Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Richard Apodaca"'
Autor:
Richard Apodaca
Despite its widespread use, Simplified Molecular Input Line Entry System (SMILES) remains underspecified. The lack of a detailed specification encourages improvisation by software developers, complicates data standardization efforts, and undermines e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6dc485800236e37f226f6bf0f25fc3e0
https://doi.org/10.26434/chemrxiv-2022-01ltp
https://doi.org/10.26434/chemrxiv-2022-01ltp
Autor:
Ann J. Barbier, Steven B Sands, Lilian Y Li, Anthony Ndifor, Chandra R. Shah, Kirsten L. Morton, Michael A. Letavic, Timothy W. Lovenberg, Anne Bonneville, Heather McAllister, Neelakandha S. Mani, Ian Fraser, Kiev S. Ly, Richard Apodaca, Nicholas I. Carruthers, Manoj Bajpai, Swanson Devin M, Michelle Kramer, Christine Dugovic, Sandra S Snook, Chennagiri R. Pandit, Jonathan Shelton, Wei Xiao, Leah Aluisio, Pascal Bonaventure, Brian Lord, S Diane Nepomuceno
Publikováno v:
ACS Medicinal Chemistry Letters. 6:450-454
The preclinical characterization of novel phenyl(piperazin-1-yl)methanones that are histamine H3 receptor antagonists is described. The compounds described are high affinity histamine H3 antagonists. Optimization of the physical properties of these h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb111c3b07b944a678c3abee290cc57f
https://doi.org/10.1021/ml5005156
https://doi.org/10.1021/ml5005156
Autor:
Sandra R. Chaplan, Brian Scott, Michele C. Rizzolio, Joan Pierce, Natalie A. Hawryluk, Mark Seierstad, Leon Chang, J. Guy Breitenbucher, Michelle L. Wennerholm, Mark J. Karbarz, Richard Apodaca, Sandy J. Wilson, John M. Keith, James A. Palmer, Allison Chambers, Michael Webb, Lin Luo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1280-1284
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc169c27063de79ede8ba3a615dade39
https://doi.org/10.1016/j.bmcl.2014.01.064
https://doi.org/10.1016/j.bmcl.2014.01.064
Autor:
Sandy J. Wilson, Brian Scott, Mark S. Tichenor, Michele C. Rizzolio, Sandra R. Chaplan, Michael Webb, James A. Palmer, J. Guy Breitenbucher, Michelle L. Wennerholm, Raymond Rynberg, Mark Seierstad, Wei Xiao, Mark J. Karbarz, Richard Apodaca, John M. Keith, William M. Jones, Joan Pierce
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(13)
The SAR of brain penetration for a series of heteroaryl piperazinyl- and piperadinyl-urea fatty acid amide hydrolase (FAAH) inhibitors is described. Brain/plasma (B/P) ratios ranging from >4:1 to as low as 0.02:1 were obtained through relatively simp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3ae76e3b864bc6dbfc824e2ac203ac5
https://pubmed.ncbi.nlm.nih.gov/27189675
https://pubmed.ncbi.nlm.nih.gov/27189675
Autor:
Timothy W. Lovenberg, Lisa Dvorak, Jamin D. Boggs, Brian Lord, Curt Mazur, Swanson Devin M, Pascal Bonaventure, Richard Apodaca, Chandra R. Shah, Kirsten L. Morton, Ann J. Barbier, Mark A. Feinstein, Sandy J. Wilson, Nicholas I. Carruthers, Wei Xiao
Publikováno v:
European Journal of Medicinal Chemistry. 44:4413-4425
A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H 3 receptor (hH 3 R). Nine of the twenty-eight compounds tested were found
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::191de461163ea927780543b36eb2f631
https://doi.org/10.1016/j.ejmech.2009.06.007
https://doi.org/10.1016/j.ejmech.2009.06.007
Autor:
James Guy Breitenbucher, Michelle Wennerholm, Sean Brown, James A. Palmer, John M. Keith, Chui-Se Tham, Jiejun Wu, Sandy J. Wilson, Michael Webb, Mark J. Karbarz, Lin Luo, Sandra R. Chaplan, Brian Scott, Leon Chang, Richard Apodaca
Publikováno v:
Anesthesia & Analgesia. 108:316-329
Fatty acid amide hydrolase (FAAH) is an integral membrane enzyme within the amidase-signature family. It catalyzes the hydrolysis of several endogenous biologically active lipids, including anandamide (arachidonoyl ethanolamide), oleoyl ethanolamide,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0041cb9146992a5748a12d4ea0cac20f
https://doi.org/10.1213/ane.0b013e31818c7cbd
https://doi.org/10.1213/ane.0b013e31818c7cbd
Autor:
James A. Palmer, Michael Webb, Michelle Wennerholm, Pattabiraman Kanaka, Mark J. Karbarz, Sandy J. Wilson, Sandra R. Chaplan, Chui-Se Tham, Lin Luo, Brian Scott, Mark Seierstad, J. Guy Breitenbucher, Wei Xiao, Jiejun Wu, Richard Apodaca, John M. Keith, Sean Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4838-4843
A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52fa7be7ec1200469cf9e6da14674efa
https://doi.org/10.1016/j.bmcl.2008.07.081
https://doi.org/10.1016/j.bmcl.2008.07.081
Autor:
Sandy J. Wilson, Timothy W. Lovenberg, Wei Xiao, Richard Apodaca, Swanson Devin M, Nicholas I. Carruthers, Ann J. Barbier, Jamin D. Boggs
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:897-900
Aplysamine-1 (1), a marine natural product, was synthesized and screened for in vitro activity at the human and rat histamine H3 receptors. Aplysamine-1 (1) was found to possess a high binding affinity for the human H3 receptor (Ki = 30+/-4 nM). Synt
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9dda172d78884728815e047fd635c5f
https://doi.org/10.1016/j.bmcl.2005.11.003
https://doi.org/10.1016/j.bmcl.2005.11.003
Autor:
Curt A. Dvorak, Craig W. Berridge, Timothy W. Lovenberg, Sandy J. Wilson, Jamin D. Boggs, Wei Xiao, Ann J. Barbier, Richard Apodaca, Nicholas I. Carruthers
Publikováno v:
Journal of Medicinal Chemistry. 48:2229-2238
Two new series of 4-(1-alkyl-piperidin-4-yloxy)-benzonitriles and 4-(1-isopropyl-piperidin-4-yloxy)-benzylamines have been prepared. In vitro activity was determined at the recombinant human H(3) receptor and several members of these new series were
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbd05bc1ee71de543278feafe86b3e46
https://doi.org/10.1021/jm049212n
https://doi.org/10.1021/jm049212n
Autor:
Leah Aluisio, Timothy W. Lovenberg, Brian Lord, Jamin D. Boggs, Cindy Pudiak, Xavier Langlois, Christine Dugovic, Curt Mazur, Wei Xiao, Richard Apodaca, Sandy J. Wilson, Nicholas I. Carruthers, Ann J. Barbier, Craig W. Berridge, Aaron D. Laposky
Publikováno v:
British Journal of Pharmacology. 143:649-661
1 1-[4-(3-piperidin-1-yl-propoxy)-benzyl]-piperidine (JNJ-5207852) is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. JNJ-5207852 is selective for the H3 receptor, wit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::00bd0cdbcc779c1237adce49d5fba483
https://doi.org/10.1038/sj.bjp.0705964
https://doi.org/10.1038/sj.bjp.0705964