Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Bernstein Peter Robert"'
Autor:
Xiawei Dang, Antonietta Franco, Daniel Walters, Bernstein Peter Robert, Sidney B. Williams, Lijun Fu, Sriram Devanathan, Gerald W. Dorn
Publikováno v:
J Med Chem
Mitochondrial fragmentation from defective fusion or unopposed fission contributes to many neurodegenerative diseases. Small molecule mitofusin activators reverse mitochondrial fragmentation in vitro, promising a novel therapeutic approach. The first
Autor:
Anand Tarage, Gopal Gole, Mandar Bhonde, Madhusudhan Reddy, Sharad Sharma, Harish Volam, Sudeep Sabde, Sanjeev Anant Kulkarni, Sadanand Mallurwar, Brahmam Sunkara, Ramesh Dattatraya Phadtare, Manoj Dandekar, Hemant Goyal, Samiron Phukan, Gayathri Sadasivam, Rupesh Kanhere, Maneesh Mehta, Nirmal Jana, Murthy Cheemala, Prashant Vidhate, Lal Dinchhana, Prashant B. Nigade, Bernstein Peter Robert, Prajakta Ahirrao, Rajan Goel, Aditya Naik, Vipul Pachpute, Sukanya Patra, Rajender Kumar Kamboj, Nilesh Mahajan, Kaustubh Tamane, Sneha Trivedi, M. K. Singh, Ajit Kumar Marisetti, Shankar Bhagwat, Mahip Verma, Atul Akarte, Dipak Lagad, Charudatt Samant, Venkata P. Palle, Vinod Patil, Anand Bokare, Dipak Modi, Chaitanya A. Kulkarni, Lakshmi Narasimham, Neetinkumar Reddy, Majid Bashir Sayyed, Sarita Koul, Shukla Manojkumar Ramprasad, Milind Gholve, Swati Tota, Vinod D. Chaudhari, Jayasagar Gundu, Manisha Shingare, Sachin J Mahangare, Shashikant Pawar
Publikováno v:
Journal of Medicinal Chemistry. 63:14700-14723
PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors are nonoptimal, showing weakness against at least one of the several important properties:
Autor:
Albi Francis, Javed S. Shaikh, Tariq Bhat, Sanjay P. Kurhade, Nivrutti Kamble, Harish Volam, Sadanand Mallurwar, Pushpak Bora, Prashant B. Nigade, Mandar Bhonde, Hemant Goyal, Gagan Kukreja, Nishant R. Gupta, Nageswara Rao Irlapati, Prajakta Ahirrao, Bernstein Peter Robert, Rajesh B. Shankar, Kumar Ram Naik, Sneha Naidu, Gopal Gole, Yogesh Pawar, Apparao Bommakanti, Vinod Patil, Rajendra G. Powar, V.R. Praveen Kumar, Rakesh Kumar, Prabhakaran Kamalakannan, Anil K. Hajare, Neelima Sinha, Rajender Kumar Kamboj, Jayasagar Gundu, Sharad Sharma, Nilesh Khedkar, Arun R. Jagdale, Navnath P. Karche, Venkata P. Palle, Dipak Modi, Saif Wahid, Vamsi Pagdala, Kochumalayil Shaji George, Ganesh R. Jadhav, Gourhari Jana, Rohan Limaye, Baban Thube, Lakshmi Narasimham, Harshal Khanwalkar, Shashikant Pawar, Kumar V.S. Nemmani, Rajesh Gupta, Minakshi Singh, Ramesh Kale, Ajay R. Tilekar, Samiron Phukan, Dhananjay Bakhle, Pradipta Kumar
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115819
The exploitation of GLU988 and LYS903 residues in PARP1 as targets to design isoquinolinone (I & II) and naphthyridinone (III) analogues is described. Compounds of structure I have good biochemical and cellular potency but suffered from inferior PK.
Autor:
David Aharony, Cyrus John Ohnmacht, William L. Rumsey, Bernstein Peter Robert, Gerard M. Koether, Brian B. Masek, Donald Andisik, Jeffrey S. Albert, Bruce Dembofsky
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:2653-2669
Previously we reported on the synthesis and properties of a series of highly potent piperidinyl 2-subsituted-3-cyano-1-naphthamide NK1 antagonists that includes 3 and 4. Here we report our efforts to alleviate a troublesome atropisomeric property of
Autor:
John Evenden, William L. Rumsey, David Aharony, Brian B. Masek, Gerard M. Koether, William Potts, Cyrus John Ohnmacht, Bruce Dembofsky, Bernstein Peter Robert, Jeffrey S. Albert
Publikováno v:
Tetrahedron. 60:4337-4347
We have previously described a series of antagonists that showed high potency and selectivity for the NK1 receptor. However, these compounds also had the undesirable property of existing as a mixture of four interconverting rotational isomers. Throug
Autor:
Pourashraf Mehrnaz, Russell C. Mauger, Steve Wesolowski, Phillip D Edwards, Simon Sydserff, Carine Lévesque, Maxime Tremblay, Thierry Groblewski, Vijayaratnam Santhakumar, Lois Ann Lazor, Bernstein Peter Robert, James Folmer, Pascall Giguère, William Potts, Denis Labrecque, Scott Throner, Joseph Cacciola, Mark Sylvester, Mohammed Dasser, Clay W Scott, Dean G. Brown, Andrew Griffin
Publikováno v:
Journal of medicinal chemistry. 57(3)
A new series of potent and selective histamine-3 receptor (H3R) antagonists was identified on the basis of an azaspiro[2.5]octane carboxamide scaffold. Many scaffold modifications were largely tolerated, resulting in nanomolar-potent compounds in the
Autor:
Benedict J. Kosmider, Herbert Barthlow, Bruce Dembofsky, Jeffrey S. Albert, William Potts, Robert F. Dedinas, David Aharony, William L. Rumsey, Russell Bialecki, Timothy Wayne Davenport, Scott Sherwood, Donald Andisik, Ashok B. Shenvi, Karin Kirkland, Keith Russell, Lihong Shen, Gerard M. Koether, David Stollman, Cyrus John Ohnmacht, Bernstein Peter Robert
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2769-2773
Exploration of the SAR around selective NK 2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK 1 and NK 2 antagonists. ZD6021 inhibited binding of [ 3 H]-NKA or [ 3 H]-SP to human NK 1 and NK 2
Autor:
Anna Zacco, Lois Ann Lazor, Stephanie Koch, Jian Yu, Stuart Ward, Joseph McLaughlin, Shuang Li, Christopher Becker, Patricia Schroeder, Carol Thompson, Nugiel David, Christopher A. Hurley, Donald E. Pivonka, Donna L. Maier, Gary Steelman, David Aharony, Jianwei Liu, Valerie Hoesch, Bernstein Peter Robert, Steven Wesolowski, Ye Wu, Hazel Hunt, Charles S. Elmore, Michael W. Wood, Dean G. Brown, Rebecca Urbanek, Simon Sydserff, Bruce Dembofsky, Clay W Scott, Karen Williams, Scott Throner
Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, along with nomifensine were tested in a rodent recepto
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03257ab664bd72a1d8bb75fec9134939
https://europepmc.org/articles/PMC4027539/
https://europepmc.org/articles/PMC4027539/
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2175-2178
The preparation and in vitro evaluation of a series of peptidic α′,β-diamino-α,α-difluoroketones are described. Comparison of the efficacy of these compounds to both their corresponding trifluoromethylketone and α-carboxamido-α,α-difluoroket