A series of 62 diarylamidine derivatives was evaluated for their antiproteolytic activity. In all but two of the compounds one or both of the amidino-substituted aryl moieties was either an indole or an indole-like ring. The latter included indene, benzimidazole, benzofuran, benzol[beta]thiophene, and several other related nitrogen-containing heterocycles. Several of the compounds exhibited considerable inhibitory potency against thrombin, trypsin, and pancreatic kallikrein. An outstanding inhibitor of trypsin was found in bis(5-amidino-2-benzimidazolyl)methane (compound 42) with a Ki value of 1.7 X 10(-8) M(pH. 8.1, 37 degrees C). Another derivative, 1,2-di(4-amidino-2-benzofuranyl)ethane (compound 21), proved to be a highly effective inhibitor of the overall blood clotting process. From a general structure-activity standpoint these compounds demonstrate that minor structural variations of low-molecular-weight inhibitors can result in significant changes in specificity and potency with regard to antiproteolytic activity.
The development of the alimentary tract in larvae of Coregonusfem fed with Artemiu nauplii has been examined histologically from the 4th to the 24th day after hatching.Buccal cavity and oesophagus are nearly completely developed before the start of feeding. The stomach exists only as an * anlage ', but starts to store food during the study period. The intestinal absorptive cells are stuffed with fat vacuoles between the 7th and 13th day after the start of feeding. During this time the rectal absorptive cells contain one large supranuclear body consisting of protein. The occurrence of large vacuoles in the intestinal and rectal absorptive cells may be caused by a partial non-functioning of the larval digestion; after two weeks of feeding this restriction seems to be overcome.
Substitution of alkyl benzimidazol‐2‐ylcarbamates by phenoxy‐ or phenylthio‐groups in the 5‐position results in an increase in anthelmintic activity. The biological spectrum is altered by substitution of the phenyl ring. A sulphonic ester substituent in the 5‐position of the benzimidazole nucleus also increases anthelmintic activity.
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