Analogue-based Drug Discovery
IUPAC, JŠnos Fischer, C. Robin Ganellin
John Wiley & Sons, Dec 13, 2006 - Science - 606 pages
The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds.
Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them.
The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability.
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ACE-inhibitors acid secretion activity affinity Agents Chemother agonist angiotensin antagonist antibacterial antihistamines Antimicrob antipsychotic atenolol atorvastatin Bayer beta-blockers betaxolol bioavailability Bisphosphonates Byk Gulden carbamates celiprolol cells CH 3 CH CH3 CH3 Chem chemical cimetidine Clin clinical clozapine compounds COOH derivatives disease dose Drug analogue Drug Discovery efficacy enzyme esmolol ester fluoroquinolones gatifloxacin half-life histamine Hoffmann-La Roche hypertension increased inhibition inhibitors interaction K+-ATPase lacidipine ligands lipophilic losartan Lovastatin Medicinal Chemistry Merck metabolism metabolite moiety molecule morphine moxifloxacin nebivolol ofthe OH O OH OH OH olanzapine omeprazole opioid receptor oral organic nitrates pantoprazole patients Pharma pharmacokinetic Pharmacol pharmacological physostigmine plasma potent PPIs produced properties quetiapine quinolones renal ring rosuvastatin Scheme selective side effects simvastatin statins structure studies substituent synthesis target Ther therapeutic therapy tion toxicity treatment valsartan vitro vivo