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Items: 1 to 50 of 73

1.

Impact of the Major Candida glabrata Triazole Resistance Determinants on the Activity of the Novel Investigational Tetrazoles VT-1598 and VT-1161.

Nishimoto AT, Whaley SG, Wiederhold NP, Zhang Q, Yates CM, Hoekstra WJ, Schotzinger RJ, Garvey EP, Rogers PD.

Antimicrob Agents Chemother. 2019 Sep 23;63(10). pii: e01304-19. doi: 10.1128/AAC.01304-19. Print 2019 Oct.

PMID:
31383660
2.

In Vitro Activities of the Novel Investigational Tetrazoles VT-1161 and VT-1598 Compared to the Triazole Antifungals against Azole-Resistant Strains and Clinical Isolates of Candida albicans.

Nishimoto AT, Wiederhold NP, Flowers SA, Zhang Q, Kelly SL, Morschhäuser J, Yates CM, Hoekstra WJ, Schotzinger RJ, Garvey EP, Rogers PD.

Antimicrob Agents Chemother. 2019 May 24;63(6). pii: e00341-19. doi: 10.1128/AAC.00341-19. Print 2019 Jun.

PMID:
30910896
3.

The Fungal Cyp51-Specific Inhibitor VT-1598 Demonstrates In Vitro and In Vivo Activity against Candida auris.

Wiederhold NP, Lockhart SR, Najvar LK, Berkow EL, Jaramillo R, Olivo M, Garvey EP, Yates CM, Schotzinger RJ, Catano G, Patterson TF.

Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e02233-18. doi: 10.1128/AAC.02233-18. Print 2019 Mar.

4.

Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues.

Simon B, Walmsley C, Jackson VJ, Garvey EP, Slater MJ, Berrisford DJ, Gardiner JM.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):339-341. doi: 10.1016/j.bmcl.2018.11.004. Epub 2018 Nov 9.

PMID:
30477891
5.

In Vivo Efficacy of VT-1129 against Experimental Cryptococcal Meningitis with the Use of a Loading Dose-Maintenance Dose Administration Strategy.

Wiederhold NP, Xu X, Wang A, Najvar LK, Garvey EP, Ottinger EA, Alimardanov A, Cradock J, Behnke M, Hoekstra WJ, Brand SR, Schotzinger RJ, Jaramillo R, Olivo M, Kirkpatrick WR, Patterson TF.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01315-18. doi: 10.1128/AAC.01315-18. Print 2018 Nov.

6.

The Fungal Cyp51 Inhibitor VT-1129 Is Efficacious in an Experimental Model of Cryptococcal Meningitis.

Wiederhold NP, Najvar LK, Garvey EP, Brand SR, Xu X, Ottinger EA, Alimardanov A, Cradock J, Behnke M, Hoekstra WJ, Schotzinger RJ, Jaramillo R, Olivo M, Kirkpatrick WR, Patterson TF.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e01071-18. doi: 10.1128/AAC.01071-18. Print 2018 Sep.

7.

The novel fungal CYP51 inhibitor VT-1598 is efficacious alone and in combination with liposomal amphotericin B in a murine model of cryptococcal meningitis.

Garvey EP, Sharp AD, Warn PA, Yates CM, Schotzinger RJ.

J Antimicrob Chemother. 2018 Oct 1;73(10):2815-2822. doi: 10.1093/jac/dky242.

PMID:
29947783
8.

VT-1598 inhibits the in vitro growth of mucosal Candida strains and protects against fluconazole-susceptible and -resistant oral candidiasis in IL-17 signalling-deficient mice.

Break TJ, Desai JV, Healey KR, Natarajan M, Ferre EMN, Henderson C, Zelazny A, Siebenlist U, Yates CM, Cohen OJ, Schotzinger RJ, Perlin DS, Garvey EP, Lionakis MS.

J Antimicrob Chemother. 2018 Aug 1;73(8):2089-2094. doi: 10.1093/jac/dky170.

9.

The Novel Fungal Cyp51 Inhibitor VT-1598 Is Efficacious in Experimental Models of Central Nervous System Coccidioidomycosis Caused by Coccidioides posadasii and Coccidioides immitis.

Wiederhold NP, Shubitz LF, Najvar LK, Jaramillo R, Olivo M, Catano G, Trinh HT, Yates CM, Schotzinger RJ, Garvey EP, Patterson TF.

Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e02258-17. doi: 10.1128/AAC.02258-17. Print 2018 Apr.

10.

Fungal-specific Cyp51 inhibitor VT-1598 demonstrates in vitro activity against Candida and Cryptococcus species, endemic fungi, including Coccidioides species, Aspergillus species and Rhizopus arrhizus.

Wiederhold NP, Patterson HP, Tran BH, Yates CM, Schotzinger RJ, Garvey EP.

J Antimicrob Chemother. 2018 Feb 1;73(2):404-408. doi: 10.1093/jac/dkx410.

PMID:
29190379
11.

VT-1161 protects mice against oropharyngeal candidiasis caused by fluconazole-susceptible and -resistant Candida albicans.

Break TJ, Desai JV, Natarajan M, Ferre EMN, Henderson C, Zelazny AM, Siebenlist U, Hoekstra WJ, Schotzinger RJ, Garvey EP, Lionakis MS.

J Antimicrob Chemother. 2018 Jan 1;73(1):151-155. doi: 10.1093/jac/dkx352.

12.

Prophylactic Treatment with VT-1161 Protects Immunosuppressed Mice from Rhizopus arrhizus var. arrhizus Infection.

Gebremariam T, Alkhazraji S, Lin L, Wiederhold NP, Garvey EP, Hoekstra WJ, Schotzinger RJ, Patterson TF, Filler SG, Ibrahim AS.

Antimicrob Agents Chemother. 2017 Aug 24;61(9). pii: e00390-17. doi: 10.1128/AAC.00390-17. Print 2017 Sep.

13.

Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors.

Yates CM, Garvey EP, Shaver SR, Schotzinger RJ, Hoekstra WJ.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3243-3248. doi: 10.1016/j.bmcl.2017.06.037. Epub 2017 Jun 15.

PMID:
28651982
14.

The Tetrazole VT-1161 Is a Potent Inhibitor of Trichophyton rubrum through Its Inhibition of T. rubrum CYP51.

Warrilow AGS, Parker JE, Price CL, Garvey EP, Hoekstra WJ, Schotzinger RJ, Wiederhold NP, Nes WD, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00333-17. doi: 10.1128/AAC.00333-17. Print 2017 Jul.

15.

Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity.

Hargrove TY, Garvey EP, Hoekstra WJ, Yates CM, Wawrzak Z, Rachakonda G, Villalta F, Lepesheva GI.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00570-17. doi: 10.1128/AAC.00570-17. Print 2017 Jul.

16.

Efficacy of the Investigational Antifungal VT-1161 in Treating Naturally Occurring Coccidioidomycosis in Dogs.

Shubitz LF, Roy ME, Trinh HT, Hoekstra WJ, Schotzinger RJ, Garvey EP.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e00111-17. doi: 10.1128/AAC.00111-17. Print 2017 May.

17.

Fungal CYP51 Inhibitors VT-1161 and VT-1129 Exhibit Strong In Vitro Activity against Candida glabrata and C. krusei Isolates Clinically Resistant to Azole and Echinocandin Antifungal Compounds.

Schell WA, Jones AM, Garvey EP, Hoekstra WJ, Schotzinger RJ, Alexander BD.

Antimicrob Agents Chemother. 2017 Feb 23;61(3). pii: e01817-16. doi: 10.1128/AAC.01817-16. Print 2017 Mar.

18.

Activity of VT-1129 against Cryptococcus neoformans clinical isolates with high fluconazole MICs.

Nielsen K, Vedula P, Smith KD, Meya DB, Garvey EP, Hoekstra WJ, Schotzinger RJ, Boulware DR.

Med Mycol. 2017 Jun 1;55(4):453-456. doi: 10.1093/mmy/myw089.

PMID:
27664991
19.

The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme.

Warrilow AG, Parker JE, Price CL, Nes WD, Garvey EP, Hoekstra WJ, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4530-8. doi: 10.1128/AAC.00349-16. Print 2016 Aug.

20.

The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.

Lockhart SR, Fothergill AW, Iqbal N, Bolden CB, Grossman NT, Garvey EP, Brand SR, Hoekstra WJ, Schotzinger RJ, Ottinger E, Patterson TF, Wiederhold NP.

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2528-31. doi: 10.1128/AAC.02770-15. Print 2016 Apr.

21.

VT-1161 Protects Immunosuppressed Mice from Rhizopus arrhizus var. arrhizus Infection.

Gebremariam T, Wiederhold NP, Fothergill AW, Garvey EP, Hoekstra WJ, Schotzinger RJ, Patterson TF, Filler SG, Ibrahim AS.

Antimicrob Agents Chemother. 2015 Dec;59(12):7815-7. doi: 10.1128/AAC.01437-15. Epub 2015 Sep 14.

22.

Evaluation of VT-1161 for Treatment of Coccidioidomycosis in Murine Infection Models.

Shubitz LF, Trinh HT, Galgiani JN, Lewis ML, Fothergill AW, Wiederhold NP, Barker BM, Lewis ER, Doyle AL, Hoekstra WJ, Schotzinger RJ, Garvey EP.

Antimicrob Agents Chemother. 2015 Dec;59(12):7249-54. doi: 10.1128/AAC.00593-15. Epub 2015 Sep 14.

23.

Efficacy of the clinical agent VT-1161 against fluconazole-sensitive and -resistant Candida albicans in a murine model of vaginal candidiasis.

Garvey EP, Hoekstra WJ, Schotzinger RJ, Sobel JD, Lilly EA, Fidel PL Jr.

Antimicrob Agents Chemother. 2015 Sep;59(9):5567-73. doi: 10.1128/AAC.00185-15. Epub 2015 Jun 29.

24.

VT-1161 dosed once daily or once weekly exhibits potent efficacy in treatment of dermatophytosis in a guinea pig model.

Garvey EP, Hoekstra WJ, Moore WR, Schotzinger RJ, Long L, Ghannoum MA.

Antimicrob Agents Chemother. 2015 Apr;59(4):1992-7. doi: 10.1128/AAC.04902-14. Epub 2015 Jan 20.

25.

Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection.

Yoshinaga T, Kobayashi M, Seki T, Miki S, Wakasa-Morimoto C, Suyama-Kagitani A, Kawauchi-Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T.

Antimicrob Agents Chemother. 2015 Jan;59(1):397-406. doi: 10.1128/AAC.03909-14. Epub 2014 Nov 3.

26.

The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.

Warrilow AG, Hull CM, Parker JE, Garvey EP, Hoekstra WJ, Moore WR, Schotzinger RJ, Kelly DE, Kelly SL.

Antimicrob Agents Chemother. 2014 Dec;58(12):7121-7. doi: 10.1128/AAC.03707-14. Epub 2014 Sep 15.

27.

Design and optimization of highly-selective fungal CYP51 inhibitors.

Hoekstra WJ, Garvey EP, Moore WR, Rafferty SW, Yates CM, Schotzinger RJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3455-8. doi: 10.1016/j.bmcl.2014.05.068. Epub 2014 Jun 9.

PMID:
24948565
28.

Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.

Johns BA, Kawasuji T, Weatherhead JG, Boros EE, Thompson JB, Koble CS, Garvey EP, Foster SA, Jeffrey JL, Fujiwara T.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3104-7. doi: 10.1016/j.bmcl.2014.05.011. Epub 2014 May 16.

PMID:
24908608
29.

Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744).

Johns BA, Kawasuji T, Weatherhead JG, Taishi T, Temelkoff DP, Yoshida H, Akiyama T, Taoda Y, Murai H, Kiyama R, Fuji M, Tanimoto N, Jeffrey J, Foster SA, Yoshinaga T, Seki T, Kobayashi M, Sato A, Johnson MN, Garvey EP, Fujiwara T.

J Med Chem. 2013 Jul 25;56(14):5901-16. doi: 10.1021/jm400645w. Epub 2013 Jul 11.

PMID:
23845180
30.

Carbamoyl pyridone HIV-1 integrase inhibitors. 2. Bi- and tricyclic derivatives result in superior antiviral and pharmacokinetic profiles.

Kawasuji T, Johns BA, Yoshida H, Weatherhead JG, Akiyama T, Taishi T, Taoda Y, Mikamiyama-Iwata M, Murai H, Kiyama R, Fuji M, Tanimoto N, Yoshinaga T, Seki T, Kobayashi M, Sato A, Garvey EP, Fujiwara T.

J Med Chem. 2013 Feb 14;56(3):1124-35. doi: 10.1021/jm301550c. Epub 2013 Jan 22.

PMID:
23316884
31.

Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups.

Johns BA, Kawasuji T, Weatherhead JG, Boros EE, Thompson JB, Koble CS, Garvey EP, Foster SA, Jeffrey JL, Fujiwara T.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):422-5. doi: 10.1016/j.bmcl.2012.11.071. Epub 2012 Dec 3.

PMID:
23245515
32.

Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors.

Johns BA, Kawasuji T, Weatherhead JG, Boros EE, Thompson JB, Garvey EP, Foster SA, Jeffrey JL, Miller WH, Kurose N, Matsumura K, Fujiwara T.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6461-4. doi: 10.1016/j.bmcl.2011.08.082. Epub 2011 Sep 8.

PMID:
21945283
33.

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.

Kobayashi M, Yoshinaga T, Seki T, Wakasa-Morimoto C, Brown KW, Ferris R, Foster SA, Hazen RJ, Miki S, Suyama-Kagitani A, Kawauchi-Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T.

Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. doi: 10.1128/AAC.01209-10. Epub 2010 Nov 29.

34.

Pharmacovirological impact of an integrase inhibitor on human immunodeficiency virus type 1 cDNA species in vivo.

Goffinet C, Allespach I, Oberbremer L, Golden PL, Foster SA, Johns BA, Weatherhead JG, Novick SJ, Chiswell KE, Garvey EP, Keppler OT.

J Virol. 2009 Aug;83(15):7706-17. doi: 10.1128/JVI.00683-09. Epub 2009 May 20.

35.

Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors.

Boros EE, Edwards CE, Foster SA, Fuji M, Fujiwara T, Garvey EP, Golden PL, Hazen RJ, Jeffrey JL, Johns BA, Kawasuji T, Kiyama R, Koble CS, Kurose N, Miller WH, Mote AL, Murai H, Sato A, Thompson JB, Woodward MC, Yoshinaga T.

J Med Chem. 2009 May 14;52(9):2754-61. doi: 10.1021/jm801404b.

PMID:
19374386
36.

The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.

Johns BA, Weatherhead JG, Allen SH, Thompson JB, Garvey EP, Foster SA, Jeffrey JL, Miller WH.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1802-6. doi: 10.1016/j.bmcl.2009.01.090. Epub 2009 Jan 30.

PMID:
19217781
37.

1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position.

Johns BA, Weatherhead JG, Allen SH, Thompson JB, Garvey EP, Foster SA, Jeffrey JL, Miller WH.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1807-10. doi: 10.1016/j.bmcl.2009.01.089. Epub 2009 Jan 30.

PMID:
19217284
38.

Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant.

Garvey EP, Schwartz B, Gartland MJ, Lang S, Halsey W, Sathe G, Carter HL 3rd, Weaver KL.

Biochemistry. 2009 Feb 24;48(7):1644-53. doi: 10.1021/bi802141y.

PMID:
19178153
39.

Secondary mutations in viruses resistant to HIV-1 integrase inhibitors that restore viral infectivity and replication kinetics.

Nakahara K, Wakasa-Morimoto C, Kobayashi M, Miki S, Noshi T, Seki T, Kanamori-Koyama M, Kawauchi S, Suyama A, Fujishita T, Yoshinaga T, Garvey EP, Johns BA, Foster SA, Underwood MR, Sato A, Fujiwara T.

Antiviral Res. 2009 Feb;81(2):141-6. doi: 10.1016/j.antiviral.2008.10.007. Epub 2008 Nov 21.

PMID:
19027039
40.

The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.

Garvey EP, Johns BA, Gartland MJ, Foster SA, Miller WH, Ferris RG, Hazen RJ, Underwood MR, Boros EE, Thompson JB, Weatherhead JG, Koble CS, Allen SH, Schaller LT, Sherrill RG, Yoshinaga T, Kobayashi M, Wakasa-Morimoto C, Miki S, Nakahara K, Noshi T, Sato A, Fujiwara T.

Antimicrob Agents Chemother. 2008 Mar;52(3):901-8. Epub 2007 Dec 26. Erratum in: Antimicrob Agents Chemother. 2008 May;52(5):1899.

41.

Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones.

Boros EE, Johns BA, Garvey EP, Koble CS, Miller WH.

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5668-72.

PMID:
16908139
42.

Identification of peptides that inhibit the DNA binding, trans-activator, and DNA replication functions of the human papillomavirus type 11 E2 protein.

Deng SJ, Pearce KH, Dixon EP, Hartley KA, Stanley TB, Lobe DC, Garvey EP, Kost TA, Petty RL, Rocque WJ, Alexander KA, Underwood MR.

J Virol. 2004 Mar;78(5):2637-41.

43.

Unexploited viral and host targets for the treatment of human immunodeficiency virus type 1 infection.

Garvey EP.

Curr Drug Targets Infect Disord. 2001 Aug;1(2):107-23. Review.

PMID:
12455408
44.

Small molecule modulators of HIV Rev/Rev response element interaction identified by random screening.

Chapman RL, Stanley TB, Hazen R, Garvey EP.

Antiviral Res. 2002 Jun;54(3):149-62.

PMID:
12062388
45.

Purification of the constitutive nitric oxide synthase.

Garvey EP.

Methods Mol Biol. 1998;100:37-41. No abstract available.

PMID:
10906990
46.

Purification of the inducible nitric oxide synthase.

Garvey EP.

Methods Mol Biol. 1998;100:33-6. No abstract available.

PMID:
10906989
47.
48.

N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.

Collins JL, Shearer BG, Oplinger JA, Lee S, Garvey EP, Salter M, Duffy C, Burnette TC, Furfine ES.

J Med Chem. 1998 Jul 16;41(15):2858-71.

PMID:
9667974
49.

Nucleotide and nucleoside analogues as inhibitors of cytosolic 5'-nucleotidase I from heart.

Garvey EP, Lowen GT, Almond MR.

Biochemistry. 1998 Jun 23;37(25):9043-51.

PMID:
9636049
50.

Response of the septic vasculature to prolonged vasopressor therapy with N(omega)-monomethyl-L-arginine and epinephrine in canines.

Freeman BD, Zeni F, Banks SM, Eichacker PQ, Bacher JD, Garvey EP, Tuttle JV, Jurgensen CH, Natanson C, Danner RL.

Crit Care Med. 1998 May;26(5):877-86.

PMID:
9590318

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