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At least 289 records · Page 16Linked to original sources
PubMed1983

The evaluation of mutagenicities of 19 structurally related aromatic amines and acetamides in Salmonella typhimurium TA98 and TA100.

19 aromatic amines were assayed for mutagenicity using Salmonella typhimurium strains TA98 and TA100 with and without the addition of S9 from Aroclor-1254-induced rat liver. These included: naphthalenes (1-amino-, 1-acetamido-, 2-amino-, 2-acetamido-, 1-amino-4-nitro- and 2-amino-1-nitro-), biphenyls (2-amino-, 2-acetamido-, 4-amino- and 4-acetamido-), fluorenes (2-amino- and 2-acetamido-), anthracenes (1-amino-, 1-acetamido-, 2-amino- and 2-acetamido-), 3-aminofluoranthene, 1-aminopyrene and 6-aminochrysene. None of the compounds were mutagenic when tested without S9. With S9, 15 of 19 were mutagenic for TA98 and 16 of the 19 were mutagenic for TA100. Overall, 2-aminoanthracene was the most potent mutagen. When compared to the parent amines, the respective acetamido derivatives were consistently less mutagenic.

Acetamides↗
PubMed2004

Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.

The first selective dopamine D4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands was measured and [3H]6b found to be suitable for use in D4 saturation and competition binding studies. The synthesis, biological, and radioactivity of this new agonist radioligand as well as preliminary SAR will be discussed.

Acetamides↗
PubMed2006

Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.

This letter describes the discovery of a novel series of potent Kv1.5 ion channel antagonists based on a diisopropyl amide scaffold. Structure-activity relationships of functionalized analogs are discussed. Key compound 1-(3-(diisopropylcarbamoyl)-2-phenyl-3-(pyridin-3-yl)propyl)-3-(2-fluorobenzyl)urea (10) exhibits significant atrial-selective effects in an in vivo model.

Acetamides↗
PubMed2006

Synthesis, crystal structures and cytotoxicities of some transition metal complexes with N-[2-{(pyridin-2-ylmethylidene)amino}ethyl]acetamide.

The synthesis and spectroscopic (IR, (1)H and (13)C NMR) characterization of new complexes of Pt(II), Pd(II), Cu(II), and Hg(II) with the Schiff base ligand MeCONHCH(2)CH(2)N=CHPy (L) (Py=pyridine) are reported, together with studies on the cytotoxicities of these complexes, L and [ReBr(CO)(3)(L)] against human leukemia (MOLT-4), breast cancer (MCF-7) and Chang Liver (non-cancerous) cells. The crystal structures of [Pt(L)Cl(2)] (2), [Cu(L)Cl(2)] (4) and [Hg(L)Cl(2)](2) (5) are also reported. Of the complexes studied, [Cu(L)Cl(2)] (4) was identified as the most cytotoxic active derivative against cells of neoplastic origin (MOLT-4, and MCF-7), while having low toxicity on cells of benign origin (Chang Liver).

Acetamides↗