29274-13-3Relevant academic research and scientific papers
In silico design of novel probes for the atypical opioid receptor MRGPRX2
Lansu, Katherine,Karpiak, Joel,Liu, Jing,Huang, Xi-Ping,McCorvy, John D.,Kroeze, Wesley K.,Che, Tao,Nagase, Hiroshi,Carroll, Frank I.,Jin, Jian,Shoichet, Brian K.,Roth, Bryan L.
, p. 529 - 536 (2017)
The primate-exclusive MRGPRX2 G protein-coupled receptor (GPCR) has been suggested to modulate pain and itch. Despite putative peptide and small-molecule MRGPRX2 agonists, selective nanomolar-potency probes have not yet been reported. To identify a MRGPRX
Structural Insights into the Inhibition of Undecaprenyl Pyrophosphate Synthase from Gram-Positive Bacteria
Workman, Sean D.,Day, Jonathan,Farha, Maya A.,El Zahed, Sara S.,Bon, Chris,Brown, Eric D.,Organ, Michael G.,Strynadka, Natalie C. J.
supporting information, p. 13540 - 13550 (2021/09/20)
The polyprenyl lipid undecaprenyl phosphate (C55P) is the universal carrier lipid for the biosynthesis of bacterial cell wall polymers. C55P is synthesized in its pyrophosphate form by undecaprenyl pyrophosphate synthase (UppS), an essentialcis-prenyltransferase that is an attractive target for antibiotic development. We previously identified a compound (MAC-0547630) that showed promise as a novel class of inhibitor and an ability to potentiate β-lactam antibiotics. Here, we provide a structural model for MAC-0547630’s inhibition of UppS and a structural rationale for its enhanced effect on UppS fromBacillus subtilisversusStaphylococcus aureus. We also describe the synthesis of a MAC-0547630 derivative (JPD447), show that it too can potentiate β-lactam antibiotics, and provide a structural rationale for its improved potentiation. Finally, we present an improved structural model of clomiphene’s inhibition of UppS. Taken together, our data provide a foundation for structure-guided drug design of more potent UppS inhibitors in the future.
Evaluation of novel 7-(hetero)aryl-substituted pyrazolo[1, 5-a]pyrimidines as phosphodiesterase-4 inhibitors
Kodimuthali Arumugam,Gupta, Rajesh,Parsa, Kishore Venkata Laxmi,Prasunamba, Padala Lakshmi,Pal, Manojit
scheme or table, p. 402 - 408 (2011/10/18)
A novel series of 7-(hetero)aryl substituted-pyrazolopyrimidines, prepared via an AlCl3 induced C-C bond forming reaction of 7-chloro-5-phenyl-pyrazolo[1,5-a]pyrimidine with arenes and heteroarenes have been investigated as PDE4 inhibitors. Amo
Reactivity of the -C(Cl){double bond, long}C-C{double bond, long}N- moiety towards AlCl3-induced C-C bond forming reactions: a new synthesis of 7-(hetero)aryl-substituted pyrazolo[1,5-a]pyrimidines
Kodimuthali, Arumugam,T. C., Nishad,Prasunamba, Padala Lakshmi,Pal, Manojit
supporting information; experimental part, p. 354 - 358 (2009/04/19)
The reactivity of the -C(Cl){double bond, long}C-C{double bond, long}N- moiety towards an AlCl3-induced C-C bond forming reaction was investigated through the reaction of 7-chloro-5-phenyl-pyrazolo[1,5-a]pyrimidine with arenes and heteroarenes.
PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
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Page/Page column 34, (2008/06/13)
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
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Page 33, (2008/06/13)
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
PYRAZOLOPYRIMIDINES AS CYCLIN-DEPENDENT KINASE INHIBITORS
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Page 57, (2008/06/13)
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Synthesis and structure-activity relationship of a new series of potent angiotensin II receptor antagonists: Pyrazolo[1,5-α]pyrimidine derivatives
Shiota, Takeshi,Yamamori, Teruo,Sakai, Katsunori,Kiyokawa, Mitsugu,Honma, Tsunetoshi,Ogawa, Masayoshi,Hayashi, Kunio,Ishizuka, Natsuki,Matsumura, Ken-Ichi,Hara, Mariko,Fujimoto, Masafumi,Kawabata, Tomoji,Nakajima, Shigeyuki
, p. 928 - 938 (2007/10/03)
We have already reported 7-oxo-4,7-dihydropyrazolo[1,5-α]pyrimidine-3- carboxylic acid derivatives, which are potent in vitro angiotensin II (AII) antagonists, but have no oral antihypertensive activity. Removal of the carboxylic acid and replacement of t
