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Publikationer i urvalet

26 träffar

Bibliografisk träff 2018-12-20

Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.

Nawrozkij MB, Forgione M, Yablokov AS, Lucidi A, Tomaselli D, Patsilinakos A, Panella C, Hailu GS, Kirillov IA, Badia R, Riveira-Muñoz E, Crespan E, Armijos Rivera JI, Cirilli R, Ragno R, Esté JA, Maga G, Mai A, Rotili D.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01238

Bibliografisk träff 2018-09-06

Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.

Gu SX, Lu HH, Liu GY, Ju XL, Zhu YY.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2018.09.013

Bibliografisk träff 2016-07-21

Computer-aided discovery of anti-HIV agents.

Jorgensen WL.

Bioorg Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2016.07.039

Bibliografisk träff 2016-03-08

Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.

Tintori C, Brai A, Dasso Lang MC, Deodato D, Greco AM, Bizzarri BM, Cascone L, Casian A, Zamperini C, Dreassi E, Crespan E, Maga G, Vanham G, Ceresola E, Canducci F, Ariën KK, Botta M.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01979

Bibliografisk träff 2016-02-08

2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.

Sergeyev S, Yadav AK, Franck P, Michiels J, Lewi P, Heeres J, Vanham G, Ariën KK, Vande Velde CM, De Winter H, Maes BU.

J Med Chem · research support, non-u.s. gov't; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/acs.jmedchem.5b01336

Bibliografisk träff 2014-08-14

From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.

Venkatraj M, Ariën KK, Heeres J, Joossens J, Dirié B, Lyssens S, Michiels J, Cos P, Lewi PJ, Vanham G, Maes L, Van der Veken P, Augustyns K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2014.08.005

Bibliografisk träff 2014-06-03

Synthesis of novel fluoro analogues of MKC442 as microbicides.

Loksha YM, Pedersen EB, Loddo R, Sanna G, Collu G, Giliberti G, La Colla P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm500139a

Bibliografisk träff 2013-10-15

Design, Synthesis, and Antiviral Evaluation of Chimeric Inhibitors of HIV Reverse Transcriptase.

Iyidogan P, Sullivan TJ, Chordia MD, Frey KM, Anderson KS.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml4002979

Bibliografisk träff 2013-07-08

Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.

Bollini M, Frey KM, Cisneros JA, Spasov KA, Das K, Bauman JD, Arnold E, Anderson KS, Jorgensen WL.

Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2013.06.093

Bibliografisk träff 2013-07-08

Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.

Bollini M, Cisneros JA, Spasov KA, Anderson KS, Jorgensen WL.

Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2013.06.091

Bibliografisk träff 2012-09-27

Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.

Venkatraj M, Ariën KK, Heeres J, Joossens J, Messagie J, Michiels J, Van der Veken P, Vanham G, Lewi PJ, Augustyns K.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2012.09.066

Bibliografisk träff 2012-03-26

2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.

Rotili D, Samuele A, Tarantino D, Ragno R, Musmuca I, Ballante F, Botta G, Morera L, Pierini M, Cirilli R, Nawrozkij MB, Gonzalez E, Clotet B, Artico M, Esté JA, Maga G, Mai A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm201308v

Bibliografisk träff 2011-09-01

Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).

Venkatraj M, Ariën KK, Heeres J, Dirié B, Joossens J, Van Goethem S, Van der Veken P, Michiels J, Vande Velde CM, Vanham G, Lewi PJ, Augustyns K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2011.08.060

Bibliografisk träff 2011-03-25

Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.

Rotili D, Tarantino D, Artico M, Nawrozkij MB, Gonzalez-Ortega E, Clotet B, Samuele A, Esté JA, Maga G, Mai A.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm101626c

Bibliografisk träff 2010-03-22

The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.

Xu HT, Quan Y, Schader SM, Oliveira M, Bar-Magen T, Wainberg MA.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article · DOI 10.1128/aac.01795-09

Bibliografisk träff 2009-08-24

Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.

Xu H, Quan Y, Brenner BG, Bar-Magen T, Oliveira M, Schader SM, Wainberg MA.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article · DOI 10.1128/aac.00800-09

Bibliografisk träff 2009-07-19

Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Tian X, Qin B, Lu H, Lai W, Jiang S, Lee KH, Chen CH, Xie L.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2009.07.080

Bibliografisk träff 2009-03-02

Reverse transcriptase inhibitors as potential colorectal microbicides.

Herrera C, Cranage M, McGowan I, Anton P, Shattock RJ.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.01096-08

Bibliografisk träff 2008-11-24

Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.

Fletcher P, Harman S, Azijn H, Armanasco N, Manlow P, Perumal D, de Bethune MP, Nuttall J, Romano J, Shattock R.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article · DOI 10.1128/aac.01156-08

Bibliografisk träff 2008-04-08

QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.

Liang YH, Chen FE.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2008.03.021

Bibliografisk träff 2007-05-03

SAR and QSAR studies: modelling of new DAPY derivatives.

Thakur A, Thakur M, Bharadwaj A, Thakur S.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2007.04.005

Bibliografisk träff 2005-03-01

From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.

De Corte BL.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/jm040127p

Bibliografisk träff 2005-03-01

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).

Janssen PA, Lewi PJ, Arnold E, Daeyaert F, de Jonge M, Heeres J, Koymans L, Vinkers M, Guillemont J, Pasquier E, Kukla M, Ludovici D, Andries K, de Béthune MP, Pauwels R, Das K, Clark AD, Frenkel YV, Hughes SH, Medaer B, De Knaep F, Bohets H, De Clerck F, Lampo A, Williams P, Stoffels P.

J Med Chem · review; journal article · DOI 10.1021/jm040840e

Bibliografisk träff 2005-03-01

Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.

Frenkel YV, Clark AD, Das K, Wang YH, Lewi PJ, Janssen PA, Arnold E.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm049439i

Bibliografisk träff 2004-05-01

Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants.

Das K, Clark AD, Lewi PJ, Heeres J, De Jonge MR, Koymans LM, Vinkers HM, Daeyaert F, Ludovici DW, Kukla MJ, De Corte B, Kavash RW, Ho CY, Ye H, Lichtenstein MA, Andries K, Pauwels R, De Béthune MP, Boyer PL, Clark P, Hughes SH, Janssen PA, Arnold E.

J Med Chem · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1021/jm030558s

Bibliografisk träff 2001-09-01

Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.

Ludovici DW, De Corte BL, Kukla MJ, Ye H, Ho CY, Lichtenstein MA, Kavash RW, Andries K, de Béthune MP, Azijn H, Pauwels R, Lewi PJ, Heeres J, Koymans LM, de Jonge MR, Van Aken KJ, Daeyaert FF, Das K, Arnold E, Janssen PA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(01)00412-7