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PubMed1983

The effect of hemin and of allyl isopropyl acetamide on protein synthesis in rat hepatocytes.

Protein synthesis was measured in incubated hepatocytes. While hemin brings about a slight stimulation, allyl isopropyl acetamide (a compound that destroys the heme bound to cytochrome P450) inhibits protein synthesis by a mechanism that appears to result exclusively from depletion of cytoplasmic heme. Indications that in hepatocytes, as in reticulocytes, protein synthesis may be in part regulated by heme at the level of initiation are: i) that inhibition is accompanied by polysome breakdown; ii) that the protein synthesis inhibitor already isolated from rat liver, is hemin reversible iii) that hepatocyte extracts contain a Mr 38,000 phosphoprotein which comigrates with the Mr 38,000 subunit of rabbit initiation factor 2 and iv) that the phosphorylation of both of these subunits is inhibited by hemin.

Acetamides↗
PubMed1996

Activities of the rodent carcinogens thioacetamide and acetamide in the mouse bone marrow micronucleus assay.

Thioacetamide is confirmed as active in the mouse bone marrow micronucleus assay, following single oral administration to both sexes of two different strains of mice (C57BL/6, BALB/c) in five separate experiments. Acetamide is shown to be consistently and clearly negative as a micronucleus-inducing agent in mouse bone marrow in four repeated assays using different sexes of two strains of mice (C57BL/6, CBA). The present findings support the adequacy of the limited micronucleus test protocol (male animals, two sampling times) for the efficient detection of genotoxic rodent carcinogens in this assay.

Acetamides↗
PubMed1992

In vitro reactivation of latent herpes simplex virus by the demethylating compound hexamethylene-bis-acetamide.

We have characterized previously a model of herpes simplex virus (HSV) infection of rat dorsal root ganglia (DRG) following cutaneous infection. During acute infection HSV can be isolated from co-cultivated rat ganglia in (mean +/- S.E.M.) 4.8 +/- 0.33 days (d) and from latently infected ganglia in 7.8 +/- 0.53 (d) (P < or = 0.0001). We treated co-cultivated rat ganglia from acute and latent infected rats with the demethylating compound hexamethylene-bis-acetamide (HEX) to see what effect, if any, it would have on HSV infection. HEX-treated ganglia from rats with acute infection did not differ significantly from controls in the proportion of rats, skin or ganglia positive for HSV. The mean time to detect virus was not different between treated (3.6 +/- 0.38 d) and control (3.1 +/- 0.46 d) (P > 0.05) groups. In latent infected rats there was no difference between treated and controlled groups in the proportions of rats, skin and ganglia positive for HSV. There was a significant difference in the mean time to CPE between the HEX and control groups respectively (4.5 +/- 0.72 d vs 8.92 +/- 1.42 d, P < 0.01). We conclude that HEX converted latent HSV infection to a productive one.

Acetamides↗
PubMed2004

Synthesis and functional activity of (2-aryl-1-piperazinyl)-N-(3-methylphenyl)acetamides: selective dopamine D4 receptor agonists.

Diaryl piperazine acetamides were identified as potent and selective dopamine D(4) receptor agonists. Our strategy is based on an amide bond reversal of an acid sensitive, dopamine D(4) receptor partial agonist, PD 168077. This reversal provided compounds with excellent potency and improved stability. Systematic evaluation of the substitution on the aryl piperazine portion revealed a significant effect on functional activity. The synthesis and biological activity of these new dopamine D(4) agonists is discussed.

Acetamides↗
PubMed2005

A new type of ketolides bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether synthesis and structure-activity relationships.

A new type of ketolides, bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and a cyclic carbonate at the C-11,12 position was prepared and the antibacterial activities of the compounds were evaluated. Some of the derivatives showed potent antibacterial activity against both Haemophilus influenzae and Streptococcus pneumoniae, which are clinically important respiratory tract pathogens. Among the derivatives prepared, compound 5s with a quinolin-4-yl moiety was found to have potent and well-balanced activity against S. pneumoniae and H. influenzae including erythromycin-resistant strains.

Acetamides↗
PubMed2006

A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether: synthesis and structure-activity relationships.

A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and its analogues were prepared, and their antibacterial activities and pharmacokinetic properties were evaluated. We found that the introduction of an (R)-alkyl group between the amide and iminoether groups could improve the pharmacokinetic properties while maintaining the activity against erythromycin-resistant Streptococcus pneumoniae. Among the ketolides prepared with the (R)-alkyl group, compound 5p with an N-(3-quinoxalin-6-yl-propyl)-propionamide moiety was found to have in vivo efficacy comparable to CAM with potent in vitro antibacterial activities against the key respiratory pathogens including Haemophilus influenzae and erythromycin-resistant S. pneumoniae.

Acetamides↗
PubMed2006

Linear and nonlinear QSAR study of N-hydroxy-2-[(phenylsulfonyl)amino]acetamide derivatives as matrix metalloproteinase inhibitors.

The inhibitory activity (IC50) toward matrix metalloproteinases (MMP-1, MMP-2, MMP-3, MMP-9, and MMP-13) of N-hydroxy-2-[(phenylsulfonyl)amino]acetamide derivatives (HPSAAs) has been successfully modeled using 2D autocorrelation descriptors. The relevant molecular descriptors were selected by linear and nonlinear genetic algorithm (GA) feature selection using multiple linear regression (MLR) and Bayesian-regularized neural network (BRANN) approaches, respectively. The quality of the models was evaluated by means of cross-validation experiments and the best results correspond to nonlinear ones (Q2>0.7 for all models). Despite the high correlation between the studied compound IC50 values, the 2D autocorrelation space brings different descriptors for each MMP inhibition. On the basis of these results, these models contain useful molecular information about the ligand specificity for MMP S'1, S1, and S'2 pockets.

Acetamides↗
PubMed2005

N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.

In the course of our screening, N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide (1), which contains a metal-chelating hydroxamate group, has been identified as a potent inhibitor of aminopeptidase N (APN, EC 3.4.11.2). Compound 1 potently inhibited APN activity with a K(i) value of 3.5 microM. It also inhibited the basic fibroblast growth-factor-induced invasion of bovine aortic endothelial cells at low micromolar concentrations.

Acetamides↗
PubMed2005

Activity coefficients and thermodynamic parameters for RbCl/CsCl + amide (acetamide, propanamide, and n-butanamide) + water system at 298.15 K.

Electromotive force (emf) of the chemical cell without liquid-junction K-ISE | RbCl/CsCl ( m(E)) | ISE-Cl and K-ISE | RbCl/CsCl (m(E)), amide (m(N)) | ISE-Cl, have been measured at 298.15 K, where m(E)=(0.005 to 0.5) mol kg(-1) and m(N)= (0.05 to 3.0) mol kg(-1). The activity coefficients of RbCl/CsCl in amide (acetamide, propanamide, and n-butanamide) + water mixture can be obtained from these electromotive force data and in the mean time the Gibbs free energy interaction parameters of RbCl/CsCl + amide pair in water, g(EN), as well as the salt constant, k(S), can be evaluated. The results show that both g(EN)>0, k(S)>0 at 298.15 K, and all the activity coefficients of electrolyte in amide + water mixture increase with increasing the m(N), but it is a little complicated for the dependence of activity coefficients on m(E). These thermodynamic parameters were discussed in terms of a model of the structural interaction and electrostatic interaction and the dependence of them on the number of carbon atoms in amide as well as the radius of metal ions were interpreted by the group additivity principle.

Acetamides↗
PubMed2004

[3H] A-369508 ([2-[4-(2-cyanophenyl)-1-piperazinyl]-N-(3-methylphenyl) acetamide): an agonist radioligand selective for the dopamine D4 receptor.

Tritiation of the dopamine D(4) receptor selective agonist A-369508 ([2-[4-(2-cyanophenyl)-1-piperazinyl]-N-(3-methylphenyl) acetamide) has provided a radioligand for the characterization of dopamine D(4) receptors. [(3)H] A-369508 binds with high affinity to the major human dopamine D(4) receptor variants D(4.2), D(4.4) and D(4.7) (K(d)=1.7, 4, and 1.2 nM, respectively). It also binds to the rat dopamine D(4) receptor, (K(d)=4.4 nM), implying similar binding affinity across human and rat receptors. A-369508 shows >400-fold selectivity over D(2L), >350-fold selectivity over 5-HT(1A) and >700-1,000-fold selectivity over all other receptors tested. Agonist activity determined by inhibition of forskolin-induced cAMP in Chinese hamster ovary cells transfected with the human dopamine D(4.4) receptor (EC(50)=7.5 nM, intrinsic activity=0.71) indicates that A-369508 is a potent agonist at the human dopamine D(4) receptor. Similar data was observed in other functional assays. [(3)H] A-369508 binds to a single, high affinity site on membranes containing the human dopamine D(4.4) receptor. When compared to the D(2)-like antagonist [(3)H] spiperone, competition binding for agonists like dopamine and apomorphine were 2-10-fold more potent with [(3)H] A-369508, while the antagonists clozapine, haloperidol and L-745870 bind with similar affinity to both ligands. Binding to rat brain regions demonstrated that the most abundant area was cerebral cortex (51.2 fmol/mg protein) followed by hypothalamus, hippocampus, striatum and cerebellum. [(3)H] A-369508 is a useful tool to define the localization and physiological role of dopamine D(4) receptors in central nervous system and can facilitate measuring accurate affinities (K(i)) for structure/activity relationship studies designed to identify dopamine D(4) receptor selective agonists.

Acetamides↗
PubMed2004

Influence of physicochemical properties and intestinal region on the absorption of 3-fluoro-2-pyrimidylmethyl 3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide, a water insoluble thrombin inhibitor, in dogs.

In this paper, we describe the physicochemical and biopharmaceutical properties of 3-fluoro-2-pyrimidylmethyl 3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide, a direct thrombin inhibitor (1, Fig. 1). Three crystalline forms were characterized and studies were planned to investigate the absorption characteristics of the three selected crystalline forms. Due to the short half-life observed in preclinical species, regional absorption studies were also conducted to support potential controlled release formulation development. Results showed that the absorption of 1 was dependent on the surface area of the particles administered as suspensions and was independent of the crystal forms. From Caco-2 cell transport studies, it was determined that the permeability of 1 was high. Based on the low aqueous solubility it would be classified as a class 2 compound in the Biopharmaceutics Classification System. Regional absorption results suggested that the compound was absorbed along the gastrointestinal tract in Beagle dogs, however colonic absorption appeared to be reduced by slower dissolution.

Acetamides↗
PubMed2006

Solvent effect on the luminescent properties of new europium and terbium nitrate complexes with 3,3,7,7-tetra[N-methyl-N-phenyl(acetamide)-2-oxymethyl]-5-oxanonane.

The multipodal ligand 3,3,7,7-tetra[N-methyl-N-phenyl(acetamide)-2-oxymethyl]-5-oxanonane (L) and its europium and terbium nitrate complexes were synthesized. The complexes were characterized by elemental analysis, IR, fluorescence spectroscopy and conductivity. The lanthanide atoms are coordinated by O atoms from CO, COC. With the difference of the solvent, the fluorescence properties of solvent effect for the complexes were investigated. Some factors that influencing the fluorescent intensity were discussed.

Acetamides↗
PubMed1979

Complete neglect of differential overlap study of the binding of salts to N-methyl acetamide.

The complete neglect of differential overlap method is used to investigate the binding of LiF, LiCl, NaF, and NaCl to N-methyl acetamide (NMA) as a model for these ions binding to a peptide moiety. The cation (formula: see text) anion interaction is shown to result in a net residual charge on NMA, which becomes less positive as the difference in electronegativity between the anion and cation of the salt present increases. A residual charge of smaller magnitude is also found on a water molecule in the analogous system cation (formula: see text) anion, which displays this same dependence.

Acetamides↗
PubMed1998

A novel, selective synthetic acetamide containing culture medium for isolating Pseudomonas aeruginosa from milk.

A selective synthetic medium has been developed both in liquid (Z-broth) and solid (Z-agar) forms for selective isolation of Pseudomonas aeruginosa from foods. The simple, easy to prepare peptone-free synthetic medium contained acetamide that is metabolized to ammonia and acetic acid providing nitrogen and carbon supply. The medium contained no inhibitors. Selectivity of the liquid medium was tested by inoculation of pure cultures of different bacteria belonging to the groups Bacillus, Pseudomonas, Enterobacteriaceae and Staphylococcus. It was found that the selectivity of the medium was complete for the examined range of bacteria. However, a similar result was obtained when nitrofurantoin broth was used. Applicability of the synthetic agar medium was also tested by a nation-wide inter-laboratory test using two milk samples containing 10(3)/ml (sample I) and 10(5)/ml (sample II) Pseudomonas aeruginosa. According to this test, no microbiologically relevant differences were found between the results obtained by Z-agar and cetrimide-agar a frequently used selective agar in case of sample II. However, a relevant and statistically significant difference was found in the results of sample I in favour of the Z-agar, that could indicate the presence of a low number of bacteria. Concerning repeatability and reproducibility, Z-agar proved to be superior to cetrimide agar.

Acetamides↗