The synthesis of a new series of 1β-methylcarbapenems having methoxyimine and substituted sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was inves...

Fifteen novel (E)-α-(methoxyimino)-benzeneacetate derivatives, the analogues of strobilurins, which contain two pharmacophoric substructures of (E)-methyl methoxyiminoacetate moiety and 1,3,4-oxadiazole ring were stereoselectively synthesized. It was first found that the coupling reaction could...

(E)-α-(Methoxyimino)-2-[1-(aryloxy)methyl] -benzeneacetates, the analogues of Kresoxim-methyl, were stereoselectively synthesized with the coupling reaction of 2-methylphenyldiazonium chloride and methyl 2-hydroxyiminoacetate in the presence of CuSO4/Na2SO3 as a key step, and it was first found...

The title 2-(methoxyimino)benzen-1-ones react with α-alkylethoxycarbonylmethylene(triphenyl)phosphoranes to give 2H-[b][1,4]benzoxazine derivatives along with benzoxazole and indole derivatives. Reaction mechanisms to explain the formation of products obtained are suggested.

N-Alkyl and N-heterocyclic substituted diphenylphosphanylglycines 1a–j were synthesized by a convenient one-pot, three-component reaction of diphenylphosphane, the corresponding primary amine and glyoxylic acid hydrate in diethyl ether. Phosphanylglycolates 2 and phosphoniobis(glycolates) 3 wer...

The substitution kinetics of the complexes [Pt(II)(bis(2-pyridylmethyl)amine)H2O](ClO4)2, Ptdpa and [Pt(II)(bis(2-pyridylmethyl)sulfide)H2O](ClO4)2, Ptdps, with a series of azole nucleophiles: Imidazole (Im), 1-methylimidazole (MIm), 1,2-Dimethylimidazole (DIm), 1,2,4-triazole (Trz) and pyrazole...

Inert C(sp3)―H bonds are ubiquitous in organic compounds, and the direct amination of these bonds represents a faster and atom-economical synthetic approach for synthesis of the alkyl amines. In this chapter, the catalytic aminations of C(sp3)―H bonds will be summarized.

Kahweol and cafestol are two diterpenes that exist mainly as esters of fatty acids in green coffee oil. To recover them under their free form they have to be either saponified or trans-esterified. These two compounds are well known to be sensitive to heat, and reagents, therefore experimental co...

A lower rate of colon cancer was observed in consumers of coffee with a high content of the diterpenes Kahweol and Cafestol (K/C). In animal models, K/C have been found to protect against the mutagenic/carcinogenic effects of compounds such as 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhI...

SummaryThe enediyne antibiotic calicheamicin (CLM) γ1I is a prominent antitumor agent that is targeted to DNA by a novel aryltetrasaccharide comprised of an aromatic unit and four unusual carbohydrates. Herein we report the heterologous expression and the biochemical characterization of the two...

Calicheamicin γ1I is an enediyne antibiotic possessing antitumor activity associated with its ability to bind and following activation, affect double-strand cleavage at oligopyrimidine·oligopurine tracts on DNA. Footprinting and chemical modification studies have identified the (T-C-C-T)·(A-G...

Calicheamicin γ1I is a diyne-ene antitumor antibiotic that binds preferentially to pyrimidine-rich sequences of DNA such as TCCT, ACCT, TCTC,

The cleavage by calicheamicin γ1I of duplex DNA containing four or more contiguous adenines on one strand proceeds through C5′ hydrogen abs

The efficient preparation of a novel analogue of the BCD oligosaccharide domain of Calicheamicin γ1I is described in which the thioester linkage found in the natural product is replaced by an ester group.

The chemical synthesis of two analogues of the calicheamicin γ1I oligosaccharide is described.

We report the hypersensitivity of SV40-transformed fibroblasts derived from ataxia telangiectasia (AT) patients to calicheamicin γ1I. In common with other free-radical generating agents such as bleomycin and ionizing radiation, treatment with calicheamicin γ1I reveals AT derived lines to be 6-...

Background: Calicheamicin γ1I is a bacterial product that is a prominent member of the enediyne class of antitumor antibiotics, and has been extensively studied. Calicheamicin γ1I binds to DNA, causing double-stranded breaks, and cells exposed to it eventually become apoptotic. It can now be m...

A new rapid, simple, sensitive and high performance thin layer chromatography (HPTLC) has been established for the simultaneous determination of ascorbic acid and gallic acid in the freeze-dried pomegranate fruit juice and herbal formulation. HPTLC method was carried out using ethyl acetate: ace...

New class IV transaminases with activity towards L-Leu, which is typical of branched-chain amino acid aminotransferases (BCAT), and with activity towards (R)-(+)-1-phenylethylamine ((R)-PEA), which is typical of (R)-selective (R)-amine:pyruvate transaminases, were identified by bioinformatics an...

Ionic liquids (ILs) constitute a large group of chemical substances, which, thanks to their desirable properties, still attract attention of scientists and representatives of the industry. This may lead to a greater commercial use of these compounds, which will undoubtedly lead to the contaminat...