There is still a great demand in the clinic for the drugs which can overcome a variety of imatinib resistant ABL mutants. Starting from a type I inhibitor axitinib, which has been reported to overcome ABL-T315I mutant induced resistance, through a structure guided drug design approach and bindin...

Through a structure-guided rational drug design approach, we have discovered a highly selective inhibitor compound 40 (JSH-150), which exhibited an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieved around 300–10000-fold selectivity over other CDK kinase family members. In a...

The structure of a new antibiotic, lactivicin, was determined to be [4S]-2-(4-acetylamino-3-oxo-2-isoxazolidinyl)-5-oxo-tetrahydrofuran-2-carboxylic acid.

A novel antibiotic, lactivicin (LTV), was isolated from the culture filtrates of two bacterial strains by various types of chromatography. LTV exists in aqueous solution as an equilibrium mixture of two epimers in a ratio of about 1:1. The chemical structure of LTV (C10H12N2O7) was determined to...

Aza analogues of lactivicin (1), a recently discovered novel antibiotic, were prepared by an application of our earlier convenient synthesis of 1 and its derivatives. A 1-unsubstituted pyrazolidinone derivative bearing 2-aminothiazol-4-yl-(Z)-methoxyiminoacetyl group exhibited in vitro antibacte...

We re-evaluated 3-bromo-1-trifluoromethanesulfonyloxypropane (3-bromopropyl triflate, 1) as the precursor for the preparation of the fluorine-18 labeled compound 2 by reoptimizing fluorine-18 incorporation reaction conditions (120°C) and developing a method to inactivate the unreacted triflate ...

Thymosin β4 is a 43 amino acid long peptide with an acetylated N-terminal serin that has a high potential as a remedy for healing ulcers, wounds and burns. Although protein biosynthesis offers attractive opportunities in terms of a large-scale production, currently thymosin β4 is mainly produc...

The phthalocyanine dyes are attractive sensitizers for photodynamic therapy of cancer. The light fluence response curves for photocytotoxicity of zinc tetrahydroxyphthalocyanine were constructed using the colony-forming ability of Chinese hamster cells as an end-point. The survival curve of cell...

A series of heterogeneous catalysts with Lewis and Bronsted basic sites, and acid–base bifunctional pairs has been used in order to perform organic reactions. By changing the chemical composition and activation conditions it is possible to have predominantly Lewis or Bronsted base catalysts wit...

The synthesis of 3-cyano-4-oxo-1,2,3,4,5,6-hexahydrobenzo[c]quinolizine (XIV), of 2-carbethoxy-3-oxo-1,2,3,4,5,6-hexahydrobenzo[c]quinolizine(XVII), and of 4-cyano-3-oxo-1,2,3,4,5,6-hexahydrobenzo[c]quinolizine (XXIX) is reported. Attempts to methylate 3-carbethoxy-4-oxo-1,2,3,4,5,6-hexahydroben...

A new, simple and fit for purpose method based on liquid chromatography with UV spectrophotometric detection and post-column derivatisation (LC-UV-PCD) for the determination of semduramicin in poultry compound feed, premixtures and feed additive as well as its discrimination from other coccidios...

A novel liquid chromatography single quadrupole mass spectrometry (LC–MS) method for the determination of the feed additive semduramicin, in poultry feed, was developed and single-laboratory validated. This work was selected as a real case scenario to outline the different steps that may be nee...

A new benzoic semduramicin anhydride (SemBz) was obtained. The new compound and its ability to form complexes with monovalent cations was studied by the ESI mass spectrometry, DFT, 2D NMR and FT-IR spectroscopic methods. The FT-IR spectra indicate that the K+ cation in SemBz complex is localised...

The cross-contamination of non-target feeds with coccidiostats may result in the occurrence of their residues in food of animal origin. To assure food safety, maximum levels (ML) of coccidiostats have been set for both feed and food. However, scientific data are not available on the transfer of ...

Isatoic anhydrides and azaisatoic anhydrides are converted by reaction with 1,4-bis (bromomagnesio) butane and 1,5-bis (bromomagnesio) pentane into the corresponding 1-(o-aminophenyl) cycloalkanols and 1-(2'-amino-3'-pyridinyl) cycloalcanols.

In this paper, we have described the conventional and microwave methods for the synthesis of 1-[2-(2-chloro-6-methyl(3-quinolyl))-5-(4-nitrophenyl)(1,3,4-oxadiazolin-3-yl)]-3-(aryl)prop-2-en-1-ones (4a–l). Through this method, we have observed a decrease in reaction time and a better yield than...

A series of N-substituted and N,N-disubstituted β-amino acids and their derivatives bearing benzenesulfonamide moiety were designed and synthesized in search of compounds that would be high-affinity and selective inhibitors of human carbonic anhydrases (CA). There are 12 catalytically active hu...

Mycobacterium tuberculosis l-alanine dehydrogenase (MTB l-AlaDH) is one of the important drug targets for treating latent/persistent tuberculosis. In this study we used crystal structure of the MTB l-AlaDH bound with cofactor NAD+ as a structural framework for virtual screening of our in-house d...

This study aimed to examine the penetration into and exposure of cefozopran in the pelvic retroperitoneal space exudate of patients undergoing radical hysterectomy and pelvic lymphadenectomy. Cefozopran (1 g) was administered by 1-h infusion after the end of surgery, and venous blood and exudate...

In this study, we first described the two configurations of cephalosporins by cefozopran, then determined their molecular structure and finally evaluated the stability and biological activity of the two configurations. Our results showed that cefozopran existed as two different configurations in...