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Items: 1 to 20 of 131

1.

Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2.

Nankervis JL, Feil SC, Hancock NC, Zheng Z, Ng HL, Morton CJ, Holien JK, Ho PW, Frazzetto MM, Jennings IG, Manallack DT, Martin TJ, Thompson PE, Parker MW.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7089-93. doi: 10.1016/j.bmcl.2011.09.109. Epub 2011 Oct 5.

PMID:
22030030
2.

Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.

Plummer MS, Cornicelli J, Roark H, Skalitzky DJ, Stankovic CJ, Bove S, Pandit J, Goodman A, Hicks J, Shahripour A, Beidler D, Lu XK, Sanchez B, Whitehead C, Sarver R, Braden T, Gowan R, Shen XQ, Welch K, Ogden A, Sadagopan N, Baum H, Miller H, Banotai C, Spessard C, Lightle S.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3438-42. doi: 10.1016/j.bmcl.2013.03.072. Epub 2013 Mar 28.

PMID:
23582272
3.

Structures of the four subfamilies of phosphodiesterase-4 provide insight into the selectivity of their inhibitors.

Wang H, Peng MS, Chen Y, Geng J, Robinson H, Houslay MD, Cai J, Ke H.

Biochem J. 2007 Dec 1;408(2):193-201.

4.

Chemical informatics uncovers a new role for moexipril as a novel inhibitor of cAMP phosphodiesterase-4 (PDE4).

Cameron RT, Coleman RG, Day JP, Yalla KC, Houslay MD, Adams DR, Shoichet BK, Baillie GS.

Biochem Pharmacol. 2013 May 1;85(9):1297-305. doi: 10.1016/j.bcp.2013.02.026. Epub 2013 Mar 5.

5.

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

Goto T, Shiina A, Yoshino T, Mizukami K, Hirahara K, Suzuki O, Sogawa Y, Takahashi T, Mikkaichi T, Nakao N, Takahashi M, Hasegawa M, Sasaki S.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3325-8. doi: 10.1016/j.bmcl.2013.03.104. Epub 2013 Apr 4.

PMID:
23602400
6.
7.

Identification of PDE4B Over 4D subtype-selective inhibitors revealing an unprecedented binding mode.

Kranz M, Wall M, Evans B, Miah A, Ballantine S, Delves C, Dombroski B, Gross J, Schneck J, Villa JP, Neu M, Somers DO.

Bioorg Med Chem. 2009 Jul 15;17(14):5336-41. doi: 10.1016/j.bmc.2009.03.061. Epub 2009 Apr 5.

PMID:
19525117
8.

Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center.

Freund YR, Akama T, Alley MR, Antunes J, Dong C, Jarnagin K, Kimura R, Nieman JA, Maples KR, Plattner JJ, Rock F, Sharma R, Singh R, Sanders V, Zhou Y.

FEBS Lett. 2012 Sep 21;586(19):3410-4. doi: 10.1016/j.febslet.2012.07.058. Epub 2012 Jul 25.

9.

Discovery of triazines as potent, selective and orally active PDE4 inhibitors.

Gewald R, Grunwald C, Egerland U.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4308-14. doi: 10.1016/j.bmcl.2013.05.099. Epub 2013 Jun 10.

PMID:
23806553
10.

C-C bond formation at C-2 of a quinoline ring: synthesis of 2-(1H-indol-3-yl)quinoline-3-carbonitrile derivatives as a new class of PDE4 inhibitors.

Kumar KS, Kiran Kumar S, Yogi Sreenivas B, Gorja DR, Kapavarapu R, Rambabu D, Rama Krishna G, Reddy CM, Basaveswara Rao MV, Parsa KV, Pal M.

Bioorg Med Chem. 2012 Apr 1;20(7):2199-207. doi: 10.1016/j.bmc.2012.02.027. Epub 2012 Feb 16.

PMID:
22386978
11.
12.

Crystal structures of the catalytic domain of phosphodiesterase 4B complexed with AMP, 8-Br-AMP, and rolipram.

Xu RX, Rocque WJ, Lambert MH, Vanderwall DE, Luther MA, Nolte RT.

J Mol Biol. 2004 Mar 19;337(2):355-65.

PMID:
15003452
13.

Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

Goto T, Shiina A, Yoshino T, Mizukami K, Hirahara K, Suzuki O, Sogawa Y, Takahashi T, Mikkaichi T, Nakao N, Takahashi M, Hasegawa M, Sasaki S.

Bioorg Med Chem. 2013 Nov 15;21(22):7025-37. doi: 10.1016/j.bmc.2013.09.013. Epub 2013 Sep 19.

PMID:
24094436
14.

Small molecule allosteric modulators of phosphodiesterase 4.

Gurney ME, Burgin AB, Magnusson OT, Stewart LJ.

Handb Exp Pharmacol. 2011;(204):167-92. doi: 10.1007/978-3-642-17969-3_7. Review.

PMID:
21695640
15.

Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).

Day JP, Lindsay B, Riddell T, Jiang Z, Allcock RW, Abraham A, Sookup S, Christian F, Bogum J, Martin EK, Rae RL, Anthony D, Rosair GM, Houslay DM, Huston E, Baillie GS, Klussmann E, Houslay MD, Adams DR.

J Med Chem. 2011 May 12;54(9):3331-47. doi: 10.1021/jm200070e. Epub 2011 Apr 13.

PMID:
21456625
16.

2-Trifluoroacetylthiophenes, a novel series of potent and selective class II histone deacetylase inhibitors.

Jones P, Bottomley MJ, Carfí A, Cecchetti O, Ferrigno F, Lo Surdo P, Ontoria JM, Rowley M, Scarpelli R, Schultz-Fademrecht C, Steinkühler C.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3456-61. doi: 10.1016/j.bmcl.2008.02.026. Epub 2008 Feb 14.

PMID:
18440229
17.

Pharmacophore modeling and virtual screening for the discovery of new type 4 cAMP phosphodiesterase (PDE4) inhibitors.

Niu M, Dong F, Tang S, Fida G, Qin J, Qiu J, Liu K, Gao W, Gu Y.

PLoS One. 2013 Dec 10;8(12):e82360. doi: 10.1371/journal.pone.0082360. eCollection 2013.

18.

Discovery of oxazole-based PDE4 inhibitors with picomolar potency.

Kuang R, Shue HJ, Xiao L, Blythin DJ, Shih NY, Chen X, Gu D, Schwerdt J, Lin L, Ting PC, Cao J, Aslanian R, Piwinski JJ, Prelusky D, Wu P, Zhang J, Zhang X, Celly CS, Billah M, Wang P.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2594-7. doi: 10.1016/j.bmcl.2012.01.115. Epub 2012 Feb 14.

PMID:
22401864
19.

Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors.

Kato Y, Kawasaki M, Nigo T, Nakamura S, Fusano A, Teranishi Y, Ito MN, Sumiyoshi T.

Bioorg Med Chem. 2013 Sep 15;21(18):5851-4. doi: 10.1016/j.bmc.2013.07.007. Epub 2013 Jul 14.

PMID:
23910988
20.

Crystal structure of phosphodiesterase 4D and inhibitor complex(1).

Lee ME, Markowitz J, Lee JO, Lee H.

FEBS Lett. 2002 Oct 23;530(1-3):53-8.

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