The interaction of the formamidine pesticides chlordimeform (CDM) and amitraz (AMZ) with rat brain alpha2-adrenoceptors was investigated. Both compounds inhibited the binding of 3H-clonidine and 3H-yohimbine in vitro with IC50 values of 62–68 μM (CDM) and 95–110 nM (AMZ). In vivo administrati...

The effects of the formamidine pesticide chlordimeform (CDM), and the carbamate carbaryl (CAR) were compared using a functional observational battery (FOB). The FOB, a series of observations and measurements that can be rapidly administered to toxicant-treated rats, includes home-cage and open-f...

Twenty-one diazepam- and chlordimeform (CDM)-related compounds were synthesized by mimicking some parts of the 1,4-benzodiazepine tranquilizing drugs, and were tested for their insecticidal activity against the German cockroach. Some of these compounds showed knockdown effects and some were inse...

The hypothesis that chlordimeform increased the amplitude of components N1P1 and P1N3 in rat pattern-reversal visual evoked potentials through actions on α2-adrenergic receptors was tested with two sets of experiments. First, rats received single injections of either vehicle, an α2-adrenergic ...

The toxic symptoms of the pesticide, chlordimeform, resemble those observed following systemic local anesthetic overdose. In view of similarities in the chemical structures of chlordimeform and the local anesthetic agent phenacaine, additional comparisons between the actions of chlordimeform and...

The effects of chlordimeform [N-(2-methyl-4-chlorophenyl)-N′,N′-dimethylformamidine] on amine regulatory mechanisms in insects were studied. Chlordimeform inhibits monoamine oxidase (MAO) from cockroach heads in vitro, and the MAO substrates serotonin and norepinephrine accumulate in poisoned ...

The acaricide chlordimeform has been reported to have adverse effects in mammals that may be mediated by an interaction with α-adrenergic receptors. Since the hormonal signals involved in the regulation of reproductive function are themselves under hypothalamic adrenergic control, the present s...

Pyrazole carboxylic acid derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide (inhibitor 1) were synthesized from ethyl 3-(chlorocarbonyl)-1-(3-nitrophenyl)-5-phenyl-1H-pyrazole-4-carboxylate compound. The inhibitory effects of inhibitor 1, acetazolamide (AAZ) and of 11 newly synthesized amide...

Thirty thiazole compounds bearing chemotherapeutically-active pharmacophores were synthesized and evaluated for their preliminary in vitro antimicrobial and anticancer activities. Nineteen compounds displayed obvious antibacterial potential, with special bactericidal activity against Gram positi...

Two series of picolinamide derivatives bearing (thio)urea and dithiocarbamate moieties were designed and synthesized as VEGFR-2 kinase inhibitors. All the new compounds were screened for their cytotoxic activity against A549 cancer cell line and VEGFR-2 inhibitory activity. Compounds 7h, 9a and ...

2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-p...

A conceptually novel strategy has been developed for the synthesis of N-(β-glycosyl)asparagine precursors in good yield by the alkylation of ethyl nitroacetate using six per-O-acetylated N-(β-glycosyl)iodoacetamides derived from mono- and disaccharides. The use of a chiral organocatalyst, N-(9...

The amidation of unactivated ethyl esters with achiral and chiral 1,2-amino alcohols under microwave irradiation and base-free conditions is described. This procedure provides a convenient method for the synthesis of β-hydroxyacetamides bearing pyrazole, imidazole, and benzimidazole groups in h...

A series of novel 2-amino-5-chlorobenzophenone derivatives (3a–3g) were prepared by the reaction of 2-(chloroacetamido)-5-chlorobenzophenone and different aniline derivatives by both conventional and microwave methods and structures were confirmed on the basis of their TLC, IR, 1H NMR and CHN e...

1,3,4,6-Tetra-O-acetyl-2-chloroacetamido-2-deoxy-β-d-glucopyranose was tested as a glycosyl donor for oligosaccharide synthesis via a ferric chloride-catalyzed coupling reaction. Glycosyl acceptors tried (6 in all) were O-benzyl-protected d-galactosides having free OH groups at positions 3 and ...

In this study, a series of polysubstituted methyl 5,5-diphenyl-1-(thiazol-2-yl)pyrrolidine-2-carboxylate derivatives were designed and synthesized by the cyclization reaction of methyl 1-(benzoylcarbamothioyl)-5,5-diphenylpyrrolidine-2-carboxylates and 2-bromo-1-(4-substituted phenyl)ethanones i...

Single crystal X‐ray diffraction (SCXRD), powder X-ray diffraction (PXRD), and solid‐state NMR (SSNMR) techniques are used to analyze the structures of two nonsolvated polymorphs of {4‐(4‐chloro‐3‐fluorophenyl)‐2‐[4‐(methyloxy)phenyl]‐1,3‐thiazol‐5‐yl} acetic acid. These polymorphs ...

Enantiomerically pure 3-hydroxypropyl diisopropylidene mannose derivatives were prepared and fully characterized. The procedure is generally applicable to monosaccharides and thus facilitates access to differently substituted glycosidic precursors.

Multivalent galactose ligands have been proposed for selective targeting of carbohydrate-binding proteins on epithelial cell surfaces, both in normal and pathological conditions. One cellular partner is galectin-3, a β-galactoside-binding protein present on many epithelial linings, such as thos...

3-Chloro-2-hydroxypropyl acetate has wide applications in production of various epoxy resins, reactive polymers used for coating metal, leather, paper and wood. Regioselective ring opening reaction of epichlorohydrin with acetic acid to synthesize 3-chloro-2-hydroxypropyl acetate was studied usi...