70404-25-0Relevant academic research and scientific papers
IMIDAZO [2,1-B] PURINE DERIVATIVES AS TRPA1 MODULATORS
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Page/Page column 21, (2009/12/27)
The present invention provides TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPAl (Transient Receptor Potenti
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity
Ahn, Ho-Sam,Bercovici, Ana,Boykow, George,Bronnenkant, Alan,Chackalamannil, Samuel,Chow, Jason,Cleven, Renee,Cook, John,Czarniecki, Michael,Domalski, Carol,Fawzi, Ahmad,Green, Michael,Gündes, Asli,Ho, Ginny,Laudicina, Malvina,Lindo, Neil,Ma, Ke,Manna, Mahua,McKittrick, Brian,Mirzai, Bita,Nechuta, Terry,Neustadt, Bernard,Puchalski, Chester,Pula, Kathryn,Silverman, Lisa,Smith, Elizabeth,Stamford, Andrew,Tedesco, Richard P.,Tsai, Hsingan,Tulshian, Deen,Vaccaro, Henry,Watkins, Robert W.,Weng, Xiaoyu,Witkowski, Joseph T.,Xia, Yan,Zhang, Hongtao
, p. 2196 - 2210 (2007/10/03)
Tetracyclic guanines have been shown to be potent and selective inhibitors of the cGMP-hydrolyzing enzymes PDE1 and PDE5. In general, these compounds are inactive or only weakly active as inhibitors of PDE3, which is a major isozyme involved in cAMP hydrolysis. Structureactivity relationships are developed at N-l, C-2, N-3, and N-5 on the core nucleus. Compound 31, with an IC50 of 70 pM, is the most potent inhibitor of PDE1, while 50, with an IC50 of 4 nM, is the most potent inhibitor of PDE5. Compounds 20, 22, 30, and 50 are potent dual inhibitors with IC50 values below 30 nM for both PDE1 and PDE5. Compounds 12, 20, and 28 reduced blood pressure by more than 45 mmHg when administered orally at 10 mg/kg to the spontaneously hypertensive rat (SHR).
1-Substituted xanthines
Bridson,Wang
, p. 855 - 858 (2007/10/02)
A convenient general procedure for the preparation of 1-alkyl-, 1-aryl-, and 1-aminoxanthines from an easily prepared imidazole precursor is described.
Polycyclic guanine derivatives
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, (2008/06/13)
Novel polycylic guanine derivatives of the formula: STR1 wherein J is oxygen or sulfur, R1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with ar
SUBSTITUTED XANTHINES AND CYTOKININ ANALOGUES AS INHIBITORS OF CYTOKININ N-GLUCOSYLATION
Hocart, Charles H.,Letham, David S.,Parker, Charles W.
, p. 2477 - 2486 (2007/10/02)
A series of 3-substituted xanthines, 2-(2-hydroxy-2-methylpropylamino)-9-methyl-6-benzylaminopurine and 7-benzylaminooxazolopyrimidine were synthesized as potential inhibitors of cytokinin N-glucosylation.In maize leaf segments the latter compound
