Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Renee M Chabin"'
Autor:
Fa-Xiang Ding, Urmi R. Bhatt, Hong C. Shen, Wayne M. Geissler, Judith N. Gorski, Ranabir SinhaRoy, Margarita Garcia-Calvo, Jinlong Jiang, Xinchun Tong, Renee M. Chabin, Beth Ann Murphy, Dong-Ming Shen, Shirly Pinto, Jeffrey J. Hale, Dan Xie, Andreas Verras, Mike E. Lassman, Qing Chen, Suoyu Xu, Judyann Wiltsie, Zhu Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1550-1556
A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure–activity relationship (SAR) is focused on improving PrCP activity and metabolic stability,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c0fea705f75363de3cf1cb0edafcd87
https://doi.org/10.1016/j.bmcl.2012.01.002
https://doi.org/10.1016/j.bmcl.2012.01.002
Autor:
Thomas H. Graham, Urmi R. Bhatt, Dong-Ming Shen, Xinchun Tong, Mike E. Lassman, Kelly Bleasby, Dan Xie, Qing Chen, Shirly Pinto, Margarita Garcia-Calvo, Andreas Verras, Renee M. Chabin, Zhicai Wu, Steven L. Colletti, Suoyu Xu, Cangming Yang, James R. Tata, Zhu Shen, Ranabir SinhaRoy, Jeffrey J. Hale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1727-1730
Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good Pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1612ca458599f3caa91f1160e81053f8
https://doi.org/10.1016/j.bmcl.2011.12.098
https://doi.org/10.1016/j.bmcl.2011.12.098
Autor:
Urmi R. Bhatt, James R. Tata, Xinchun Tong, Hong C. Shen, Andreas Verras, Renee M. Chabin, Michael E. Lassman, Changyou Zhou, Margarita Garcia-Calvo, J. J. Hale, Ranabir SinhaRoy, Steven L. Colletti, Yusheng Xiong, Dong-Ming Shen, Dunlu Chen, Wayne M. Geissler, Fa-Xiang Ding, Shirly Pinto, Suoyu Xu, Dan Xie, Zhu Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1299-1305
A series of benzimidazole pyrrolidinyl amides containing a piperidinyl group were discovered as novel prolylcarboxypeptidase (PrCP) inhibitors. Low-nanomolar IC(50)'s were achieved for several analogs, of which compound 9b displayed modest ex vivo ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d3367bcef8145d697e3909a57ae1efb
https://doi.org/10.1016/j.bmcl.2011.01.090
https://doi.org/10.1016/j.bmcl.2011.01.090
Publikováno v:
Enzyme and Microbial Technology. 35:300-308
The l -lysine-adding enzyme encoded by the murE gene catalyzes the ATP-dependent formation of UDP-MurNAc- l -alanyl- d -glutamyl- l -lysine (UDP-MurNAc-tripeptide). MurE has been cloned from Streptococcus pyogenes ( Spy ) and expressed as a glutathio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::45b603d4d9943f748c3197b46fe884d1
https://doi.org/10.1016/j.enzmictec.2004.03.020
https://doi.org/10.1016/j.enzmictec.2004.03.020
Autor:
R Marschhofer, W. B. Knight, A M Edison, Mario Guarneri, Renee M. Chabin, Chiara Beatrice Vicentini, X Huang, V Andrisano, Salvatore Guccione, Thierry Langer, Paolo Giori
Publikováno v:
Scopus-Elsevier
As a part of an investigation on molecular hybrids as new serine protease inhibitors, the pyrazolo [4,3-c][1,2,5]oxadiazin-3(5H)-one ring system was selected as a model of potential mechanism-based inhibitors. Due to the inherent reactivity of this s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7875da8156982f04527dece0ba90a0a7
https://doi.org/10.1080/14756360109162352
https://doi.org/10.1080/14756360109162352
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:1643-1648
A series of transition-state analog inhibitors of the D-glutamic acid-adding enzyme (MurD) of bacterial peptidoglycan biosynthesis has been synthesized and evaluated for inhibition of the E. coli enzyme.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::083f7685d89b797885d1239f3dd17964
https://doi.org/10.1016/s0960-894x(98)00285-6
https://doi.org/10.1016/s0960-894x(98)00285-6
Autor:
C. S. Burgey, Liesch J, Shrenik K. Shah, David W. Kuo, Renee M. Chabin, B G Green, Alan L. Maycock, Gale P, Sander G. Mills, Dennis J. Underwood
Publikováno v:
Biochemistry. 34:14331-14343
The monocyclic beta-lactams reported by Knight et al. [Knight, W. B., et al. (1992) Biochemistry 31, 8160; Chabin, R., et al. (1993) Biochemistry 32, 8970] as inhibitors of human leucocyte elastase (HLE) produce stable HLE-inhibitor complexes that sl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a21c8c4964ff8ea7e572ee6a061a7fee
https://doi.org/10.1021/bi00044a010
https://doi.org/10.1021/bi00044a010
Autor:
Renee M. Chabin, Daniel S. Fletcher, William A. Hanlon, Barbara G. Green, W. B. Knight, Thomas J. Lanza, Stephen G. Pacholok, John L. Humes, Malcolm MacCoss, Philippe L. Durette, Richard A. Mumford
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:271-274
Analogs of the monocyclic β-lactam human leukocyte elastase (HLE) inhibitor L-680,833 in which the carboxyl group is replaced by phosphorous acid moieties were synthesized and found to be potent inhibitors of the enzyme ( k inact / K i in the range
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ca84286af99004f9cc4d9ded5354ccc0
https://doi.org/10.1016/0960-894x(95)00022-l
https://doi.org/10.1016/0960-894x(95)00022-l
Autor:
Filippo Russo, Renee M. Chabin, W. B. Knight, Salvatore Guccione, David W. Kuo, Giuseppe Romeo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2399-2404
A novel thiazinoindole tricyclic ring system was designed as potential inhibitors of serine proteases. The compounds were synthesized by ring closure at 80–90°C in poliphosphoric acid of the appropriate N′-alkyl or aryl substituted indolylthiour
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b6be4448adf80668703c68af64ed74a0
https://doi.org/10.1016/s0960-894x(01)80398-x
https://doi.org/10.1016/s0960-894x(01)80398-x
Autor:
Jeffrey J. Hale, Andreas Verras, Wayne M. Geissler, Margarita Garcia-Calvo, Zhu Shen, Matthew Lombardo, Ranabir SinhaRoy, Suoyu Xu, Xinchun Tong, Steven L. Colletti, Dan Xie, Urmi R. Bhatt, Zhicai Wu, Dong-Ming Shen, Shirly Pinto, Renee M. Chabin, Qing Chen, Mike E. Lassman, James R. Tata, Yusheng Xiong, Zhe Feng, Cangming Yang
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(4)
Efforts to modify the central proline portion of lead compound 4 lead to the discovery of novel prolylcarboxypeptidase (PrCP) inhibitors. Especially, replacement with alanine afforded compound 19 displaying more potent human and mouse PrCP inhibitory
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8dcc1034f6c930f822d4b151768942a3
https://pubmed.ncbi.nlm.nih.gov/22248857
https://pubmed.ncbi.nlm.nih.gov/22248857