SYNTHESIS AND RADIOPROTECTIVE ACTIVITY SF WR-1065 DERIVATIVES - N-(2-ACETYLTHIOETHYL)-1,3-PROPANEDIAMINE AND N,N'-BIS(2-ACEATYLTHIOETHYL)-1,3-PROPANEDIAMINE

Citation
J. Oiry et al., SYNTHESIS AND RADIOPROTECTIVE ACTIVITY SF WR-1065 DERIVATIVES - N-(2-ACETYLTHIOETHYL)-1,3-PROPANEDIAMINE AND N,N'-BIS(2-ACEATYLTHIOETHYL)-1,3-PROPANEDIAMINE, European journal of medicinal chemistry, 30(1), 1995, pp. 47-52
Citations number
37
Categorie Soggetti
Chemistry Medicinal
ISSN journal
02235234
Volume
30
Issue
1
Year of publication
1995
Pages
47 - 52
Database
ISI
SICI code
0223-5234(1995)30:1<47:SARASW>2.0.ZU;2-E
Abstract
N-(2-Acetylthioethyl)-1,3-propanediamine (13a, as its 2HBr salt, or 13 b, as its 2CF(3)CO(2)H salt) and N,N'-bis(2-acetyl-thioethyl)-1,3-prop anediamine (16, as its 2CF(3)CO(2)H salt) have been prepared and evalu ated as potential radioprotectors in mice. Their toxicity and radiopro tective activity (survival rate) have been determined and compared wit h that of WR-2721. Intermediate N-(2-acetylthioethyl)-N,N'-bis(Z or Bo c)-1,3-propanediamines were prepared in two ways from the correspondin g alcohols. The most convenient method (the Mitsunobu procedure) was u sed to obtain the N,N'-bis(2-acetylthioethylated) derivative from the corresponding diol. Surprisingly, none of these compounds possesses ra dioprotective activity.