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2005
Thiazole derivatives
R 0260
Studies on the Reactivity of Fused Thiazole Toward Nucleophilic Reagents:
of New Thiazolo-Derivatives of Potential Antischistosomal Activity. —
35- 144 Synthesis
Due to the toxic effect of 2-amino-5-nitrothiazoles, active against S. mansoni and S.
haematobium, new derivatives of a heteroaromatic amine with a thiazole moiety are
synthesized. The amino function of salt (I) is replaceable by carbonionic species in
sodium hydroxide solution. Dicyanomethylene derivative (III) condenses with electrophilic reagents enabling the preparation of new biologically interesting thiazoles. Treatment of (I) with sodium hydroxide solution yields the intermediate diamino thiazole
which is condensed with acetal (IV) providing di-amidine structure (VI). Salt (I) and
2,4-diaminothiazole show moderate efficacy with regard to worm reduction, whereas
the dimethylimidoformamide moieties combined with the thiazole ring, (V) and (VI),
exhibit 83% and 90% worm reduction, resp., with some normalization of liver function
and significant reduction in hepatic granuloma diameters. — (MANHI*, F. M.;
MAHMOUD, M. R.; Heteroat. Chem. 16 (2005) 2, 121-131; Natl. Organ. Drug
Control Res., Cairo, Egypt; Eng.) — H. Hoennerscheid
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