Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Herbert Binch"'
Autor:
William J. Greenlee, William Billard, Herbert Binch, Lian-Yong Chen, Ruth A. Duffy, Charles Liu, Gordon Crosby, Stuart W. McCombie, John W. Clader, Jennifer Ford, Shengjian Li, Joseph A. Kozlowski, Gowei Zhou, Vice Susan F, Jean E. Lachowicz
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:319-326
Anthranilamide analogues such as 23 are potent and highly selective muscarinic M2 antagonists that also show good oral bioavailability and in vivo activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7fb6725ef949509463e302ecb37ec1f
https://doi.org/10.1016/j.bmc.2003.11.005
https://doi.org/10.1016/j.bmc.2003.11.005
Autor:
Dennis V. Nazareno, Guowei Zhou, Herbert Binch, William J. Greenlee, Mary Cohen-Williams, Jayaram R. Tagat, Diane E. Grotz, Jean E. Lachowicz, James J. Kaminski, Joseph A. Kozlowski, Gordon Crosby, Stuart W. McCombie, Vicki L. Coffin, Kathleen Cox, Vilma Ruperto, Craig D. Boyle, Samuel Chackalamannil, Ruth A. Duffy, Hubert B. Josien, Yuguang Wang, John W. Clader, William Billard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2311-2314
The potential toxicological liabilities of the M(2) muscarinic antagonist 1 were addressed by replacing the methylenedioxyphenyl moiety with a p-methoxyphenyl group, resulting in M(2) selective compounds such as 3. Several halogenated naphthamide der
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4596ee0f6758218aaf4305ca38b8523f
https://doi.org/10.1016/s0960-894x(01)00435-8
https://doi.org/10.1016/s0960-894x(01)00435-8
Autor:
Shengjian Li, Kathleen Cox, Ruth A. Duffy, C Liu, William J. Greenlee, Stuart W. McCombie, Jennifer Ford, Vicki L. Coffin, Gouwei Zhou, Vice Susan F, H Zhao, Theodros Asberom, Herbert Binch, Vilma Ruperto, Jean E. Lachowicz, Robert W. Watkins, Henry Guzik, Lisa A. Taylor, Derek B. Lowe, William Billard, Joseph A. Kozlowski, John W. Clader, R Crosby, Catherine D. Strader
Publikováno v:
Il Farmaco. 56:247-250
Alzheimer's disease (AD) is a neurodegenerative disease characterized by cognitive impairment and personality changes. The development of drugs for the treatment of the cognitive deficits of AD has focused on agents which counteract loss in cholinerg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ddc0fc1346ec5180de31419a16a4154d
https://doi.org/10.1016/s0014-827x(01)01102-8
https://doi.org/10.1016/s0014-827x(01)01102-8
Autor:
Ruth A. Duffy, Sundeep Dugar, Gordon Crosby, Vilma Ruperto, Herbert Binch, Robert D. McQuade, Lian-Yong Chen, Kristen Bratzler, John W. Clader, Lisa A. Taylor, Pradeep B. Pushpavanam, Jean E. Lachowicz, William Billard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2209-2212
Piperidine analogues of our previously described piperazine muscarinic antagonists are described. Piperidine analogues show a distinct structure–activity relationship (SAR) that differs from comparable piperazines. Compounds with high selectivity a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a0f16531fa2122abbc029d35dfcd592
https://doi.org/10.1016/s0960-894x(00)00437-6
https://doi.org/10.1016/s0960-894x(00)00437-6
Autor:
Samuel Chackalamannil, Ruth A. Duffy, William J. Greenlee, Gordon Crosby, Zhiyong Hu, Robert D. McQuade, Herbert Binch, Vilma Ruperto, William Billard, Yuguang Wang, John W. Clader, Jean E. Lachowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2247-2250
Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db62408e0f1c04cc91498acbe2956e04
https://doi.org/10.1016/s0960-894x(00)00457-1
https://doi.org/10.1016/s0960-894x(00)00457-1
Autor:
Guowei Zhou, Ruth A. Duffy, Herbert Binch, Jean E. Lachowicz, Lisa A. Taylor, William Billard, Derek B. Lowe, Joseph A. Kozlowski, Robert D. McQuade, Gordon Crosby, Vilma Ruperto, Henry Guzik
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2255-2257
Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned hu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4687a6dfde6b8966420c582c2ce3bbeb
https://doi.org/10.1016/s0960-894x(00)00438-8
https://doi.org/10.1016/s0960-894x(00)00438-8
Autor:
Samuel Chackalamannil, Ruth A. Duffy, Yuguang Wang, Herbert Binch, Zhiyong Hu, William Billard, Mary Cohen-Williams, Kathleen Cox, William J. Greenlee, Diane E. Grotz, Vilma Ruperto, Gordon Crosby, Craig D. Boyle, Vicki L. Coffin, John W. Clader, James J. Kaminski, Jean E. Lachowicz
Publikováno v:
Journal of medicinal chemistry. 45(25)
In search of a backup M(2) muscarinic receptor antagonist to the previously reported compound 1, we discovered compound (+)-14, which showed superior oral efficacy in animal models. The improvement of oral efficacy was achieved by modulating both the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8f01b5159480e9fea3765195aa02e5d
https://pubmed.ncbi.nlm.nih.gov/12459007
https://pubmed.ncbi.nlm.nih.gov/12459007
Autor:
Kathleen Cox, Vilma Ruperto, Stuart W. McCombie, Claire M. Lankin, Gordon Crosby, Vice Susan F, Vicki L. Coffin, Diane E. Grotz, Mary-Cohen Williams, Craig D. Boyle, Jean E. Lachowicz, Herbert Binch, Samuel Chackalamannil, Ruth A. Duffy, Jennifer Campion, William Billard
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(23)
We previously reported the initial discovery of a novel class of stabilized benzylidene ketal M 2 receptor antagonists. This paper discusses new analogues consisting of benzamide modifications which not only improved M 2 receptor affinity and selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14a5968458929f694f38fca5c0351bd4
https://pubmed.ncbi.nlm.nih.gov/12419388
https://pubmed.ncbi.nlm.nih.gov/12419388
Autor:
Michael Grzelak, William Billard, Henry Guzik, Herbert Binch, Derek B. Lowe, Pond Annamarie, Galen J Carey, Joseph A. Kozlowski, Mary Cohen-Williams, Gordon Crosby, Vicki L. Coffin, Robert W. Watkins, Richard P. Tedesco
Publikováno v:
European journal of pharmacology. 431(2)
The present studies were designed to assess whether the novel muscarinic M2 receptor antagonist 4-cyclohexyl-α-[4[[4-methoxyphenyl]sulphinyl]-phenyl]-1-piperazineacetonitrile (SCH 57790) could increase acetylcholine release in the central nervous sy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::388b7b6c66eb795f1e93a028ba5aee5f
https://pubmed.ncbi.nlm.nih.gov/11728425
https://pubmed.ncbi.nlm.nih.gov/11728425
Autor:
Craig D. Boyle, Gordon Crosby, Mary Cohen-Williams, Vilma Ruperto, Herbert Binch, William Billard, Lian-Yong Chen, Sundeep Dugar, Samuel Chackalamannil, Ruth A. Duffy, Vicki L. Coffin, Jean E. Lachowicz, Pradeep B. Pushpavanam
Publikováno v:
Bioorganicmedicinal chemistry letters. 10(24)
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic rece
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b406901ff829e79d78cf7c829827d951
https://pubmed.ncbi.nlm.nih.gov/11133078
https://pubmed.ncbi.nlm.nih.gov/11133078