Analogue-based Drug Discovery by Janos Fischer, C. Robin Ganellin, David P. Rotella

By Janos Fischer, C. Robin Ganellin, David P. Rotella

The 1st authoritative assessment of prior and present recommendations for profitable drug improvement via analog new release, this special source spans all vital drug sessions and all significant healing fields, together with histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds.Of the nineteen analog periods provided intimately, nine are defined through the scientists who discoverd them.The publication contains a desk of the main winning drug analogs as in accordance with the IMS rating and compares them by way of chemical constitution, mode of motion and patentability.

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Med. , 2003, 46, 558–570. Wenlock MC, Austin RP, Barton P, Davis AM, Leeson PD. A comparison of physicochemical property profiles of development and marketed oral drugs. J. Med. , 2003, 46, 1250–1256. Shu YZ, Cutrone JQ, Klohr SE, Huang S. BMS-192548, a tetracyclic binding inhibitor of neuropeptide Y receptors, from Aspergillus niger WB2346. II. Physico-chemical properties and structural characterization. J. , 1995, 48, 1060–1065. 23 25 2 Drug Likeness and Analogue-Based Drug Discovery John R. Proudfoot Natural products or other drug structures have served as lead structures for the majority of drugs launched during the past 100 years.

Once a hit is observed with a given drug molecule, the task is then to prepare analogues of this molecule in order to transform the observed “side activity” into the main effect and to strongly reduce or abolish the initial pharmacological activity. 2 Rationale The rationale behind the SOSA approach lies in the fact that, in addition to their main activity, almost all drugs used in human therapy show one or several side effects. In other words, if they are able to exert a strong interaction with the main target, they exert also less strong interactions with some other biological targets.

Originality On occasion, the screening of a library of several hundred therapeutically diverse drug molecules ultimately produces very surprising results. A nice example of unexpected findings resulting from a systematic screening is found in the tetracyclic compound 11 (BMS-192548) extracted from Aspergillus niger WB2346 (Fig. 21). OH O OH O OH O OH O OH O OH NH2 H HO CH3 H H3C OH N O CH3 CH3O OH OH CH3 10: tetracycline 11: BMS-192548 Fig. 21 Unexpected CNS activity of the tetracycline analogue 11 (BMS-192548) [48].

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