By Manoj C Desai
Annual stories in Medicinal Chemistry offers well timed and significant experiences of significant themes in medicinal chemistry with an emphasis on rising issues within the organic sciences which are anticipated to supply the root for totally new destiny therapies.
- Reviews on sizzling issues of curiosity in small molecule drug discovery seriously pursued by means of commercial examine organizations
- Provides preclinical info within the context of chemical structures
- Knowledgeable part editors who review invited stories for medical rigor
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Hogenkamp, D. ; Fick, D. ; Lan, N. ; Gee, K. ; Carter, R. B. J. Pharmacol. Exp. Ther. 1999, 291, 1317–1323. 68. ; Ungard, J. ; Carter, R. ; Witkin, J. M. Neuropharmacology 2000, 39, 1184–1196. 42 Gabriel Martinez-Botella et al. 69. Kokate, T. ; Pannell, L. ; Carroll, D. ; Grossman, A. ; Rogawski, M. A. J. Pharmacol. Exp. Ther. 1998, 287, 553–558. 70. Upasani, R. ; Askew, B. ; Harrison, B. ; Distefano, P. ; Salituro, F. ; Robichaud, A. J. 3,3 Disubstituted 19-nor Pregnane Compounds, Compositions, and Uses Thereof.
28 The in vivo activity of this compound and related analogs was shown using dephosphorylation of S1292 as a measure of LRRK2 kinase activity. Although 40 is an excellent tool compound for probing the effect of LRRK2 inhibition in vivo, it has some major liabilities, thus further optimization was needed for progression 53 Development of LRRK2 Kinase Inhibitors for PD toward a potential clinical candidate. As the diaminopyrimidine forms the key hinge interactions with LRRK2, optimization was focused around the side chain.
Lan, N. ; Gee, K. ; Carter, R. B. J. Pharmacol. Exp. Ther. 1999, 291, 1317–1323. 68. ; Ungard, J. ; Carter, R. ; Witkin, J. M. Neuropharmacology 2000, 39, 1184–1196. 42 Gabriel Martinez-Botella et al. 69. Kokate, T. ; Pannell, L. ; Carroll, D. ; Grossman, A. ; Rogawski, M. A. J. Pharmacol. Exp. Ther. 1998, 287, 553–558. 70. Upasani, R. ; Askew, B. ; Harrison, B. ; Distefano, P. ; Salituro, F. ; Robichaud, A. J. 3,3 Disubstituted 19-nor Pregnane Compounds, Compositions, and Uses Thereof. WO2013056181, 2013.
Annual Reports in Medicinal Chemistry by Manoj C Desai