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Items: 38

1.

6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity.

Zhang YM, Greco MN, Macielag MJ, Teleha CA, DesJarlais RL, Tang Y, Ho G, Hou C, Chen C, Zhao S, Kauffman J, Camacho R, Qi J, Murray W, Demarest K, Leonard J.

J Med Chem. 2018 Nov 21;61(22):10276-10298. doi: 10.1021/acs.jmedchem.8b01467. Epub 2018 Oct 31.

PMID:
30339387
2.

Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.

Matthews JM, McNally JJ, Connolly PJ, Xia M, Zhu B, Black S, Chen C, Hou C, Liang Y, Tang Y, Macielag MJ.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5346-5349. doi: 10.1016/j.bmcl.2016.09.025. Epub 2016 Sep 10.

PMID:
27671496
3.

Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.

Zhu B, Matthews JM, Xia M, Black S, Chen C, Hou C, Liang Y, Tang Y, Macielag MJ.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5597-5601. doi: 10.1016/j.bmcl.2016.09.026. Epub 2016 Sep 12.

PMID:
27671499
4.

7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors.

Grant EB, Foleno BD, Goldschmidt R, Hilliard JJ, Lin SC, Morrow B, Paget SD, Weidner-Wells MA, Xu X, Xu X, Murray WV, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5502-6. doi: 10.1016/j.bmcl.2014.10.014. Epub 2014 Oct 12.

PMID:
25455493
5.

Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists.

Zhu B, Xia M, Xu X, Ludovici DW, Tennakoon M, Youngman MA, Matthews JM, Dax SL, Colburn RW, Qin N, Hutchinson TL, Lubin ML, Brandt MR, Stone DJ, Flores CM, Macielag MJ.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2234-7. doi: 10.1016/j.bmcl.2013.01.062. Epub 2013 Feb 4.

PMID:
23411075
6.

Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution.

Schalk-Hihi C, Schubert C, Alexander R, Bayoumy S, Clemente JC, Deckman I, DesJarlais RL, Dzordzorme KC, Flores CM, Grasberger B, Kranz JK, Lewandowski F, Liu L, Ma H, Maguire D, Macielag MJ, McDonnell ME, Mezzasalma Haarlander T, Miller R, Milligan C, Reynolds C, Kuo LC.

Protein Sci. 2011 Apr;20(4):670-83. doi: 10.1002/pro.596. Epub 2011 Mar 1.

7.

New β-lactam antibiotics and β-lactamase inhibitors.

Bush K, Macielag MJ.

Expert Opin Ther Pat. 2010 Oct;20(10):1277-93. doi: 10.1517/13543776.2010.515588. Review.

PMID:
20839927
8.

In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.

Morrow BJ, He W, Amsler KM, Foleno BD, Macielag MJ, Lynch AS, Bush K.

Antimicrob Agents Chemother. 2010 May;54(5):1955-64. doi: 10.1128/AAC.01374-09. Epub 2010 Feb 22.

9.

Synthesis and antibacterial activity of 7-(1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-7-yl) quinolones.

Zhu B, Marinelli BA, Goldschmidt R, Foleno BD, Hilliard JJ, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4933-6. doi: 10.1016/j.bmcl.2009.07.087. Epub 2009 Jul 22.

PMID:
19646867
10.

In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.

Hilliard JJ, Fernandez J, Melton J, Macielag MJ, Goldschmidt R, Bush K, Abbanat D.

Antimicrob Agents Chemother. 2009 May;53(5):2028-33. doi: 10.1128/AAC.00833-08. Epub 2009 Mar 9.

11.

Synthesis and antibacterial activity of 3-keto-6-O-carbamoyl-11,12-cyclic thiocarbamate erythromycin A derivatives.

Zhu B, Marinelli BA, Abbanat D, Foleno BD, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3900-4. Epub 2007 May 3.

PMID:
17502142
12.

Anti-MRSA beta-lactams in development, with a focus on ceftobiprole: the first anti-MRSA beta-lactam to demonstrate clinical efficacy.

Bush K, Heep M, Macielag MJ, Noel GJ.

Expert Opin Investig Drugs. 2007 Apr;16(4):419-29. Review.

PMID:
17371191
13.

In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.

Foleno BD, Abbanat D, Goldschmidt RM, Flamm RK, Paget SD, Webb GC, Wira E, Macielag MJ, Bush K.

Antimicrob Agents Chemother. 2007 Jan;51(1):361-5. Epub 2006 Nov 13.

14.

Synthesis and antibacterial activity of C6-carbazate ketolides.

Tennakoon MA, Henninger TC, Abbanat D, Foleno BD, Hilliard JJ, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6231-5. Epub 2006 Sep 25.

PMID:
16997549
15.

Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.

Paget SD, Boggs CM, Foleno BD, Goldschmidt RM, Hlasta DJ, Weidner-Wells MA, Werblood HM, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4537-42. Epub 2006 Jun 27.

PMID:
16806921
16.

Synthesis and antibacterial activity of 6-O-heteroarylcarbamoyl-11,12-lactoketolides.

Grant EB, Guiadeen D, Abbanat D, Foleno BD, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1929-33. Epub 2006 Jan 30.

PMID:
16446089
17.

Synthesis and antibacterial activity of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives.

Zhu B, Marinelli BA, Abbanat D, Foleno BD, Henninger TC, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1054-9. Epub 2005 Nov 11.

PMID:
16289812
18.

Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.

Jiang W, Guan J, Macielag MJ, Zhang S, Qiu Y, Kraft P, Bhattacharjee S, John TM, Haynes-Johnson D, Lundeen S, Sui Z.

J Med Chem. 2005 Mar 24;48(6):2126-33.

PMID:
15771456
19.

Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics.

Henninger TC, Xu X, Abbanat D, Baum EZ, Foleno BD, Hilliard JJ, Bush K, Hlasta DJ, Macielag MJ.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4495-9.

PMID:
15357979
20.

The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.

Weidner-Wells MA, Werblood HM, Goldschmidt R, Bush K, Foleno BD, Hilliard JJ, Melton J, Wira E, Macielag MJ.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3069-72.

PMID:
15149646
21.

Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.

Lanter JC, Sui Z, Macielag MJ, Fiordeliso JJ, Jiang W, Qiu Y, Bhattacharjee S, Kraft P, John TM, Haynes-Johnson D, Craig E, Clancy J.

J Med Chem. 2004 Jan 29;47(3):656-62.

PMID:
14736245
22.

Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.

Paget SD, Foleno BD, Boggs CM, Goldschmidt RM, Hlasta DJ, Weidner-Wells MA, Werblood HM, Wira E, Bush K, Macielag MJ.

Bioorg Med Chem Lett. 2003 Dec 1;13(23):4173-7.

PMID:
14622996
23.

Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.

Sui Z, Guan J, Macielag MJ, Jiang W, Qiu Y, Kraft P, Bhattacharjee S, John TM, Craig E, Haynes-Johnson D, Clancy J.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):761-5.

PMID:
12639576
24.

Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.

Jiang W, Sui Z, Macielag MJ, Walsh SP, Fiordeliso JJ, Lanter JC, Guan J, Qiu Y, Kraft P, Bhattacharjee S, Craig E, Haynes-Johnson D, John TM, Clancy J.

J Med Chem. 2003 Jan 30;46(3):441-4.

PMID:
12540243
25.

Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.

Sui Z, Guan J, Macielag MJ, Jiang W, Zhang S, Qiu Y, Kraft P, Bhattacharjee S, John TM, Haynes-Johnson D, Clancy J.

J Med Chem. 2002 Sep 12;45(19):4094-6.

PMID:
12213052
26.

Amidino benzimidazole inhibitors of bacterial two-component systems.

Weidner-Wells MA, Ohemeng KA, Nguyen VN, Fraga-Spano S, Macielag MJ, Werblood HM, Foleno BD, Webb GC, Barrett JF, Hlasta DJ.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1545-8.

PMID:
11412977
27.

Inhibitors of bacterial two-component signalling systems.

Macielag MJ, Goldschmidt R.

Expert Opin Investig Drugs. 2000 Oct;9(10):2351-69. Review.

PMID:
11060812
28.

SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.

Sui Z, Guan J, Hlasta DJ, Macielag MJ, Foleno BD, Goldschmidt RM, Loeloff MJ, Webb GC, Barrett JF.

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1929-34.

PMID:
9873461
29.

Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.

Hlasta DJ, Demers JP, Foleno BD, Fraga-Spano SA, Guan J, Hilliard JJ, Macielag MJ, Ohemeng KA, Sheppard CM, Sui Z, Webb GC, Weidner-Wells MA, Werblood H, Barrett JF.

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1923-8.

PMID:
9873460
30.

Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria.

Macielag MJ, Demers JP, Fraga-Spano SA, Hlasta DJ, Johnson SG, Kanojia RM, Russell RK, Sui Z, Weidner-Wells MA, Werblood H, Foleno BD, Goldschmidt RM, Loeloff MJ, Webb GC, Barrett JF.

J Med Chem. 1998 Jul 30;41(16):2939-45.

PMID:
9685233
31.

Antibacterial agents that inhibit two-component signal transduction systems.

Barrett JF, Goldschmidt RM, Lawrence LE, Foleno B, Chen R, Demers JP, Johnson S, Kanojia R, Fernandez J, Bernstein J, Licata L, Donetz A, Huang S, Hlasta DJ, Macielag MJ, Ohemeng K, Frechette R, Frosco MB, Klaubert DH, Whiteley JM, Wang L, Hoch JA.

Proc Natl Acad Sci U S A. 1998 Apr 28;95(9):5317-22.

32.

Motilin and OHM-11526 activate a calcium current in human and canine jejunal circular smooth muscle.

Farrugia G, Macielag MJ, Peeters TL, Sarr MG, Galdes A, Szurszewski JH.

Am J Physiol. 1997 Aug;273(2 Pt 1):G404-12.

PMID:
9277420
33.

Antagonistic properties of [Phe3,Leu13]porcine motilin.

Depoortere I, Macielag MJ, Galdes A, Peeters TL.

Eur J Pharmacol. 1995 Nov 24;286(3):241-7.

PMID:
8608785
34.

Synthesis and characterization of site-specific biotinylated probes for the motilin receptor.

Macielag MJ, Peeters T, Depoortere I.

Int J Pept Protein Res. 1994 Dec;44(6):582-8.

PMID:
7705980
35.

The motilin antagonist ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit.

Peeters TL, Depoortere I, Macielag MJ, Dharanipragada R, Marvin MS, Florance JR, Galdes A.

Biochem Biophys Res Commun. 1994 Jan 28;198(2):411-6.

PMID:
8297350
36.

D-amino acid and alanine scans of the bioactive portion of porcine motilin.

Peeters TL, Macielag MJ, Depoortere I, Konteatis ZD, Florance JR, Lessor RA, Galdes A.

Peptides. 1992 Nov-Dec;13(6):1103-7.

PMID:
1494493
37.

Synthesis and in vitro evaluation of [Leu13]porcine motilin fragments.

Macielag MJ, Peeters TL, Konteatis ZD, Florance JR, Depoortere I, Lessor RA, Bare LA, Cheng YS, Galdes A.

Peptides. 1992 May-Jun;13(3):565-9.

PMID:
1523168
38.

Capillary zone electrophoresis studies of motilin peptides. Effects of charge, hydrophobicity, secondary structure and length.

Florance JR, Konteatis ZD, Macielag MJ, Lessor RA, Galdes A.

J Chromatogr. 1991 Oct 18;559(1-2):391-9.

PMID:
1761627

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