Synthesis of (E)- and (Z)-fluoro-olefin analogues of potent dipeptidyl peptidase IV inhibitors

(E)- and (Z)-fluoro-olefin analogues of potent dipeptidyl peptidase IV inhibitors were synthesized. A Wadsworth-Horner-Emmons reaction, followed by amide formation and reduction of the amide were used for the construction of the α-fluoro-α,β-unsaturated amine functionality.     

NMR and stereochemical studies of non aromatic heterocyclic compounds—II : 13C and 31P NMR of 2-methoxy-1,3,2-dioxaphosphorinanes

¹³C and ³¹P chemical shift data for eight 2-methoxy-1,3,2-dioxaphosphorinanes are reported. Examination of pairs of geometrical isomers, which differ only in the orientation of the OMe substituent on P^III, have shown that both the ³¹P and the ¹³C signals of C_4,6 atoms appear 3–4 ppm at higher field when the OMe is axial compared with the equatorial isomer. This observation can be associated with the 1–3 syn diaxial interaction between the phosphorus axial substituent and the axial hydrogens on C_4,6 and should thus constitute, in the future, a supplementary tool for the structural analysis of this kind of compound. Important long range δ effects were observed both on ¹³C and especially on ³¹P chemical shifts. It is suggested that the high field δ_e effects could reflect a direct stereoelectronic interaction between the P atom and the cyclic C-5 atom. This interpretation is supported by a study of the ³¹P…¹³C coupling constants and their stereochemical dependence.     

Equitable resolvable coverings

In an earlier article, Willem H. Haemers has determined the minimum number of parallel classes in a resolvable 2‐(qk,k,1) covering for all k ≥ 2 and q = 2 or 3. Here, we complete the case q = 4, by construction of the desired coverings using the method of simulated annealing. Secondly, we look at equitable resolvable 2‐(qk,k,1) coverings. These are resolvable coverings which have the additional property that every pair of points is covered at most twice. We show that these coverings satisfy k < 2q ? , and we give several examples. In one of these examples, k > q. © 2003 Wiley Periodicals, Inc. J Combin Designs 11: 113–123, 2003; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/jcd.10024     

Spectral Characterizations of Some Distance-Regular Graphs

When can one see from the spectrum of a graph whether it is distance-regular or not? We give some new results for when this is the case. As a consequence we find (among others) that the following distance-regular graphs are uniquely determined by their spectrum: The collinearity graphs of the generalized octagons of order (2,1), (3,1) and (4,1), the Biggs-Smith graph, the M ₂₂ graph, and the coset graphs of the doubly truncated binary Golay code and the extended ternary Golay code.     

An odd characterization of the generalized odd graphs

We show that any connected regular graph with d+1 distinct eigenvalues and odd-girth 2d+1 is distance-regular, and in particular that it is a generalized odd graph.     

Skew-adjacency matrices of graphs

The spectra of the skew-adjacency matrices of a graph are considered as a possible way to distinguish adjacency cospectral graphs. This leads to the following topics: graphs whose skew-adjacency matrices are all cospectral; relations between the matchings polynomial of a graph and the characteristic polynomials of its adjacency and skew-adjacency matrices; skew-spectral radii and an analogue of the Perron–Frobenius theorem; and, the number of skew-adjacency matrices of a graph with distinct spectra.     

Thiazolopyridine analogs of nalidixic acid. 2. Thiazolo[4,5-b]pyridines

A series of 2-substituted 4-ethyl-4,7-dihydro-7-oxothiazolo[4,5-b]pyridine-6-carboxylic acids were synthesized. Antibacterial activity was tested in vitro. None of the new compounds prepared showed any interesting antibacterial activity in vitro against the strains tested.     

Graphs cospectral with distance-regular graphs

We determine all graphs with the spectrum of a distance-regular graph with at most 30 vertices (except possibly for the Taylor graph on 28 vertices)     

Study of the enzymatic degradation of vasostatin I and II and their precursor chromogranin A by dipeptidyl peptidase IV using high-performance liquid chromatography/electrospray mass spectrometry

The interaction of dipeptidyl peptidase IV with structurally related proteins differing in chain length, namely vasostatin I and II and their precursor protein chromogranin A, was examined using high-performance liquid chromatography in combination with electrospray mass spectrometry. Suitable analytical procedures were developed involving the use of reversed-phase high-performance liquid chromatography for purification of the enzymatic degradation products and a peptide mapping procedure for evaluating the enzymatic degradation of the large precursor protein chromogranin A. While vasostatin I was found to be a substrate for dipeptidyl peptidase IV, no N-terminal cleavage of Leu-Pro could be noted for chromogranin A. With respect to vasostatin II, N-terminal degradation was only observed after degradation in the C-terminal domain to proteins containing < or = 78 amino acids. The specificity of the N-terminal release of Leu-Pro was proved by addition of a DPP IV specific inhibitor.