Direct Structure-Efficacy

Interpreting these results on a detailed molecular basis is difficult because we have at present no direct structural data proving the nature of the split Co(IIl/lI) voltammetry (which seems critical to the electrocatalytic efficacy). Experiments on the dissolved monomeric porphyrin, in CH-C solvent, reveal a strong tendency for association, especially for the tetra(o-aminophenyl)porphyrin. From this observation, we have speculated (3) that the split Co(III/II) wave may represent reactivity of non-associated (dimer ) and associated forms of the cobalt tetra(o-aminophenyl)porphyrins, and that these states play different roles in the dioxygen reduction chemistry. That dimeric cobalt porphyrins in particular can yield more efficient four electron dioxygen reduction pathways is well known (24). Our results suggest that efforts to incorporate more structurally well defined dimeric porphyrins into polymer films may be a worthwhile line of future research. 

A compound lich is potent and has an interesting biological profile will be forwarded to toxicology studies before final decisions are made for advancement to trials or not In some cases lack of toxicity is sufficient - for example carboplatin was developed because of Us lack of nephrotoxicity. Approximately 28 direct structural analogs of cisplatin entered clinical trials but most have been abandoned through a combination of unaccqitable toxicity profile and/or lack of improved or expanded anticancer efficacy (29). Some obstacles to successfol execution of clincial trials are ... 

The end 70-ies was noted by the development of universal efficacious agents for the therapy of OPC affection, H-oximes or reactivators of the second generation, by means of structural modification of the first generation reactivators. The most efficacious compounds were synthesized in Germany under the direction off Hagedom [8],... 

Attractive alternative to oral retinoid therapy in psoriasis (e.g., etretinate), primarily due to less toxicity. Structural changes to the basic retinoid structure (e.g., conformational rigidity) are claimed to enhance therapeutic efficacy and reduce the local toxicity associated with topical tretinoin (retinoic acid). However, place in therapy should await direct comparisons vs standard regimens in terms of efficacy, toxicity, and cost... 

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