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Items: 1 to 20 of 23


Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734,821 Pyrrolidine Bis-piperazines.

Houghten RA, Ganno ML, McLaughlin JP, Dooley CT, Eans SO, Santos RG, LaVoi T, Nefzi A, Welmaker G, Giulianotti MA, Toll L.

ACS Comb Sci. 2016 Jan 11;18(1):51-64. doi: 10.1021/acscombsci.5b00126.


Identification of Small Molecule Inhibitors of Human As(III) S-Adenosylmethionine Methyltransferase (AS3MT).

Dong H, Madegowda M, Nefzi A, Houghten RA, Giulianotti MA, Rosen BP.

Chem Res Toxicol. 2015 Dec 21;28(12):2419-25. doi: 10.1021/acs.chemrestox.5b00432. Epub 2015 Dec 6.


Diversity oriented synthesis and IKK inhibition of aminobenzimidazole tethered quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines.

Dadiboyena S, Arfaoui A, Amri H, Piedrafita FJ, Nefzi A.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):685-9. doi: 10.1016/j.bmcl.2014.11.078. Epub 2014 Dec 8.


Substituted dithiazole piperazine benzamides as novel amyloid beta peptide reducing agents.

Wang H, Wang R, Lakshmana MK, Nefzi A.

Bioorg Med Chem Lett. 2014 Sep 15;24(18):4384-8. doi: 10.1016/j.bmcl.2014.08.022. Epub 2014 Aug 13.


Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.

Wu J, Zhang Y, Maida LE, Santos RG, Welmaker GS, LaVoi TM, Nefzi A, Yu Y, Houghten RA, Toll L, Giulianotti MA.

J Med Chem. 2013 Dec 27;56(24):10103-17. doi: 10.1021/jm401543h. Epub 2013 Dec 12.


Striking reduction of amyloid plaque burden in an Alzheimer's mouse model after chronic administration of carmustine.

Hayes CD, Dey D, Palavicini JP, Wang H, Patkar KA, Minond D, Nefzi A, Lakshmana MK.

BMC Med. 2013 Mar 26;11:81. doi: 10.1186/1741-7015-11-81.


Increased diversity of libraries from libraries: chemoinformatic analysis of bis-diazacyclic libraries.

López-Vallejo F, Nefzi A, Bender A, Owen JR, Nabney IT, Houghten RA, Medina-Franco JL.

Chem Biol Drug Des. 2011 May;77(5):328-42. doi: 10.1111/j.1747-0285.2011.01100.x. Epub 2011 Mar 1.


Parallel synthesis and anti-inflammatory activity of cyclic peptides cyclosquamosin D and Met-cherimolacyclopeptide B and their analogs.

Dellai A, Maricic I, Kumar V, Arutyunyan S, Bouraoui A, Nefzi A.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5653-7. doi: 10.1016/j.bmcl.2010.08.033. Epub 2010 Aug 11.


On resin amino acid side chain attachment strategy for the head to tail synthesis of new glutamine containing gramicidin-S analogs and their antimicrobial activity.

Derbal S, Hensler M, Fang W, Nizet V, Ghedira K, Nefzi A.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5701-4. doi: 10.1016/j.bmcl.2010.08.015. Epub 2010 Aug 8.


Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.

Dadiboyena S, Nefzi A.

Eur J Med Chem. 2010 Nov;45(11):4697-707. doi: 10.1016/j.ejmech.2010.07.045. Epub 2010 Aug 6. Review.


Small molecule functional analogs of peptides that inhibit lambda site-specific recombination and bind Holliday junctions.

Ranjit DK, Rideout MC, Nefzi A, Ostresh JM, Pinilla C, Segall AM.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4531-4. doi: 10.1016/j.bmcl.2010.06.029. Epub 2010 Jun 8.


Solid-phase synthesis of N-substituted pyrrolidinone-tethered N-substituted piperidines via Ugi reaction.

Liu Z, Nefzi A.

J Comb Chem. 2010 Jul 12;12(4):566-70. doi: 10.1021/cc100054u.


Identification of two novel, potent, low-liability antinociceptive compounds from the direct in vivo screening of a large mixture-based combinatorial library.

Reilley KJ, Giulianotti M, Dooley CT, Nefzi A, McLaughlin JP, Houghten RA.

AAPS J. 2010 Sep;12(3):318-29. doi: 10.1208/s12248-010-9191-3. Epub 2010 Apr 27.


Synthesis of chiral polyaminothiazoles.

Arutyunyan S, Nefzi A.

J Comb Chem. 2010 May 10;12(3):315-7. doi: 10.1021/cc9001907. No abstract available.


Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.

Yongye AB, Appel JR, Giulianotti MA, Dooley CT, Medina-Franco JL, Nefzi A, Houghten RA, Martínez-Mayorga K.

Bioorg Med Chem. 2009 Aug 1;17(15):5583-97. doi: 10.1016/j.bmc.2009.06.026. Epub 2009 Jun 21.

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