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Items: 1 to 20 of 109

1.

A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.

Atobe M, Maekawara N, Ishiguro N, Sogame S, Suenaga Y, Kawanishi M, Suzuki H, Jinno N, Tanaka E, Miyoshi S.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2106-10. doi: 10.1016/j.bmcl.2013.01.121. Epub 2013 Feb 9.

PMID:
23453070
2.

Design, synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors.

Atobe M, Maekawara N, Kawanishi M, Suzuki H, Tanaka E, Miyoshi S.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2111-6. doi: 10.1016/j.bmcl.2013.01.120. Epub 2013 Feb 9.

PMID:
23453072
3.

Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.

Sogame S, Suenaga Y, Atobe M, Kawanishi M, Tanaka E, Miyoshi S.

Eur J Med Chem. 2014 Jan;71:250-8. doi: 10.1016/j.ejmech.2013.10.075. Epub 2013 Nov 15.

PMID:
24316668
4.

Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).

Bursavich MG, Gilbert AM, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1185-8. Epub 2006 Dec 12.

PMID:
17210251
5.

Synthesis and evaluation of 2(3H)-thiazole thiones as tyrosinase inhibitors.

Emami S, Hosseinimehr SJ, Shahrbandi K, Enayati AA, Esmaeeli Z.

Arch Pharm (Weinheim). 2012 Aug;345(8):629-37. doi: 10.1002/ardp.201200028. Epub 2012 Apr 25.

PMID:
22532401
6.

Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.

Yu XY, Hill JM, Yu G, Wang W, Kluge AF, Wendler P, Gallant P.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):375-80.

PMID:
10091687
7.

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.

Maingot L, Elbakali J, Dumont J, Bosc D, Cousaert N, Urban A, Deglane G, Villoutreix B, Nagase H, Sperandio O, Leroux F, Deprez B, Deprez-Poulain R.

Eur J Med Chem. 2013 Nov;69:244-61. doi: 10.1016/j.ejmech.2013.08.027. Epub 2013 Aug 30.

PMID:
24044937
8.

N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).

Gilbert AM, Bursavich MG, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6454-7. doi: 10.1016/j.bmcl.2008.10.065. Epub 2008 Oct 18.

PMID:
18974001
9.

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.

Nuti E, Santamaria S, Casalini F, Yamamoto K, Marinelli L, La Pietra V, Novellino E, Orlandini E, Nencetti S, Marini AM, Salerno S, Taliani S, Da Settimo F, Nagase H, Rossello A.

Eur J Med Chem. 2013 Apr;62:379-94. doi: 10.1016/j.ejmech.2012.12.058. Epub 2013 Jan 11.

PMID:
23376997
10.

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

Das J, Liu C, Moquin RV, Lin J, Furch JA, Spergel SH, Doweyko AM, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2006 May 1;16(9):2411-5. Epub 2006 Feb 14. Erratum in: Bioorg Med Chem Lett. 2006 Aug 1;16(15):4148. Doweyko, Arthur M [added].

PMID:
16481166
11.

Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors.

Shiozaki M, Maeda K, Miura T, Ogoshi Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1575-80. doi: 10.1016/j.bmcl.2009.02.024. Epub 2009 Feb 11.

PMID:
19243944
12.
13.

Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.

Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR.

J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5.

PMID:
25415648
14.

Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.

Gilmore JL, King BW, Asakawa N, Harrison K, Tebben A, Sheppeck JE 2nd, Liu RQ, Covington M, Duan JJ.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4678-82. Epub 2007 Jun 7.

PMID:
17576061
15.

Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.

Liu Y, Zhang L, Gong J, Fang H, Liu A, Du G, Xu W.

J Enzyme Inhib Med Chem. 2011 Aug;26(4):506-13. doi: 10.3109/14756366.2010.534732. Epub 2010 Dec 14.

PMID:
21143042
16.

5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.

Gilbert AM, Bursavich MG, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1189-92. Epub 2006 Dec 12.

PMID:
17210252
17.

Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.

Xiang JS, Hu Y, Rush TS, Thomason JR, Ipek M, Sum PE, Abrous L, Sabatini JJ, Georgiadis K, Reifenberg E, Majumdar M, Morris EA, Tam S.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):311-6. Epub 2005 Nov 3.

PMID:
16275085
18.

Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.

Andrews DM, Stokes ES, Carr GR, Matusiak ZS, Roberts CA, Waring MJ, Brady MC, Chresta CM, East SJ.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2580-4. doi: 10.1016/j.bmcl.2008.03.041. Epub 2008 Mar 16.

PMID:
18378449
19.

Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.

Shirude PS, Madhavapeddi P, Naik M, Murugan K, Shinde V, Nandishaiah R, Bhat J, Kumar A, Hameed S, Holdgate G, Davies G, McMiken H, Hegde N, Ambady A, Venkatraman J, Panda M, Bandodkar B, Sambandamurthy VK, Read JA.

J Med Chem. 2013 Nov 14;56(21):8533-42. doi: 10.1021/jm4012033. Epub 2013 Oct 25.

PMID:
24107081
20.

Synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase activity by imidazo[2,1-b]thiazole derivatives.

Andreani A, Granaiola M, Guardigli M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Roda A.

Eur J Med Chem. 2005 Dec;40(12):1331-4. Epub 2005 Aug 29.

PMID:
16129518
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