Selective optimization of side activities: the SOSA approach.
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[1] C. Wermuth,et al. SR 46559A: a novel and potent muscarinic compound with no cholinergic syndrome , 2005, Psychopharmacology.
[2] W. Humphreys,et al. Discovering drugs through biological transformation: role of pharmacologically active metabolites in drug discovery. , 2004, Journal of medicinal chemistry.
[3] R. Silvestri,et al. Imidazole analogues of fluoxetine, a novel class of anti-Candida agents. , 2004, Journal of medicinal chemistry.
[4] C. Wermuth. Selective optimization of side activities: another way for drug discovery. , 2004, Journal of medicinal chemistry.
[5] J. Greer,et al. Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues. , 2004, Journal of medicinal chemistry.
[6] P. Worms,et al. Dopamine-like activities of an aminopyridazine derivative, CM 30366: A behavioural study , 1986, Naunyn-Schmiedeberg's Archives of Pharmacology.
[7] G. Forloni,et al. Neurochemical effects of minaprine, a novel psychotropic drug, on the central cholinergic system of the rat , 2004, Psychopharmacology.
[8] P. Leeson,et al. A comparison of physiochemical property profiles of development and marketed oral drugs. , 2003, Journal of medicinal chemistry.
[9] Christel A. S. Bergström,et al. Absorption classification of oral drugs based on molecular surface properties. , 2003, Journal of medicinal chemistry.
[10] Ping Chen,et al. Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. , 2003, Journal of medicinal chemistry.
[11] André Mann,et al. Nouveaux ligands des récepteurs dopaminergiques D3 , 2003 .
[12] J. Proudfoot. Drugs, leads, and drug-likeness: an analysis of some recently launched drugs. , 2002, Bioorganic & medicinal chemistry letters.
[13] Stephen R. Johnson,et al. Molecular properties that influence the oral bioavailability of drug candidates. , 2002, Journal of medicinal chemistry.
[14] J. Kelly,et al. Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors. , 2002, Journal of medicinal chemistry.
[15] C. Wermuth,et al. Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. , 2001, Journal of medicinal chemistry.
[16] Tudor I. Oprea,et al. Is There a Difference between Leads and Drugs? A Historical Perspective , 2001, J. Chem. Inf. Comput. Sci..
[17] C. Wermuth. The Sosa approach: An alternative to high-throughput screening , 2001 .
[18] B. Lagu. Identification of alpha1A-adrenoceptor selective antagonists for the treatment of benign prostatic hyperplasia , 2001 .
[19] U. Gerlach. IKs channel blockers: Potential antiarrhythmic agents , 2001 .
[20] A. Doherty,et al. Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors. , 2000, Journal of medicinal chemistry.
[21] T. Raju. The Nobel Chronicles , 2000, The Lancet.
[22] Kleeman Hw,et al. Recent developments in the field of inhibitors of the Na+/H+ exchanger. , 1999 .
[23] B. Everitt,et al. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist , 1999, Nature.
[24] C. Wermuth,et al. Aminopyridazines as acetylcholinesterase inhibitors. , 1999, Journal of medicinal chemistry.
[25] C. Wermuth. Search for new lead compounds: The example of the chemical and pharmacological dissection of aminopyridazines , 1998 .
[26] Scott A. Peterson,et al. Discovering transthyretin amyloid fibril inhibitors by limited screening. , 1998, Bioorganic & medicinal chemistry.
[27] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .
[28] H. Böhm,et al. Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. , 1996, Journal of medicinal chemistry.
[29] Y. Shu,et al. BMS-192548, a tetracyclic binding inhibitor of neuropeptide Y receptors, from Aspergillus niger WB2346. I. Taxonomy, fermentation, isolation and biological activity. , 1995, The Journal of antibiotics.
[30] Y. Shu,et al. BMS-192548, a tetracyclic binding inhibitor of neuropeptide Y receptors, from Aspergillus niger WB2346. II. Physico-chemical properties and structural characterization. , 1995, The Journal of antibiotics.
[31] N. Murugesan,et al. The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide. , 1994, Journal of medicinal chemistry.
[32] P. Soubrié,et al. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. , 1993, Proceedings of the National Academy of Sciences of the United States of America.
[33] C. Wermuth,et al. SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndrome , 1992 .
[34] C. Wermuth,et al. 3-aminopyridazine derivatives with atypical antidepressant, serotonergic, and dopaminergic activities. , 1989, Journal of medicinal chemistry.
[35] D. Cucinotta,et al. Comparison of minaprine and placebo in the treatment of Alzheimer's disease and multi‐infarct dementia , 1987 .
[36] C. Wermuth,et al. SR 95191, a selective inhibitor of type A monoamine oxidase with dopaminergic properties. I. Psychopharmacological profile in rodents. , 1987, The Journal of pharmacology and experimental therapeutics.
[37] C. Wermuth,et al. Profil pharmacologique d'un psychotrope original, la minaprine: comparaison avec six antidépresseurs de référence , 1986 .
[38] L. Sternbach. The benzodiazepine story. , 1983, Journal of psychoactive drugs.
[39] J. Kan,et al. Pharmacological evaluation of minaprine dihydrochloride, a new psychotropic drug. , 1982, Arzneimittel-Forschung.
[40] R. Roncucci,et al. The biotransformation of [14C]minaprine in man and five animals species. , 1981, Xenobiotica; the fate of foreign compounds in biological systems.