A series of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds were prepared and evaluated for their antagonistic activities to the angiotensin II (AII) receptor. Among them, the 4-(1-hydroxyalkyl)-imidazole derivatives had strong binding affinity to the AII receptor and potently inhibited the AII-induced pressor response by intravenous administration. Various esters of these acids showed potent and long-lasting antagonistic activity by oral administration. The most promising compounds were (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (CS-866) and (pivaloyloxy)-methyl esters of 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[(2'-1H-tetrazol-5- ylbiphenyl-4-yl)-methyl]imidazole-5-carboxylic acid (26c). A study involving stereochemical comparison of 26c with the acetylated C-terminal pentapeptide of AII was also undertaken.
Cornexistint, a new compound demonstrating promising herbicidal activity, was purified from the culture nitrate of a newly-isolated fungus identified as Paecilomyces variotii SANK 21086. The compoundwas extracted with organic solvents from the culture nitrate, purified using column chromatography on Sephadex LH-20 and finally crystallized from methylene chloride. Following analysis of its physico-chemical properties it was identified to be a new compound belonging to the nonadride group. Chemical structure elucidation was conducted by analyses of various spectral data and the structure was finally confirmed by means of X-ray crystallographic analysis. Based on its herbicidal characteristics cornexistin may be classified as a postemergence herbicide active against certain young annual and perennial monocotyledonous and dicotyledonous plants with selective protection for corn.
The in vitro activity of LJC10,627, a new carbapenem, was compared with those of imipenem and ceftazidime. LJC10,627 had broad-spectrum activity against gram-positive and gram-negative clinical isolates.
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