[Mucocele appendicis retrocaecalis].
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Biomedical subjects
Publications and source records attributed to B Serafin.
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A series of chloromethylsulfonyl derivatives of amines, biguanides and amidineureas (Scheme 1) has been prepared and their antimalarial properties investigated.
The molecule of RC 12 which was found previously to exhibit antimalarial activity has been modified, by replacing groups in positions 1 and 2 by NHAr, S-Ar, NO2, sulfonamido and other substituents. The new derivatives (Table 1) were tested for toxicity and antimalarial activity agains Plasmodium berghei in mice (Table 2).
A series of new derivatives of indole of expected biological activity was prepared. Amidines 7 and 8 were obtained from the corresponding nitriles 3 and 4 and iminoethers 6.
A series of benzimidazole derivatives was synthesized and tested for their hypotensive activity. The most interesting compounds were: BS1/81 (2-guanidino-benzimidazole) and BS1/84 (2-guanidino-5-aminobenzimidazole dihydrochloride), which effects were comparable to those of aminophylline. It was found that substitution of guanidine nitrogen atom with phenyl group caused a distinct decrease of activity while cyclization of guanidine rest to pyrimidine ring caused only a small decrease of activity.
Series of dihydrotriazines and arylbiguanides were synthetized and tested for their hypotensive effect. Compounds I and II in doses corresponding to 0.2 of their LD50 produced small hypotension. The biguanides exerted the hypotensive effect when given in a dose of 0.05 of their LD50, but the effect was weaker than that of aminophylline.