MDL 62208, MDL 62211, and MDL 62873 are three semisynthetic amide derivatives of teicoplanin (MDL 62208 is an amide of teicoplanin aglycone, MDL 62211 is an amide of the teicoplanin A2 complex, and MDL 62873 is the corresponding derivative of peak A2-2 of the complex). The three semisynthetic glycopeptides were evaluated for in vitro antibacterial activity in comparison with the parent drug (te...

In the title compound, [CdCl2(C13H12N4S)]·CH3OH, the coord-ination geometry of the Cd(II) ion is slightly distorted square-pyramidal, as indicated by the τ index of 0.36 (8). The S atom, two N atoms from the pyridyl-azomethine moiety and one of the Cl atoms comprise the basal plane, while the other Cl atom occupies the apical position. The hydrazinecarbo-thio-amide moiety adopts an E conformati...

Two independent but virtually identical mol-ecules comprise the asymmetric unit of the title compound, [Sn(C(3)H(6)NO)I(3)]. The CI(3)O coordination geometry around the Sn(IV) atom is defined by a chelating carbamoylethyl ligand (C(1),O-bidentate) and three I atoms, and is based on a distorted trigonal bipyramid with the carbonyl O atom occupying a position trans to one of the I atoms which for...

The chiral β -diketimine ligand [(S)-Ph(Me)CH-N=C(Me)]CH2was prepared by condensation of acetylacetone with the commercially available chiral building block (S)-Ph(Me)CH-NH2. Reaction of bis(o-Me2N-α-Me3Si-benzyl)calcium with this β -diketimine led to double deprotonation. Reaction of bis(o-Me2N-α-Me3Si-benzyl)calcium with the commercially available chiral bis-oxazoline (S)-Ph-BOX gave diastere...

Using bis(amide) Zn(HMDS)2 (HMDS = 1,1,1,3,3,3-hexamethyldisilazide) as a precursor, this study explores the synthesis of N-heterocyclic carbene stabilized mixed amido-hydride zinc complexes using two alternative hydride sources, namely dimethylamine borane (DMAB) and phenylsilane PhSiH3. Hydride-rich zinc cluster Zn4(HMDS)2H6·2IPr () (IPr = 1,3-bis(2,6-di-isopropylphenyl)imidazol-2-ylidene), w...

Pulmonate snails have a more complex array of cardioexcitatory peptides than other molluscs, and Helix has a more complex array than most other pulmonates. Since a full characterisation of the cardioexcitatory peptides is necessary for an understanding of physiology, we sought to identify the members of two families of such peptides - the small cardioactive peptides (SCPs) and the FMRFamide-rel...

Two new magnesium complexes containing the important utility amide 2,2,6,6tetramethylpiperidide (TMP) have been synthesised. Treating the magnesium bis(alkyl) reagent (Me3SiCH2)2Mg with a molar equivalent of TMP(H) in hydrocarbon medium produces the dimeric alkylmagnesium amide complex [(Me3SiCH2)Mg(μ-TMP)]2 2, which was isolated in high yield. X-ray crystallography revealed that 2 was an unsym...

Molecular dynamics simulations using a combined QM/MM potential have been performed to study the catalytic mechanism of human cathepsin K, a member of the papain family of cysteine proteases. We have determined the two-dimensional free energy surfaces of both acylation and deacylation steps to characterize the reaction mechanism. These free energy profiles show that the acylation step is rate l...

Glucagon-like peptide 1 (GLP-1) lowers glycemia by modulating gastric emptying and endocrine pancreatic secretion. Rapidly after its secretion, GLP-1-(7-36) amide is degraded to the metabolite GLP-1-(9-36) amide. The effects of GLP-1-(9-36) amide in humans are less well characterized. Fourteen healthy volunteers were studied with intravenous infusion of GLP-1-(7-36) amide, GLP-1-(9-36) amide, o...

Rat ear cartilage was studied using Fourier transform-infrared (FT-IR) microspectroscopy to expand the current knowledge which has been established for relatively more complex cartilage types. Comparison of the FT-IR spectra of the ear cartilage extracellular matrix (ECM) with published data on articular cartilage, collagen II and 4-chondroitin-sulfate standards, as well as of collagen type I-c...