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Synthetic Communications, ISSN 0039-7911, 06/2019, Volume 49, Issue 11, pp. 1436 - 1443
AT13387 is an orally bioavailable clinical candidate developed to inhibit heat shock protein 90 (Hsp90). This article describes a modified synthetic route for... 
Hsp90 | iso-indoline | cost-effective synthetic route | AT13387 | proteostasis | COMPLEX | MOLECULAR CHAPERONES | CHEMISTRY, ORGANIC | DISCOVERY
Journal Article
Assay and Drug Development Technologies, ISSN 1540-658X, 05/2018, Volume 16, Issue 4, pp. 193 - 193
Journal Article
RSC Drug Discovery Series, ISSN 2041-3203, 2017, Volume 2017-, Issue 56, pp. 175 - 193
Journal Article
PLoS Pathogens, ISSN 1553-7366, 07/2011, Volume 7, Issue 7, p. e1002112
Journal Article
Neuropsychopharmacology, ISSN 0893-133X, 2014, Volume 39, Issue 7, pp. 1578 - 1593
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 07/2016, Volume 57, Issue 30, pp. 3252 - 3253
A second-generation approach to the BC spirocycle of ‘upenamide is reported. Central to the synthesis is an endo selective Diels–Alder reaction between 1-(... 
Hemiaminal | Diels–Alder | Staudinger reaction | Quaternary stereocenter | Stereocontrol | CORE | CHEMISTRY, ORGANIC | Diels-Alder
Journal Article
ACS Chemical Neuroscience, ISSN 1948-7193, 07/2014, Volume 5, Issue 10, pp. 920 - 942
Journal Article
Acta Crystallographica Section A Foundations and Advances, ISSN 2053-2733, 08/2016, Volume 72, Issue a1, pp. s26 - s26
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2019, Volume 29, Issue 3, p. 362
This letter describes a focused exercise to explore the role of the [beta]-amino carboxamide moiety found in all of the first generation M.sub.4 PAMs and... 
Medical colleges | Hydrogen | Liability (Law) | Drug discovery | Hydrogen bonding
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2019, Volume 29, Issue 3, pp. 362 - 366
This letter describes a focused exercise to explore the role of the β-amino carboxamide moiety found in all of the first generation M PAMs and question if the... 
Tricycle | Structure-Activity Relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
International Journal of Antimicrobial Agents, ISSN 0924-8579, 10/2019, Volume 54, Issue 4, pp. 496 - 501
Leishmania parasites are the causative agents of a wide spectrum of human diseases. The clinical manifestations of leishmaniasis range from self-healing skin... 
High-throughput screening | 2,4-diaminoquinazoline | Leishmaniasis | Drug discovery | DRUG | INFECTIOUS DISEASES | IN-VITRO | DISEASES | MICROBIOLOGY | PHARMACOLOGY & PHARMACY | PROMASTIGOTES | Chemotherapy | World health | Skin | Drug resistance | Cancer
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 12/2017, Volume 27, Issue 23, pp. 5179 - 5184
Herein we describe the continued optimization of M positive allosteric modulators (PAMs) within the 5-amino-thieno[2,3- ]pyridazine series of compounds. In... 
Azetidine | Schizophrenia | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor | Positive Allosteric modulator (PAM)
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, pp. 1714 - 1718
This letter describes progress towards an M PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-... 
Structure-activity relationship (SAR) | Pharmacokinetics | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 07/2019, Volume 29, Issue 14, p. 1714
This letter describes progress towards an M.sub.4 PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the... 
Medical colleges | Neurosciences | Drug discovery
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2019, Volume 29, Issue 16, pp. 2224 - 2228
This letter describes progress towards an M PAM preclinical candidate inspired by an unexpected aldehyde oxidase (AO) metabolite of a novel, CNS penetrant... 
Aldehyde oxidase (AO) | Structure-activity relationship (SAR) | Positive allosteric modulator (PAM) | Muscarinic acetylcholine receptor
Journal Article