Amidation growth inhibitors

Pyridine-3-sulfonic acid and its amide as inhibitors of bacterial growth. 

The effect of a-amidation on DHFR binding and cell growth inhibition has been evaluated [240], The of (VII. 11) as an inhibitor of DHFR from L1210... 

Strain. By these criteria, methyl methanesulfonate, A -acetoxyfluorenylacet-amide, captan, and others are preferential inhibitors of the pol Ai strain (Tables 7 and 8). On the other hand, streptomycin and chloramphenicol, although they induce lethality in both indicator strains, do not preferentially kill the pol Ar strain (SI = 1.12 and 1.02, respectively). It should be noted that this procedure is compatible with metabolic activation. Thus, the precarcinogens 2-aminofluorene and cyclophosphamide, which require metabolic activation by hepatic enzymes, do not preferentially inhibit the pol Ai strain in the absence of rat liver microsomes, but do so in the presence of this preparation (Tables 7 and 8). This procedure has the added advantage that results obtained by this modified pol Ai assay are expressed quantitatively, rather than as differences in the diameters of the zones of growth inhibition. As will be seen below, this modified procedure greatly increases the usefulness of the pol A assay (Table 9). 

In order to develop new antidiabetic agents, guanidine and tetrazole substituted amides of 6-fluoroquinolin-2-carboxamides 205, 206 and 207 have been obtained [138]. Compound 207 acts as fibroblast growth factor receptor 3 (FGFR ) inhibitor and can be used for treatment of multiple myeloma (Scheme 89) [139,140]. 

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