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Development of dual-acting pyrimidinediones as novel and highly potent topical anti-HIV microbicides.

Watson Buckheit K, Yang L, Buckheit RW Jr.

Antimicrob Agents Chemother. 2011 Nov;55(11):5243-54. doi: 10.1128/AAC.05237-11. Epub 2011 Sep 6.


Comparative evaluation of virus transmission inhibition by dual-acting pyrimidinedione microbicides using the microbicide transmission and sterilization assay.

Watson KM, Buckheit CE, Buckheit RW Jr.

Antimicrob Agents Chemother. 2008 Aug;52(8):2787-96. doi: 10.1128/AAC.01657-07. Epub 2008 Jun 16.


Antiviral interactions of combinations of highly potent 2,4(1H,3H)-pyrimidinedione congeners and other anti-HIV agents.

Hartman TL, Yang L, Buckheit RW Jr.

Antiviral Res. 2011 Dec;92(3):505-8. doi: 10.1016/j.antiviral.2011.10.013. Epub 2011 Oct 19.


Clinical development of microbicides for the prevention of HIV infection.

D'Cruz OJ, Uckun FM.

Curr Pharm Des. 2004;10(3):315-36. Review.


Development of a comprehensive human immunodeficiency virus type 1 screening algorithm for discovery and preclinical testing of topical microbicides.

Lackman-Smith C, Osterling C, Luckenbaugh K, Mankowski M, Snyder B, Lewis G, Paull J, Profy A, Ptak RG, Buckheit RW Jr, Watson KM, Cummins JE Jr, Sanders-Beer BE.

Antimicrob Agents Chemother. 2008 May;52(5):1768-81. doi: 10.1128/AAC.01328-07. Epub 2008 Mar 3.


Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.

Buckheit RW Jr, Hartman TL, Watson KM, Chung SG, Cho EH.

Antimicrob Agents Chemother. 2008 Jan;52(1):225-36. Epub 2007 Oct 29.


In vitro activities of candidate microbicides against cell-associated HIV.

Selhorst P, Grupping K, Bourlet T, Delézay O, Ariën KK, Vanham G.

Antimicrob Agents Chemother. 2012 Feb;56(2):805-15. doi: 10.1128/AAC.05801-11. Epub 2011 Nov 14.


Inhibitory activity of 9-phenylcyclohepta[d]pyrimidinedione derivatives against different strains of HIV-1 as non-nucleoside reverse transcriptase inhibitors.

Huang Y, Wang X, Yu X, Yuan L, Guo Y, Xu W, Liu T, Liu J, Shao Y, Ma L.

Virol J. 2011 May 15;8:230. doi: 10.1186/1743-422X-8-230.


Inactivation of human immunodeficiency virus type 1 by nonoxynol-9, C31G, or an alkyl sulfate, sodium dodecyl sulfate.

Krebs FC, Miller SR, Malamud D, Howett MK, Wigdahl B.

Antiviral Res. 1999 Oct;43(3):157-73.


The structure-activity relationships of 2,4(1H,3H)-pyrimidinedione derivatives as potent HIV type 1 and type 2 inhibitors.

Buckheit RW Jr, Hartman TL, Watson KM, Kwon HS, Lee SH, Lee JW, Kang DW, Chung SG, Cho EH.

Antivir Chem Chemother. 2007;18(5):259-75.


SJ-3366, a unique and highly potent nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1) that also inhibits HIV-2.

Buckheit RW Jr, Watson K, Fliakas-Boltz V, Russell J, Loftus TL, Osterling MC, Turpin JA, Pallansch LA, White EL, Lee JW, Lee SH, Oh JW, Kwon HS, Chung SG, Cho EH.

Antimicrob Agents Chemother. 2001 Feb;45(2):393-400.


Inhibitory effect of PRO 2000, a candidate microbicide, on dendritic cell-mediated human immunodeficiency virus transfer.

Teleshova N, Chang T, Profy A, Klotman ME.

Antimicrob Agents Chemother. 2008 May;52(5):1751-8. doi: 10.1128/AAC.00707-07. Epub 2008 Mar 10.


Human immunodeficiency virus type 1 (HIV-1) integration: a potential target for microbicides to prevent cell-free or cell-associated HIV-1 infection.

Terrazas-Aranda K, Van Herrewege Y, Hazuda D, Lewi P, Costi R, Di Santo R, Cara A, Vanham G.

Antimicrob Agents Chemother. 2008 Jul;52(7):2544-54. doi: 10.1128/AAC.01627-07. Epub 2008 May 12.


Griffithsin, a potent HIV entry inhibitor, is an excellent candidate for anti-HIV microbicide.

Emau P, Tian B, O'keefe BR, Mori T, McMahon JB, Palmer KE, Jiang Y, Bekele G, Tsai CC.

J Med Primatol. 2007 Aug;36(4-5):244-53.


Syndecan-Fc hybrid molecule as a potent in vitro microbicidal anti-HIV-1 agent.

Bobardt MD, Chatterji U, Schaffer L, de Witte L, Gallay PA.

Antimicrob Agents Chemother. 2010 Jul;54(7):2753-66. doi: 10.1128/AAC.01606-09. Epub 2010 May 3.


Combinations of 3-hydroxyphthalic anhydride-modified ovalbumin with antiretroviral drug-based microbicide candidates display synergistic and complementary effects against HIV-1 infection.

Li L, Tan S, Lu H, Lu L, Yang J, Jin H, Liu S, Jiang S.

J Acquir Immune Defic Syndr. 2011 Apr 15;56(5):384-92. doi: 10.1097/QAI.0b013e31820a4a8d.


Vaginal microbicide gel for delivery of IQP-0528, a pyrimidinedione analog with a dual mechanism of action against HIV-1.

Mahalingam A, Simmons AP, Ugaonkar SR, Watson KM, Dezzutti CS, Rohan LC, Buckheit RW Jr, Kiser PF.

Antimicrob Agents Chemother. 2011 Apr;55(4):1650-60. doi: 10.1128/AAC.01368-10. Epub 2011 Jan 18.


Unique anti-human immunodeficiency virus activities of the nonnucleoside reverse transcriptase inhibitors calanolide A, costatolide, and dihydrocostatolide.

Buckheit RW Jr, White EL, Fliakas-Boltz V, Russell J, Stup TL, Kinjerski TL, Osterling MC, Weigand A, Bader JP.

Antimicrob Agents Chemother. 1999 Aug;43(8):1827-34.


Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages.

Khoury G, Ewart G, Luscombe C, Miller M, Wilkinson J.

Antimicrob Agents Chemother. 2010 Feb;54(2):835-45. doi: 10.1128/AAC.01308-09. Epub 2009 Dec 7.

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