N-Substituted imidazolylzinc chlorides were reacted with 2-bromopyridine in the presence of Pd(PPh3)4 and a two-fold excess of ZnCl2 to afford cross-coupled products in 58–93% yields. Deprotection provided convenient routes to 2- or 4(5)-(2-pyridinyl)imidazoles.

2-(5-Chloro/nitro-1H-benzimidazol-2-yl)-4-bromo/nitro-phenols (HLx; x = 1–4) and their complexes with zinc(II)nitrate have been synthesized and characterized. In the tetrahedral mononuclear complexes, the ligands are bidentate, via the imine nitrogen and the phenolate oxygen atoms. The structur...

d-Ribono-1,4-lactone was treated with ethylamine in DMF to afford N-ethyl-d-ribonamide 8a in quantitative yield. Using this reaction procedure, N-butyl, N-hexyl, N-dodecyl, N-benzyl, N-(3-methyl-pyridinyl)-, N-(2-hydroxy-ethyl)-, and N-(2-cyano-ethyl)-d-ribonamides 8b–h were obtained in quantit...

Orexins play an important role in sleep/wake regulation, and orexin receptor antagonists are a focus of novel therapy for the treatment of insomnia. We identified 27e (TASP0428980) as a potent dual orexin receptor antagonist through the systematic modification of our original designed lead A. We...

Trimeresurus wagleri venom is the most potent inducer of platelet aggregation among the seven Trimeresurus snake venoms tested. By means of CM-Sephadex C-50 column chromatography, T. wagleri venom was separated into 19 fractions. Fraction XVI possessed the strongest aggregating activity and was ...

An antineoplastic factor, dolabellanin C, inducing tumor lysis was purified to apparent homogeneity from the body fluid of the sea hare Dollabella auricularia. Purified dolabellanin C is a glyco-protein of 215 K daltons containing 3 subunits of 70 K daltons. The amino acid sequence of the amino ...

There are currently no clinically available inhibitors of metallo-β-lactamases (MBLs). These enzymes confer resistance to bacteria against a broad range of commonly used β-lactam antibiotics, and are produced by an increasing number of bacterial pathogens. In this study, several thiol derivati...

123I 15-(p-iodophenyl)-3(R,S)-methylpentadecanoic acid (BMIPP) myocardial scintigraphy and exercise stress thallium (Tl)-201 myocardial scintigraphy were performed in 17 patients with hypertrophic cardiomyopathy (HCM) to evaluate the existence of abnormal fatty acid metabolism in the myocardium ...

BackgroundAlthough iodine 123 15-(p-iodophenyl)-3-(R,S) methylpentadecanoic acid (BMIPP) can assess abnormal utilization of fatty acid in the diseased myocardium, the prognostic value of BMIPP imaging at rest in patients with known or suspected coronary artery disease (CAD) remains unclear.

Lack of cell-type specificity and proteolytic susceptibility have long been the major bottlenecks for the development of peptide-based biomaterials for targeted drug delivery. Though a poly-l backbone provides the adaptability to re-conform the peptide structure to bind to a receptor, it also ma...

New ideas and methods are being developed to generate highly designable small functional protein folds beyond the confines of natural structures, from secondary to quaternary level. Highly designable folds can have multiple sequence solutions, which are thermodynamically and kinetically stable. ...

Delivery systems are likely to be central for the translation of antimicrobial peptides (AMPs) towards therapeutics. Addressing AMP interactions with microgel carriers, we here investigate how poly(ethylene glycol) conjugation (‘PEGylation’) of AMPs affect their loading and release to/from mic...

Previous work by others shows that d-limonene (LIM) inhibits carcinogen-induced lung tumorigenesis in mice and strongly suggests that LIM can inhibit the metabolic activation of nitrosamines such as 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK). Thus, in the current study, the ability of ...

As part of a routine screening assay, benzaldehyde was found to inhibit 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) metabolism. Consequently, the effects of benzaldehyde and several structurally related compounds on NNK metabolism were examined in murine hepatic and pulmonary microsomes...

Cigarette smoke is a risk factor for human health, and many studies were conducted to investigate its adverse effects on humans and other mammals. However, since large amounts of cigarette products are produced and consumed, it is possible that tobacco chemicals can end up in aquatic environment...

The potential endogenous nitrosation of nicotine and/or nicotine metabolites has led to speculation on the possible formation of 4-(methylnitrosamino)-4-(3-pyridyl)butyric acid (iso-NNAC) in smokers. A gas chromatographic method with thermal energy analytical detection is described for the deter...

The preparation, spectroscopic and magnetic properties of ML2Cl2 (M=Cu(II), Mn(II), Ni(II)) and [ML3]Cl3 (M=Fe(III), Cr(III)), L=N-4-methoxyphenyl-N-4-chlorobenzoyl hydrazide are reported. In all the studied complexes the N-4-methoxyphenyl-N-4-chlorobenzoyl hydrazide acts as a neutral bidentate ...

The intermediate in the reaction catalysed by 4-chlorobenzoate dehalogenase from Pseudomonas sp. CBS3 was identified as 4-chlorobenzoyl-CoA. One component of 4-chlorobenzoate debalogenase worked as a a 4-chlorobenzoyl-CoA ligase catalysing the formation of 4-chlorobenzoyl-CoA from 4-chlorobenzoa...

Complexes [Zn2(HL1)2(CH3COO)2] (1) and [Zn2(L2)2] (2) were synthesized with salicylaldehyde semicarbazone (H2L1) and salicylaldehyde-4-chlorobenzoyl hydrazone (H2LASSBio-1064, H2L2), respectively. The crystal structure of (1) was determined. Upon recrystallization of previously prepared [Zn2(HL2...

Allosteric enhancers for the A1 adenosine receptor represent a novel and unique drug design strategy to augment the response to endogenous adenosine in a site- and event-specific manner. We have previously investigated a detailed structure–activity relationship study around a wide series of 2-a...