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Items: 31

1.

Hit-to-Lead Studies for the Antimalarial Tetrahydroisoquinolone Carboxanilides.

Floyd DM, Stein P, Wang Z, Liu J, Castro S, Clark JA, Connelly M, Zhu F, Holbrook G, Matheny A, Sigal MS, Min J, Dhinakaran R, Krishnan S, Bashyum S, Knapp S, Guy RK.

J Med Chem. 2016 Sep 8;59(17):7950-62. doi: 10.1021/acs.jmedchem.6b00752. Epub 2016 Aug 25.

2.

Dimerization and comments on the reactivity of homophthalic anhydride.

Hong J, Wang Z, Levin A, Emge TJ, Floyd DM, Knapp S.

Tetrahedron Lett. 2015 Jun 3;56(23):3001-3004.

3.
4.

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.

Jiménez-Díaz MB, Ebert D, Salinas Y, Pradhan A, Lehane AM, Myrand-Lapierre ME, O'Loughlin KG, Shackleford DM, Justino de Almeida M, Carrillo AK, Clark JA, Dennis AS, Diep J, Deng X, Duffy S, Endsley AN, Fedewa G, Guiguemde WA, Gómez MG, Holbrook G, Horst J, Kim CC, Liu J, Lee MC, Matheny A, Martínez MS, Miller G, Rodríguez-Alejandre A, Sanz L, Sigal M, Spillman NJ, Stein PD, Wang Z, Zhu F, Waterson D, Knapp S, Shelat A, Avery VM, Fidock DA, Gamo FJ, Charman SA, Mirsalis JC, Ma H, Ferrer S, Kirk K, Angulo-Barturen I, Kyle DE, DeRisi JL, Floyd DM, Guy RK.

Proc Natl Acad Sci U S A. 2014 Dec 16;111(50):E5455-62. doi: 10.1073/pnas.1414221111. Epub 2014 Dec 1. Erratum in: Proc Natl Acad Sci U S A. 2015 Oct 20;112(42):E5764.

5.

N-methylimidazole promotes the reaction of homophthalic anhydride with imines.

Liu J, Wang Z, Levin A, Emge TJ, Rablen PR, Floyd DM, Knapp S.

J Org Chem. 2014 Aug 15;79(16):7593-9. doi: 10.1021/jo501316m. Epub 2014 Jul 24.

6.

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.

Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK.

J Med Chem. 2011 Jun 9;54(11):3935-49. doi: 10.1021/jm200265b. Epub 2011 May 12.

7.

Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.

Stein PD, Floyd DM, Bisaha S, Dickey J, Girotra RN, Gougoutas JZ, Kozlowski M, Lee VG, Liu EC, Malley MF, et al.

J Med Chem. 1995 Apr 14;38(8):1344-54.

PMID:
7731020
8.

A rapid and versatile method for screening endothelin converting enzyme activity.

Little DK, Floyd DM, Tymiak AA.

J Pharmacol Toxicol Methods. 1994 Aug;31(4):199-205.

PMID:
7949376
9.

The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.

Stein PD, Hunt JT, Floyd DM, Moreland S, Dickinson KE, Mitchell C, Liu EC, Webb ML, Murugesan N, Dickey J, et al.

J Med Chem. 1994 Feb 4;37(3):329-31. No abstract available.

PMID:
8308857
10.

1-Benzazepin-2-one calcium channel blockers--VI. Receptor-binding model and possible relationship to desmethoxyverapamil.

Kimball SD, Hunt JT, Barrish JC, Das J, Floyd DM, Lago MW, Lee VG, Spergel SH, Moreland S, Hedberg SA, et al.

Bioorg Med Chem. 1993 Oct;1(4):285-307.

PMID:
8081860
11.

Structure-activity studies of endothelin leading to novel peptide ETA antagonists.

Hunt JT, Lee VG, McMullen D, Liu EC, Bolgar M, Delaney CL, Festin SM, Floyd DM, Hedberg A, Natarajan S, et al.

Bioorg Med Chem. 1993 Jul;1(1):59-65.

PMID:
8081838
12.

Site-specific biotinylation. A novel approach and its application to endothelin-1 analogs and PTH-analog.

Natarajan S, Festin SM, Hedberg A, Liu EC, Floyd DM, Hunt JT.

Int J Pept Protein Res. 1992 Dec;40(6):567-74.

PMID:
1286942
13.

Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.

Das J, Floyd DM, Kimball SD, Duff KJ, Lago MW, Krapcho J, White RE, Ridgewell RE, Obermeier MT, Moreland S, et al.

J Med Chem. 1992 Jul 10;35(14):2610-7.

PMID:
1635059
14.

Pharmacological characterization of potent, long-acting thromboxane receptor antagonists, SQ 33,261 and SQ 33,552.

Harris DN, Michel IM, Goldenberg HJ, Hartl KS, Allen GT, Steinbacher TE, Schumacher WA, Han WC, Hall SE, Floyd DM, et al.

J Pharmacol Exp Ther. 1992 Apr;261(1):131-7.

PMID:
1532833
15.

Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.

Das J, Floyd DM, Kimball SD, Duff KJ, Vu TC, Lago MW, Moquin RV, Lee VG, Gougoutas JZ, Malley MF, et al.

J Med Chem. 1992 Feb 21;35(4):773-80.

PMID:
1542103
16.

Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.

Floyd DM, Kimball SD, Krapcho J, Das J, Turk CF, Moquin RV, Lago MW, Duff KJ, Lee VG, White RE, et al.

J Med Chem. 1992 Feb 21;35(4):756-72.

PMID:
1542102
17.

Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site.

Kimball SD, Floyd DM, Das J, Hunt JT, Krapcho J, Rovnyak G, Duff KJ, Lee VG, Moquin RV, Turk CF, et al.

J Med Chem. 1992 Feb 21;35(4):780-93.

PMID:
1311765
18.

Dihydropyrimidine calcium channel blockers. 3. 3-Carbamoyl-4-aryl-1,2,3,4-tetrahydro-6-methyl-5-pyrimidinecarboxylic acid esters as orally effective antihypertensive agents.

Atwal KS, Swanson BN, Unger SE, Floyd DM, Moreland S, Hedberg A, O'Reilly BC.

J Med Chem. 1991 Feb;34(2):806-11.

PMID:
1995904
19.

Dihydropyrimidine calcium channel blockers. 2. 3-substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.

Atwal KS, Rovnyak GC, Kimball SD, Floyd DM, Moreland S, Swanson BN, Gougoutas JZ, Schwartz J, Smillie KM, Malley MF.

J Med Chem. 1990 Sep;33(9):2629-35.

PMID:
2391701
20.

Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.

Atwal KS, Rovnyak GC, Schwartz J, Moreland S, Hedberg A, Gougoutas JZ, Malley MF, Floyd DM.

J Med Chem. 1990 May;33(5):1510-5.

PMID:
2329573
21.

Minimum requirements for inhibition of smooth-muscle myosin light-chain kinase by synthetic peptides.

Hunt JT, Floyd DM, Lee VG, Little DK, Moreland S.

Biochem J. 1989 Jan 1;257(1):73-8.

22.

Hydroxyamino acid specificity of smooth muscle myosin light chain kinase.

Pearson RB, Floyd DM, Hunt JT, Lee VG, Kemp BE.

Arch Biochem Biophys. 1988 Jan;260(1):37-44.

PMID:
3341750
23.

The preparation of leukocyte-poor red cells from AS-1 red cells by the spin-cool-filter method.

Helton MR, Huang ST, Floyd DM, McGowan EI.

Transfusion. 1987 May-Jun;27(3):279-80.

PMID:
3590292
24.

SQ 27,786 and SQ 28,853: two angiotensin converting enzyme inhibitors with potent diuretic activity.

DeForrest JM, Waldron TL, Powell JR, Floyd DM, Sundeen JE.

J Cardiovasc Pharmacol. 1987 Feb;9(2):154-9.

PMID:
2435992
25.

Quantitation of ABO mixed-cell populations by a peroxidase-anti-peroxidase immunoenzyme method.

Floyd DM, Huang ST, Poon MC.

Transfusion. 1982 Sep-Oct;22(5):352-4.

PMID:
6750873
26.

SQ 26,180, a novel monobactam. II Isolation, structure determination and synthesis.

Parker WL, Koster WH, Cimarusti CM, Floyd DM, Liu WC, Rathnum ML.

J Antibiot (Tokyo). 1982 Feb;35(2):189-95. No abstract available.

27.

Monobactams: isolation and structure determination.

Parker WL, Cimarusti CM, Floyd DM, Koster WH, Liu WC, Principe PA, Rathnum ML, Slusarchyk WA.

J Antimicrob Chemother. 1981 Dec;8 Suppl E:17-20. No abstract available.

PMID:
7199043
28.

Monocyclic beta-lactam antibiotics produced by bacteria.

Sykes RB, Cimarusti CM, Bonner DP, Bush K, Floyd DM, Georgopapadakou NH, Koster WM, Liu WC, Parker WL, Principe PA, Rathnum ML, Slusarchyk WA, Trejo WH, Wells JS.

Nature. 1981 Jun 11;291(5815):489-91. No abstract available.

PMID:
7015152
29.

Extraction of light filth from tea: collaborative study.

Lim FF, Barnett J, Bright A, Chaput MP, Cox C, Floyd DM, Gentry J, Thrasher J, Washbon EC.

J Assoc Off Anal Chem. 1981 Mar;64(2):287-90.

PMID:
7228825
30.

Type and hold system for better blood utilization.

Huang ST, Lair J, Floyd DM, Cole GW.

Transfusion. 1980 Nov-Dec;20(6):725-8.

PMID:
6776668
31.

11,15-Epiprostaglandin E 2 and its enantiomer. Biological activity and synthesis.

Corey EJ, Terashima S, Ramwell PW, Jessup R, Weinshenker NM, Floyd DM, Crosby GA.

J Org Chem. 1972 Sep 22;37(19):3043-4. No abstract available.

PMID:
4627020

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