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Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Mazurov AA, Miao L, Bhatti BS, Strachan JP, Akireddy S, Murthy S, Kombo D, Xiao YD, Hammond P, Zhang J, Hauser TA, Jordan KG, Miller CH, Speake JD, Gatto GJ, Yohannes D. Mazurov AA, et al. Among authors: speake jd. J Med Chem. 2012 Nov 8;55(21):9181-94. doi: 10.1021/jm3006542. Epub 2012 Jul 27. J Med Chem. 2012. PMID: 22793665
Identification and pharmacological characterization of 3,6-diazabicyclo[3.1.1]heptane-3-carboxamides as novel ligands for the α4β2 and α6/α3β2β3 nicotinic acetylcholine receptors (nAChRs).
Strachan JP, Kombo DC, Mazurov A, Heemstra R, Bhatti BS, Akireddy R, Murthy S, Miao L, Jett JE, Speake J, Bencherif M. Strachan JP, et al. Eur J Med Chem. 2014 Oct 30;86:60-74. doi: 10.1016/j.ejmech.2014.08.019. Epub 2014 Aug 7. Eur J Med Chem. 2014. PMID: 25147147
3D molecular descriptors important for clinical success.
Kombo DC, Tallapragada K, Jain R, Chewning J, Mazurov AA, Speake JD, Hauser TA, Toler S. Kombo DC, et al. Among authors: speake jd. J Chem Inf Model. 2013 Feb 25;53(2):327-42. doi: 10.1021/ci300445e. Epub 2013 Jan 18. J Chem Inf Model. 2013. PMID: 23244494
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Mowbray CE, Braillard S, Glossop PA, Whitlock GA, Jacobs RT, Speake J, Pandi B, Nare B, Maes L, Yardley V, Freund Y, Wall RJ, Carvalho S, Bello D, Van den Kerkhof M, Caljon G, Gilbert IH, Corpas-Lopez V, Lukac I, Patterson S, Zuccotto F, Wyllie S. Mowbray CE, et al. J Med Chem. 2021 Nov 11;64(21):16159-16176. doi: 10.1021/acs.jmedchem.1c01437. Epub 2021 Oct 28. J Med Chem. 2021. PMID: 34711050 Free PMC article.
23 results