Potential radioprotective agents-V. Melatonin analogs. Oral activity of p-aminopropiophenone and its ethylene ketal was written by Blickenstaff, Robert T.;Reddy, Shailaja;Witt, Robert. And the article was included in Bioorganic & Medicinal Chemistry in 1994.Category: amides-buliding-blocks This article mentions the following:
Seven new amides of 5-methoxytryptamine were synthesized and tested for radioprotective activity in mice. One of them, the heptafluorobutyramide 4, is moderately active (57% survivors); the rest demonstrate little or no activity. Of twelve compounds that had been found to exhibit high radioprotective activity by i.p. injection, only two [p-aminopropiophenone (9) and its ethylene ketal 8] retain that high activity (92-95% survivors) when administered orally. Three are moderately active: p-aminobenzonitrile (10, 55%), 5-methoxytryptamine octanoic amide (11, 50%), and p-aminobenzophenone (12, 48%). In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Category: amides-buliding-blocks).
3,4-Dichlorobenzamide (cas: 2670-38-4) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics