine derivatives featuring an Ugi-4CR/cyclization protocol are reported. These approaches exploit the reactivity of the peptidyl position present in the Ugi adducts, allowing the facile construction of the γ-lactam core, as well as the introduction of a N-substituted methyl group into ...

The basic algorithm is derived from the weak-commitment algorithm (WC) of Yokoo [17], which has been shown to outperform breakout and min-conflict backtracking on certain classes of problems. Weakcommitment search is that part of WC which results from removing the learning mechanism; this will be called WC-NL. WC-NL is coupled with learning-by-merging to form the new algorithm WC-NG. Experiment...

Interlocked feedback loops may represent a common feature among the regulatory systems controlling circadian rhythms. The Neurospora circadian feedback loops involve white collar-1 (wc-1), wc-2, and frequency (frq) genes. We show that WC-1 and WC-2 proteins activate the transcription of frq gene, whereas FRQ protein plays dual roles: repressing its own transcription, probably by interacting wit...

Two syntheses of natural viridic acid, an unusual triply N-methylated peptide with two anthranilate units, are presented. The first one is based on peptide-coupling strategies and affords the optically active natural product in 20% overall yield over six steps. A more economical approach with only four steps leads to the similarly active racemate by utilizing a Ugi four-component reaction (Ugi-...

The effect of coherency WC/Co phase boundaries on the fracture toughness of the nanocrystalline WC-Co cemented carbides is studied by MD simulation method. The simulation results show that the nanocrystalline WC-Co cemented carbides with coherency WC/Co phase boundaries has higher fracture toughness than that without coherency WC/Co phase boundaries. Moreover, the mechanism of why coherency WC/...

AIM To compare the maximal power output (MPO) of subjects presenting a central adiposity to those of controls and to study the links between plasma leptin or indices of insulin sensitivity (QUICKI) and physical fitness (PF). METHODS MPO was determined for 169 middle-aged men divided into two groups according to waist circumference (WC- < 94 cm, WC+ ≥ 94 cm) each subdivided in two subgroups wi...