etravirine and nevirapine
etravirine has been researched along with nevirapine in 144 studies
Compound Research Comparison
Studies (etravirine) | Trials (etravirine) | Recent Studies (post-2010) (etravirine) | Studies (nevirapine) | Trials (nevirapine) | Recent Studies (post-2010) (nevirapine) |
---|---|---|---|---|---|
572 | 90 | 321 | 3,212 | 509 | 1,108 |
Protein Interaction Comparison
Protein | Taxonomy | etravirine (IC50) | nevirapine (IC50) |
---|---|---|---|
Chain B, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | 0.08 | |
Chain A, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | 0.08 | |
Chain A, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | 0.08 | |
Chain A, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | 0.08 | |
Chain B, Hiv-1 Reverse Transcriptase | Human immunodeficiency virus 1 | 0.08 | |
Chain A, Reverse transcriptase/ribonuclease H | Human immunodeficiency virus 1 | 1.165 | |
Prothrombin | Bos taurus (cattle) | 1.15 | |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 BH10 | 1.4504 | |
Gag-Pol polyprotein | Human immunodeficiency virus type 2 (ISOLATE ROD) | 2.05 | |
Gag-Pol polyprotein | HIV-1 M:B_HXB2R | 1.4353 | |
Imidazoleglycerol-phosphate dehydratase | Saccharomyces cerevisiae S288C | 1.7 | |
Cytochrome P450 3A4 | Homo sapiens (human) | 0.181 | |
Cytochrome P450 2C9 | Homo sapiens (human) | 0.181 | |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | 0.69 | |
Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | 0.7 | |
Microsomal triglyceride transfer protein large subunit | Homo sapiens (human) | 5.75 | |
Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | 0.18 | |
Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | 2.071 | |
Protease | Human immunodeficiency virus 1 | 0.101 | |
Reverse transcriptase | Human immunodeficiency virus 1 | 3.995 |
Research
Studies (144)
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 14 (9.72) | 29.6817 |
2010's | 108 (75.00) | 24.3611 |
2020's | 22 (15.28) | 2.80 |
Authors
Authors | Studies |
---|---|
Andries, K; Arnold, E; Azijn, H; Daeyaert, FF; Das, K; de Béthune, MP; De Corte, BL; de Jonge, MR; Heeres, J; Ho, CY; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Van Aken, KJ; Ye, H | 1 |
Andries, K; Arnold, E; Boyer, PL; Clark, AD; Clark, P; Daeyaert, F; Das, K; De Béthune, MP; De Corte, B; De Jonge, MR; Heeres, J; Ho, CY; Hughes, SH; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Vinkers, HM; Ye, H | 1 |
De Corte, BL | 1 |
Anderson, KS; Basavapathruni, A; Hamilton, AD; Jorgensen, WL; Ruiz-Caro, J; Tirado-Rives, J | 1 |
Anderson, KS; Bailey, CM; Basavapathruni, A; Hamilton, AD; Jorgensen, WL; Kim, JT; Ruiz-Caro, J; Wang, L | 1 |
Anderson, KS; Bailey, CM; Domaoal, RA; Hamilton, AD; Jorgensen, WL; Kim, JT; Thakur, VV; Wang, L | 1 |
Anderson, KS; Bailey, CM; Barreiro, G; Domaoal, RA; Guimarães, CR; Jorgensen, WL; Kim, JT; Wang, L | 1 |
Alongi, M; Angeli, L; Armand-Ugon, M; Baltzinger, M; Bec, G; Bellucci, L; Botta, M; Casaluce, G; Dumas, P; Ennifar, E; Esté, JA; Giorgi, G; Gonzalez, E; Maga, G; Radi, M; Samuele, A; Tafi, A; Zanoli, S | 1 |
DiStefano, DJ; Hazuda, DJ; Lai, MT; McKenna, PM; Miller, MD; Munshi, V; Touch, S; Tucker, TJ; Tynebor, RM; Williams, TM | 1 |
Bar-Magen, T; Brenner, BG; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, H | 1 |
Azijn, H; Boven, K; de Béthune, MP; Jochmans, D; Kraus, G; Picchio, G; Rimsky, LT; Tirry, I; Van Craenenbroeck, E; Vingerhoets, J | 1 |
Akonde, A; Calvez, V; Cisse, M; Costagliola, D; Derache, A; Descamps, D; Diarra, B; Katlama, C; Koita, V; Maïga, AI; Malet, I; Marcelin, AG; Masquelier, B; Morand-Joubert, L; Tounkara, A; Verlinden, Y; Wirden, M | 1 |
Gatanaga, H; Hachiya, A; Hayashida, T; Ode, H; Oka, S; Sato, H | 1 |
Anderson, KS; Bollini, M; Domaoal, RA; Jorgensen, WL; Leung, CS; Spasov, KA; Thakur, VV; Zeevaart, JG | 1 |
Bar-Magen, T; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, HT | 1 |
Barbault, F; Chen, CH; Huang, L; Huang, R; Jiang, S; Jiang, X; Lee, KH; Lu, H; Qian, K; Qin, B; Tian, X; Xie, L | 1 |
Corbau, R; Fishburn, L; Irving, S; Knöchel, T; Martin, A; Mori, J; Mowbray, C; Panton, W; Perros, M; Phillips, C; Ringrose, H; Smith-Burchnell, C; Thornberry, A; Westby, M; Wood, A | 1 |
Haefeli, WE; Weiss, J; Zembruski, NC | 1 |
Balzarini, J; Chen, FE; De Clercq, E; Gu, SX; He, QQ; Ma, XD; Pannecouque, C; Yang, SQ | 1 |
Chen, W; Chen, X; De Clercq, E; Li, D; Li, X; Liu, X; Pannecouque, C; Tian, Y; Zhan, P | 1 |
Balzarini, J; Chen, FE; Clercq, ED; Dai, HF; Gu, SX; He, QQ; Ma, XD; Pannecouque, C; Yang, SQ | 1 |
Anderson, KS; Bollini, M; Domaoal, RA; Gallardo-Macias, R; Jorgensen, WL; Spasov, KA; Thakur, VV | 1 |
Balzarini, J; Chen, X; De Clercq, E; Liu, X; Pannecouque, C; Zhan, P | 1 |
Balzarini, J; Chen, FE; De Clercq, E; Gu, SX; He, QQ; Li, ZM; Ma, XD; Pannecouque, C; Yang, SQ | 1 |
Chen, X; Cheng, Z; De Clercq, E; Liu, X; Meng, C; Pannecouque, C; Shao, S; Zhan, P | 1 |
Brancale, A; Clotet, B; Coluccia, A; Cosconati, S; Esté, JA; Famiglini, V; Gonzalez, E; La Regina, G; Maga, G; Novellino, E; Piscitelli, F; Samuele, A; Schols, D; Silvestri, R | 1 |
Briñón, MC; Daelemans, D; Dehaen, W; Leen, V; Madrid, M; Pannecouque, C; Ribone, SR | 1 |
Anderson, KS; Bollini, M; Gallardo-Macias, R; Jorgensen, WL; Spasov, KA; Tirado-Rives, J | 1 |
Balzarini, J; De Clercq, E; Li, D; Liu, H; Liu, X; Pannecouque, C; Zhan, P | 1 |
Chen, FE; Daelemans, D; De Clercq, E; Liu, Y; Ma, XD; Pannecouque, C; Yang, S | 1 |
Anderson, KS; Bollini, M; Cisneros, JA; Jorgensen, WL; Spasov, KA | 1 |
Balzarini, J; Chen, FE; Chen, WX; Daelemans, D; De Clercq, E; He, QQ; Pannecouque, C; Wu, HQ; Yan, ZH | 1 |
Balzarini, J; Chen, X; De Clercq, E; Li, Z; Liu, H; Liu, X; Pannecouque, C; Xie, Z; Zhan, P; Zhang, L; Zhao, T | 1 |
Balzarini, J; Chen, W; De Clercq, E; Liu, H; Liu, X; Pannecouque, C; Rai, D; Zhan, P; Zhou, Z | 1 |
De Clercq, E; Li, Z; Liu, H; Liu, X; Pannecouque, C; Wang, J; Zhan, P | 1 |
De Clercq, E; Du, D; Liu, H; Liu, X; Pannecouque, C; Rai, D; Tian, Y; Wang, L; Zhan, P | 1 |
Chen, FE; Chen, WX; De Clercq, E; He, QQ; Huang, XY; Pannecouque, C; Wu, HQ; Yan, ZH | 1 |
Badia, R; Brancale, A; Cirilli, R; Clotet, B; Coluccia, A; Crespan, E; Esté, JA; Famiglini, V; La Regina, G; Maga, G; Novellino, E; Pelliccia, S; Silvestri, R | 1 |
Chen, FE; Chen, WX; De Clercq, E; He, QQ; Pannecouque, C; Piao, HR; Wu, HQ; Wu, Y; Yan, ZH | 1 |
Collu, G; Giliberti, G; La Colla, P; Loddo, R; Loksha, YM; Pedersen, EB; Sanna, G | 1 |
Ariën, KK; Augustyns, K; Cos, P; Dirié, B; Heeres, J; Joossens, J; Lewi, PJ; Lyssens, S; Maes, L; Michiels, J; Van der Veken, P; Vanham, G; Venkatraj, M | 1 |
Chen, W; De Clercq, E; Liu, X; Liu, Z; Pannecouque, C; Zhan, P | 1 |
Anderson, KS; Bollini, M; Frey, KM; Gallardo-Macias, R; Jorgensen, WL; Lee, WG; Spasov, KA | 1 |
Agostino, B; Badia, R; Botta, M; Brancale, A; Cirilli, R; Coluccia, A; Crespan, E; Esté, JA; Famiglini, V; Ferretti, R; La Regina, G; Limongelli, V; Maga, G; Novellino, E; Pelliccia, S; Riveira-Muñoz, E; Schols, D; Silvestri, R; Zamperini, C | 1 |
De Clercq, E; Guo, J; Liu, H; Liu, X; Pannecouque, C; Zhang, L | 1 |
Chen, FE; Chen, WX; Daelemans, D; De Clercq, E; He, QQ; Pannecouque, C; Wu, HQ; Yao, J | 1 |
Balzarini, J; Chen, W; De Clercq, E; Fu, L; Huang, B; Li, C; Liu, H; Liu, T; Liu, X; Pannecouque, C; Sun, Y; Yu, M; Zhan, P | 1 |
Chen, W; De Clercq, E; Fu, L; Huang, B; Li, C; Li, X; Liang, X; Liu, H; Liu, T; Liu, X; Pannecouque, C; Sun, Y; Zhan, P | 1 |
Chen, FE; Chen, WX; Daelemans, D; De Clercq, E; He, QQ; Mao, TQ; Pannecouque, C; Tang, GF; Wan, ZY | 1 |
Chen, FE; Daelemans, D; De Clercq, E; Lu, YP; Mao, TQ; Pannecouque, C; Tao, Y; Wan, ZY; Wang, HF; Wang, XL; Wu, Y; Yao, J; Yin, H | 1 |
Chen, FE; Daelemans, D; De Clercq, E; Mao, TQ; Pannecouque, C; Piao, HR; Tao, Y; Wan, ZY; Wang, YF; Yin, H | 1 |
Chen, FE; Chen, WX; Daelemans, D; De Clercq, E; Mao, TQ; Pannecouque, C; Wan, ZY; Wang, HF; Wang, XL; Yao, J; Yin, H | 1 |
Balzarini, J; De Clercq, E; Gu, SX; Ju, XL; Liu, H; Pannecouque, C; Qiao, H; Shu, QC; Zhu, YY | 1 |
Chen, W; Daelemans, D; De Clercq, E; Huang, B; Kang, D; Li, X; Liu, X; Liu, Z; Lu, X; Pannecouque, C; Yang, J; Zhan, P | 1 |
Daelemans, D; De Clercq, E; Gao, P; Huang, B; Li, X; Liu, X; Pannecouque, C; Zhan, P; Zhou, Z | 1 |
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
Chen, X; Daelemans, D; De Clercq, E; Huang, B; Kang, D; Li, W; Liu, X; Meng, Q; Pannecouque, C; Zhan, P | 1 |
Chizhov, AO; Geisman, AN; Khandazhinskaya, AL; Kochetkov, SN; Naesens, L; Novikov, MS; Ozerov, AA; Pannecouque, C; Seley-Radtke, KL; Valuev-Elliston, VT | 1 |
Buckheit, RW; Cushman, M; Hartman, TL; Hoshi, A; Okazaki, M; Pannecouque, C; Sakamoto, T; Takayama, J; Xuan, M | 1 |
Chen, W; Daelemans, D; De Clercq, E; Huang, B; Liu, X; Pannecouque, C; Yang, J; Zhan, P | 1 |
Elgaher, WA; Hartmann, RW; Haupenthal, J; Mély, Y; Pires, M; Real, E; Saladini, F; Sharma, KK | 1 |
Jorgensen, WL | 1 |
Daelemans, D; De Clercq, E; Huang, B; Kang, D; Li, X; Liu, X; Lu, X; Pannecouque, C; Yang, J; Zhan, P; Zhao, F; Zhou, Z | 1 |
Daelemans, D; De Clercq, E; Ding, X; Fang, Z; Huang, B; Kang, D; Li, Z; Liu, X; Lu, X; Pannecouque, C; Xu, H; Zhan, P; Zhang, H; Zhou, Z | 1 |
De Clercq, E; Huo, Z; Kang, D; Liu, H; Liu, X; Pannecouque, C; Tian, Y; Zhan, P; Zhang, H; Zhou, Z | 1 |
Gu, SX; Ju, XL; Li, TT; Lu, HH; Pannecouque, C; Xiao, T; Xue, P; Zhang, X; Zheng, XJ; Zhu, YY | 1 |
Gu, SX; Ju, XL; Liu, GY; Lu, HH; Pannecouque, C; Xue, P; Zhang, XL; Zheng, XJ; Zhu, YY | 1 |
Daelemans, D; De Clercq, E; Ding, X; Fang, Z; Huang, B; Huo, Z; Kang, D; Liu, X; Lu, X; Meng, Q; Pannecouque, C; Tian, Y; Wu, G; Xu, H; Yu, Z; Zhan, P; Zhang, H; Zhou, Z | 1 |
Badia, R; Brambilla, A; Brancale, A; Catalano, M; Cirilli, R; Coluccia, A; Crespan, E; Esté, JA; Famiglini, V; Formica, FR; La Regina, G; Limatola, C; Maga, G; Masci, D; Novellino, E; Riveira-Muñoz, E; Silvestri, R | 1 |
Chen, Z; Daelemans, D; De Clercq, E; Huang, B; Li, W; Liu, H; Liu, X; Pannecouque, C; Sun, S; Wang, X; Zhan, P | 1 |
Daelemans, D; De Clercq, E; Huang, B; Kang, D; Liu, J; Liu, X; Liu, Z; Pannecouque, C; Tian, Y; Zhan, P | 1 |
Daelemans, D; De Clercq, E; Ding, X; Feng, D; Huo, Z; Kang, D; Liu, X; Pannecouque, C; Tian, Y; Wang, Z; Wu, G; Zhan, P; Zhao, T; Zhou, Z | 1 |
Chen, F; De Clercq, E; Jin, K; Meng, G; Pannecouque, C; Yin, H | 1 |
Daelemans, D; De Clercq, E; Huang, B; Kang, D; Liu, X; Pannecouque, C; Tian, Y; Zhan, P; Zhou, Z | 1 |
Daelemans, D; De Clercq, E; Gao, P; Kang, D; Liu, X; Lu, X; Pannecouque, C; Yang, J; Zhan, P | 1 |
Chen, CH; Daelemans, D; De Clercq, E; Huang, B; Kang, D; Lee, KH; Liu, J; Liu, X; Liu, Z; Pannecouque, C; Tian, Y; Zhan, P; Zhang, H | 1 |
Daelemans, D; De Clercq, E; Desta, S; Ding, X; Huo, Z; Jing, L; Kang, D; Liu, X; Pannecouque, C; Wang, Z; Wu, G; Zhan, P; Zhang, H; Zhou, Z; Zuo, X | 1 |
Clercq, E; Daelemans, D; Ding, X; Feng, D; Guma, S; Huang, B; Huo, Z; Jing, L; Kang, D; Liu, X; Luo, W; Pannecouque, C; Wang, Z; Wu, G; Zhan, P; Zhang, H; Zhang, J; Zhao, T; Zhou, Z; Zuo, X | 1 |
De Clercq, E; Jin, K; Meng, G; Pannecouque, C; Sang, Y | 1 |
Byrareddy, SN; Kongsted, J; Kramer, VG; Kurup, S; Liu, X; Namasivayam, V; Vanangamudi, M; Zhan, P | 1 |
Armijos Rivera, JI; Badia, R; Cirilli, R; Crespan, E; Esté, JA; Forgione, M; Hailu, GS; Kirillov, IA; Lucidi, A; Maga, G; Mai, A; Nawrozkij, MB; Panella, C; Patsilinakos, A; Ragno, R; Riveira-Muñoz, E; Rotili, D; Tomaselli, D; Yablokov, AS | 1 |
Daelemans, D; De Clercq, E; Kang, D; Liu, X; Pannecouque, C; Tian, Y; Wang, Z; Yu, Z; Zhan, P; Zhang, J | 1 |
Chen, F; De Clercq, E; Han, S; Jin, K; Meng, G; Pannecouque, C; Sang, Y | 1 |
Anderson, KS; Frey, KM; Gannam, ZTK; Jorgensen, WL; Kudalkar, SN; Lee, WG; Sasaki, T; Spasov, KA | 1 |
Chen, F; De Clercq, E; Han, S; Pannecouque, C; Sang, Y; Zhuang, C | 2 |
Chen, FE; De Clercq, E; Han, S; Pannecouque, C; Sang, Y; Tao, Y; Wu, Y; Zhuang, C | 1 |
Chen, FE; Gu, SX; Liu, GY; Meng, G; Pannecouque, C; Tang, JF; Wu, FS; Xiao, T; Xu, ZQ; Zhu, YY | 1 |
Arnold, E; De Clercq, E; Fang, Z; Feng, D; Kang, D; Liu, X; Pannecouque, C; Pilch, A; Ruiz, FX; Sun, Y; Wang, Z; Wei, F; Zhan, P; Zhao, T | 1 |
De Clercq, E; Feng, D; Jiang, X; Jing, L; Kang, D; Liu, X; Pannecouque, C; Sun, Y; Wei, F; Wu, G; Zhan, P | 1 |
Chen, FE; Chen, X; De Clercq, E; Ding, L; Pannecouque, C; Tao, Y; Zhuang, C | 1 |
Armijos Rivera, JI; Badia, R; Brambilla, A; Catalano, M; Cinquina, E; Coluccia, A; Crespan, E; Esté, JA; Falasca, F; La Regina, G; Limatola, C; Maga, G; Masci, D; Nalli, M; Riveira-Muñoz, E; Silvestri, R; Turriziani, O | 1 |
Cherukupalli, S; De Clercq, E; Feng, D; Fu, Z; Jiang, X; Kang, D; Liu, X; Pannecouque, C; Wang, Z; Zhan, P | 1 |
De Clercq, E; Huang, B; Jiang, X; Kang, D; Li, J; Liu, X; Olotu, FA; Pannecouque, C; Soliman, MES; Wang, Z; Zhan, P | 1 |
Chen, CH; De Clercq, E; Feng, D; Jing, L; Kang, D; Lee, KH; Lin, H; Liu, X; Olotu, FA; Pannecouque, C; Soliman, M; Zhan, P; Zuo, X | 1 |
Arnold, E; De Clercq, E; Feng, D; Gao, S; Jing, L; Kang, D; Liu, X; Pannecouque, C; Ruiz, FX; Sun, L; Sun, Y; Wang, Z; Zhan, P; Zhang, T | 1 |
Chen, FE; De Clercq, E; Ding, L; Pannecouque, C; Zhuang, C | 3 |
De Clercq, E; Gao, P; Liu, X; Pannecouque, C; Song, S; Sun, L; Wang, Z; Zhan, P; Zhang, J | 1 |
Cherukupalli, S; De Clercq, E; Fu, Z; Gao, S; Kang, D; Liu, X; Pannecouque, C; Sun, L; Zhan, P; Zhang, T; Zhou, Z | 1 |
Chen, FE; De Clercq, E; Jin, X; Pannecouque, C; Piao, HR; Zhuang, C | 1 |
Cherukupalli, S; De Clercq, E; Jia, R; Jiang, X; Kang, D; Liu, X; Pannecouque, C; Wang, W; Wang, Z; Xie, M; Zhan, P | 1 |
Cheng, Y; De Clercq, E; Gao, P; Gao, S; Kang, D; Liu, X; Pannecouque, C; Song, L; Song, S; Sun, L; Xu, S; Zhan, P; Zhao, F | 1 |
Chen, FE; De Clercq, E; Huang, WJ; Jin, X; Pannecouque, C; Wang, S; Zhang, YX; Zhao, LM | 1 |
Chen, FE; Clercq, E; Hao, QQ; Ling, X; Pannecouque, C | 1 |
Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M | 1 |
Danner, SA; Gruzdev, B; Jurriaans, S; Lange, JM; Peeters, M; Prins, JM; Rakhmanova, A; Sankatsing, SU; van't Klooster, G; Weverling, GJ | 1 |
Balzarini, J; Gago, F; Rodríguez-Barrios, F | 1 |
Clotet, B; Llibre, JM; Moltó, J; Paredes, R; Puig, T; Ruiz, L; Santos, JR | 1 |
Calabresi, A; Carosi, G; Castelnuovo, F; Ceresoli, F; Costarelli, S; Gargiulo, F; Lapadula, G; Manca, N; Paraninfo, G; Quiros-Roldan, E; Torti, C | 1 |
Anta, L; Blanco, JL; de Mendoza, C; García, F; Gutiérrez, F; Leal, M; Pérez-Elías, MJ; Poveda, E; Ribera, E; Soriano, V | 1 |
Adewole, I; Akanmu, S; Chaplin, B; Gashau, W; Idoko, J; Kanki, P; Meloni, S; Murphy, R; Penugonda, S; Taiwo, B | 1 |
Chantratita, W; Kiertiburanakul, S; Sukasem, C; Sungkanuparph, S; Wiboonchutikul, S | 1 |
de Souza, DF; Diaz, RS; Inocencio, LA; Janini, LM; Munerato, P; Oliveros, MP; Pereira, AA; Sucupira, MC | 1 |
Holmes, SP; Reuman, EC; Rhee, SY; Shafer, RW | 1 |
Butler, DM; Chantratita, W; Manosuthi, W; Richman, DD; Smith, DM; Sukasem, C | 1 |
Decha, P; Hannongbua, S; Intharathep, P; Parasuk, V; Sompornpisut, P; Udommaneethanakit, T; Wolschann, P | 1 |
Bar-Magen, T; Oliveira, M; Quan, Y; Wainberg, MA; Xu, HT | 1 |
Chirara, M; Crombe, A; Goodall, RL; Gupta, RK; Kaleebu, P; Kityo, C; McCormick, AL; Parry, CM; Pillay, D; Towers, GJ | 1 |
Balzarini, J; Brancale, A; Coluccia, A; Gatti, V; La Regina, G; Maga, G; Novellino, E; Pannecouque, C; Piscitelli, F; Samuele, A; Schols, D; Silvestri, R | 1 |
Bambara, RA; Demeter, LM; Dykes, C; Li, D; Liang, H; Lowe, NR; Smith, HM; Wang, J; Wu, H; Zhang, G | 1 |
Claassen, M; Preiser, W; van der Merwe, L; van Zyl, GU; Zeier, M | 1 |
Aleixo, AW; Arruda, MB; de M Brindeiro, R; Greco, DB; Martins, AN; Pires, AF; Tanuri, A | 1 |
Alcaro, S; Alteri, C; Artese, A; Bertoli, A; Calvez, V; Ceccherini-Silberstein, F; Costa, G; Descamps, D; Flandre, P; Forbici, F; Marcelin, AG; Masquelier, B; Ortuso, F; Parrotta, L; Perno, CF; Santoro, MM; Sing, T; Svicher, V | 1 |
Ananworanich, J; Bhakeecheep, S; Bowonwattanuwong, C; Bunupuradah, T; Chetchotisakd, P; Hirschel, B; Jirajariyavej, S; Kantipong, P; Klinbuayaem, V; Munsakul, W; Petoumenos, K; Prasithsirikul, W; Ruxrungtham, K; Sirivichayakul, S; Sungkanuparph, S | 1 |
Giaquinto, C; Penazzato, M | 1 |
Bettinger, D; Bouvier-Alias, M; Calvez, V; Cottalorda, J; Delaugerre, C; Descamps, D; Flandre, P; Henquell, C; Izopet, J; Marcelin, AG; Masquelier, B; Morand-Joubert, L; Rogez, S; Ruffault, A; Signori-Schmuck, A; Tamalet, C; Trabaud, MA; Vallet, S | 1 |
Eleftheriou, P; Geronikaki, A; Mehta, VP; Pitta, E; Surmava, S; Van der Eycken, EV | 1 |
Anquetil, D; Deshpande, A; Fleury, HJ; Le Bihan, L; Pinson, PR; Zongo, D | 1 |
Balamane, M; Fessel, WJ; Katzenstein, DA; Melikian, GL; Shafer, RW; Varghese, V | 1 |
Albanese, A; Asmuth, DM; Hayes, T; Knight, TH; Ma, ZM; Mann, S; Melcher, GP; Miller, CJ; Pollard, RB; Troia-Cancio, P; Yotter, T | 1 |
Allavena, C; Bouquié, R; Dailly, E; Deslandes, G; Jolliet, P; Raffi, F | 1 |
Colby-Germinario, SP; Han, Y; Huang, W; Oliveira, M; Petropoulos, CJ; Quan, Y; Wainberg, MA; Xu, HT | 1 |
Cahn, P; Chokephaibulkit, K; Dincq, S; Fourie, J; Kakuda, TN; Karatzios, C; Nijs, S; Opsomer, M; Tambuyzer, L; Tomaka, FL; Tudor-Williams, G | 1 |
Crawford, KW | 1 |
Aboulker, JP; Charreau, I; de Castro, N; Delaugerre, C; Gallien, S; Mahjoub, N; Molina, JM; Nere, ML; Simon, F | 1 |
Hannongbua, S; Ishii, K; Kato, K; Thammaporn, R; Uchiyama, S; Yagi-Utsumi, M | 1 |
Avihingsanon, A; Mekprasan, S; Ohata, PJ; Putcharoen, O; Ruxrungtham, K; Sirivichayakul, S; Teeranaipong, P | 1 |
Diphoko, T; Essex, M; Gaseitsiwe, S; Kasvosve, I; Makhema, J; Marlink, R; Moyo, S; Musonda, R; Novitsky, V; Okatch, H; Wainberg, M | 1 |
Abraham, OC; Demosthenes, JP; Ghale, BC; Kannangai, R; Ramalingam, VV; Rupali, P; Varghese, GM | 1 |
Chen, M; Daelemans, D; De Clercq, E; Feng, D; Jiang, X; Jing, L; Kang, D; Liu, X; Pannecouque, C; Wang, Z; Wu, G; Zhan, P; Zhou, Z; Zuo, X | 1 |
Andreoni, M; Antinori, A; Bagnarelli, P; Borghi, V; Bruzzone, B; Callegaro, AP; De Gennaro, M; Gianotti, N; Maffongelli, G; Maggiolo, F; Saladini, F; Sterrantino, G; Vergori, A; Zaccarelli, M; Zazzi, M | 1 |
Bonora, S; Calcagno, A; De Benedetto, I; Guastamacchia, G; Trunfio, M | 1 |
Reviews
5 review(s) available for etravirine and nevirapine
Article | Year |
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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.
Topics: Anti-HIV Agents; Benzodiazepines; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; Imidazoles; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2005 |
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Topics: Acetamides; Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Prodrugs; Pyridones; Reverse Transcriptase Inhibitors; Triazoles | 2019 |
Role of non-nucleoside reverse transcriptase inhibitors in treating HIV-infected children.
Topics: Adolescent; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Child; Child, Preschool; Cyclopropanes; HIV Infections; Humans; Infant; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2011 |
A review of the potential mechanisms of neuronal toxicity associated with antiretroviral drugs.
Topics: Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Astrocytes; Atazanavir Sulfate; Benzoxazines; Central Nervous System; Cognitive Dysfunction; Cyclopropanes; Dideoxynucleosides; Endothelial Cells; HIV Infections; Humans; Neurons; Nevirapine; Nitriles; Oligodendroglia; Pyrimidines | 2020 |
Trials
6 trial(s) available for etravirine and nevirapine
Article | Year |
---|---|
TMC125 exerts similar initial antiviral potency as a five-drug, triple class antiretroviral regimen.
Topics: Adult; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; CD4 Lymphocyte Count; Dideoxynucleosides; Double-Blind Method; Drug Therapy, Combination; Female; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Indinavir; Lamivudine; Male; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; RNA, Viral; Treatment Outcome; Zidovudine | 2003 |
Etravirine and rilpivirine resistance in HIV-1 subtype CRF01_AE-infected adults failing non-nucleoside reverse transcriptase inhibitor-based regimens.
Topics: Adult; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV-1; Humans; Lamivudine; Male; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; RNA, Viral; Stavudine | 2011 |
Gastrointestinal-associated lymphoid tissue immune reconstitution in a randomized clinical trial of raltegravir versus non-nucleoside reverse transcriptase inhibitor-based regimens.
Topics: Acquired Immunodeficiency Syndrome; Anti-HIV Agents; CD4 Lymphocyte Count; CD4-Positive T-Lymphocytes; CD8-Positive T-Lymphocytes; Drug Therapy, Combination; Endoscopy; Female; Gastrointestinal Tract; Humans; Immune Reconstitution Inflammatory Syndrome; Immunohistochemistry; Lymphocyte Activation; Lymphoid Tissue; Male; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Pyrrolidinones; Raltegravir Potassium; Reverse Transcriptase Inhibitors; RNA, Viral; Viral Load | 2012 |
Effect of efavirenz, nevirapine, etravirine, and raltegravir administration on the pharmacokinetics of ritonavir-boosted darunavir in a population of HIV-infected patients.
Topics: Adult; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Cyclopropanes; Darunavir; Drug Synergism; Female; HIV Infections; HIV Protease Inhibitors; Humans; Male; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Pyrrolidinones; Raltegravir Potassium; Ritonavir; Sulfonamides | 2013 |
Etravirine in treatment-experienced, HIV-1-infected children and adolescents: 48-week safety, efficacy and resistance analysis of the phase II PIANO study.
Topics: Adolescent; Area Under Curve; Child; Drug Eruptions; Drug Resistance, Viral; Female; HIV Infections; Humans; Male; Medication Adherence; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Treatment Outcome; Viral Load | 2014 |
Archived HIV-1 DNA resistance mutations to rilpivirine and etravirine in successfully treated HIV-1-infected individuals pre-exposed to efavirenz or nevirapine.
Topics: Adult; Aged; Alkynes; Antiretroviral Therapy, Highly Active; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV-1; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Retreatment; Reverse Transcriptase Inhibitors; Rilpivirine; Young Adult | 2015 |
Other Studies
133 other study(ies) available for etravirine and nevirapine
Article | Year |
---|---|
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
Topics: Anti-HIV Agents; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Inhibitory Concentration 50; Mutation; Nitriles; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2001 |
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 varian
Topics: Anti-HIV Agents; Crystallography, X-Ray; Drug Resistance, Viral; HIV Reverse Transcriptase; Models, Molecular; Mutation; Nitriles; Protein Conformation; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2004 |
Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Topics: Computer-Aided Design; Drug Resistance, Multiple, Viral; HIV Infections; HIV Reverse Transcriptase; Models, Molecular; Molecular Structure; Monte Carlo Method; Mutation; Reverse Transcriptase Inhibitors | 2006 |
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Topics: Amines; Drug Resistance, Multiple, Viral; Heterocyclic Compounds; HIV Infections; HIV Reverse Transcriptase; Hydrophobic and Hydrophilic Interactions; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiazoles | 2006 |
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Topics: Amines; HIV Reverse Transcriptase; HIV-1; Pyrimidines; Triazines | 2006 |
From docking false-positive to active anti-HIV agent.
Topics: Anti-HIV Agents; Cell Line; Databases, Factual; HIV Reverse Transcriptase; HIV-1; Humans; Ligands; Models, Molecular; Molecular Conformation; Oxadiazoles; Quantitative Structure-Activity Relationship; Reverse Transcriptase Inhibitors; Thermodynamics | 2007 |
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
Topics: Cell Line, Tumor; Computer Simulation; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; Humans; Kinetics; Models, Molecular; Mutation; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Pyrimidinones; Reverse Transcriptase Inhibitors; Stereoisomerism; Sulfides; Surface Plasmon Resonance | 2009 |
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cell Line; Cyclopropanes; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Nevirapine; Nitriles; Pyrazoles; Pyridazines; Pyridines; Pyrimidines; Reverse Transcriptase Inhibitors | 2009 |
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Reverse Transcriptase; Microbial Sensitivity Tests; Mutation; Nitriles; Pyridazines; Pyrimidines; Recombinant Proteins; Reverse Transcriptase Inhibitors | 2009 |
TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cell Line; Cells, Cultured; Cyclopropanes; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Molecular Structure; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine | 2010 |
Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
Topics: Anti-HIV Agents; Drug Resistance, Viral; Genotype; HIV Infections; HIV-1; Humans; Mutation; Nitriles; Phylogeny; Pyridazines; Pyrimidines | 2010 |
Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
Topics: Alkynes; Amino Acid Substitution; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Genes, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; In Vitro Techniques; Models, Molecular; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Recombination, Genetic; Virus Replication | 2010 |
Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
Topics: Azoles; HIV-1; Models, Molecular; Reverse Transcriptase Inhibitors | 2010 |
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
Topics: Anti-HIV Agents; Base Sequence; Cell Line; DNA, Viral; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Recombinant Proteins; Reverse Transcriptase Inhibitors; Virus Replication | 2010 |
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Aniline Compounds; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Hydrogen Bonding; Magnetic Resonance Spectroscopy; Models, Molecular; Reverse Transcriptase Inhibitors; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship | 2010 |
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
Topics: Cell Line; Cell Line, Tumor; Crystallography, X-Ray; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Sequence Data; Mutagenesis, Site-Directed; Nitriles; Pyrazoles; Reverse Transcriptase Inhibitors | 2010 |
Interaction potential of etravirine with drug transporters assessed in vitro.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Blotting, Western; Cell Line; Cell Line, Tumor; Cell Proliferation; Dogs; Humans; Neoplasm Proteins; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2011 |
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
Topics: Aniline Compounds; Cell Line; Chlorine; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2011 |
Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
Topics: Acetamides; Anti-HIV Agents; Cell Line; HIV Infections; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazoles; Virus Replication | 2011 |
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
Topics: Anti-HIV Agents; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2011 |
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
Topics: Anti-HIV Agents; Catechols; Computer Simulation; Ethers; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Structure; Protein Binding; Quantitative Structure-Activity Relationship; Reverse Transcriptase Inhibitors; Stereoisomerism; T-Lymphocytes | 2011 |
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Cell Line; Chemistry Techniques, Synthetic; HIV Reverse Transcriptase; HIV-1; Inhibitory Concentration 50; Piperidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazines | 2012 |
Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
Topics: HIV Reverse Transcriptase; HIV-1; HIV-2; Models, Molecular; Protein Conformation; Pyrimidines; Reverse Transcriptase Inhibitors; Stereoisomerism | 2012 |
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
Topics: Amines; Anti-HIV Agents; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Piperidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazines | 2012 |
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Cell Line; HIV Reverse Transcriptase; HIV-1; Indoles; Mutation; Nitrogen; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones | 2012 |
Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Antineoplastic Agents; Benzene Derivatives; Cell Survival; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Models, Molecular; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Tumor Cells, Cultured | 2012 |
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
Topics: Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
Topics: Cell Line; Delavirdine; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Nevirapine; Pyridazines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Benzophenones; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
Topics: Anti-HIV Agents; Cell Line, Transformed; Cell Proliferation; Dose-Response Relationship, Drug; HIV-1; Humans; Hydrazines; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Solubility; Structure-Activity Relationship | 2013 |
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
Topics: Binding Sites; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Pyrimidines; Pyrimidinones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2013 |
Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
Topics: Aniline Compounds; Anti-HIV Agents; Drug Design; HIV-1; Humans; Models, Molecular; Piperidines; Structure-Activity Relationship | 2014 |
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
Topics: Anti-HIV Agents; Crystallization; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyridones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2014 |
Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
Topics: Cell Line; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Magnetic Resonance Spectroscopy; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Pyridines; Reverse Transcriptase Inhibitors; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship; Virus Replication | 2014 |
Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Design; Heterocyclic Compounds; HIV; HIV Reverse Transcriptase; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Nitrogen; Pyrazoles; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2014 |
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Binding Sites; Cell Line; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Protein Structure, Tertiary; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2014 |
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Cell Line; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Indoles; Inhibitory Concentration 50; Models, Molecular; Protein Conformation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones | 2014 |
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Benzamides; Cell Survival; Cells, Cultured; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Docking Simulation; Molecular Structure; Nitriles; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Tumor Cells, Cultured; Virus Replication | 2014 |
Synthesis of novel fluoro analogues of MKC442 as microbicides.
Topics: Anti-HIV Agents; Cell Line; Drug Resistance, Viral; HIV Protease Inhibitors; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Pyrimidinones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Uracil | 2014 |
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
Topics: Anti-HIV Agents; Cell Line; Cell Survival; Dose-Response Relationship, Drug; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Parasitic Sensitivity Tests; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosoma brucei rhodesiense | 2014 |
Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
Topics: Anti-HIV Agents; Catalytic Domain; Dose-Response Relationship, Drug; Drug Design; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Structure; Niacinamide; Protein Conformation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Tumor Cells, Cultured | 2014 |
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
Topics: | 2014 |
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; HIV-1; Indoles; Inhibitory Concentration 50; Molecular Docking Simulation; Reverse Transcriptase Inhibitors; Stereoisomerism; Structure-Activity Relationship; Sulfones | 2014 |
Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents.
Topics: Aniline Compounds; Anti-HIV Agents; Cell Line; Drug Design; Ether; HIV Infections; HIV-1; Humans; Models, Molecular; Reverse Transcriptase Inhibitors | 2015 |
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Topics: Anti-HIV Agents; Binding Sites; Cell Line; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2015 |
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
Topics: Anti-HIV Agents; Cell Line, Tumor; Dose-Response Relationship, Drug; Heterocyclic Compounds; Heterocyclic Compounds, 2-Ring; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Nitrogen; Reverse Transcriptase Inhibitors; Solubility; Structure-Activity Relationship; Sulfones | 2015 |
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
Topics: Anti-HIV Agents; Chemistry Techniques, Synthetic; Computational Biology; Drug Design; HIV Reverse Transcriptase; HIV-1; Imidazoles; Molecular Docking Simulation; Protein Conformation; Pyrazines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2015 |
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
Topics: Anti-HIV Agents; Binding Sites; Cell Line; Drug Design; Granulocyte Precursor Cells; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Docking Simulation; Pyrimidines; Quinolones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Tetradecanoylphorbol Acetate; Virus Latency | 2015 |
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Cells, Cultured; Drug Discovery; HIV Reverse Transcriptase; Humans; Molecular Structure; Nitriles; Piperidines; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2015 |
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Acetanilides; Anti-HIV Agents; Cell Line; Chemistry Techniques, Synthetic; Drug Discovery; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Dynamics Simulation; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazoles | 2015 |
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
Topics: Acetanilides; Anti-HIV Agents; Conserved Sequence; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Molecular Structure; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Tumor Cells, Cultured | 2015 |
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Design; HIV-1; HIV-2; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Pyrimidines; Structure-Activity Relationship | 2015 |
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
Topics: Anti-HIV Agents; Binding Sites; Drug Design; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Point Mutation; Pyridines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2016 |
Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.
Topics: Acetanilides; Anti-HIV Agents; Drug Discovery; Imidazoles; Molecular Structure; Pyridines; Reverse Transcriptase Inhibitors | 2016 |
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
Topics: Anti-HIV Agents; Binding Sites; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Virus Replication | 2016 |
1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
Topics: Animals; Antiviral Agents; Cells, Cultured; Dogs; Dose-Response Relationship, Drug; HIV-1; Influenza A Virus, H1N1 Subtype; Madin Darby Canine Kidney Cells; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Structure-Activity Relationship; Uracil | 2016 |
Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
Topics: Anti-HIV Agents; Drug Stability; Esters; HIV-1; Humans; Inhibitory Concentration 50; Methane; Models, Molecular; Reverse Transcriptase Inhibitors | 2016 |
Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
Topics: Binding Sites; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; Molecular Docking Simulation; Protein Conformation; Pyridines; Pyrimidines; Reverse Transcriptase Inhibitors; Solubility; Structure-Activity Relationship; Water | 2016 |
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
Topics: Anti-Bacterial Agents; Anti-HIV Agents; Carboxylic Acids; DNA-Directed RNA Polymerases; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; Escherichia coli; HEK293 Cells; HeLa Cells; HIV; Humans; Microbial Sensitivity Tests; Molecular Structure; RNA-Directed DNA Polymerase; Structure-Activity Relationship; Thiophenes | 2016 |
Computer-aided discovery of anti-HIV agents.
Topics: Anti-HIV Agents; Computer-Aided Design; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; T-Lymphocytes | 2016 |
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
Topics: Acetanilides; Anti-HIV Agents; Carbon-13 Magnetic Resonance Spectroscopy; HIV-1; Models, Molecular; Proton Magnetic Resonance Spectroscopy; Reverse Transcriptase Inhibitors; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship | 2016 |
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
Topics: Animals; Anti-HIV Agents; Cell Line, Tumor; Drug Resistance, Viral; Heterocyclic Compounds, 2-Ring; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Molecular Docking Simulation; Mutation; Pyrimidines; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfonamides; Thiophenes | 2016 |
Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
Topics: Animals; Anti-HIV Agents; Cell Line; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Mice; Models, Molecular; Reverse Transcriptase Inhibitors; Solubility; Structure-Activity Relationship; Uracil | 2017 |
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
Topics: Anti-HIV Agents; Carbon-13 Magnetic Resonance Spectroscopy; HIV-1; Molecular Docking Simulation; Proton Magnetic Resonance Spectroscopy; Pyrimidines; Reverse Transcriptase Inhibitors; Spectrometry, Mass, Electrospray Ionization | 2017 |
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
Topics: Anti-HIV Agents; Cell Line; Drug Design; HIV Infections; HIV Integrase; HIV Integrase Inhibitors; HIV-1; Humans; Keto Acids; Molecular Docking Simulation; Pyrimidines; Reverse Transcriptase Inhibitors | 2017 |
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Topics: Animals; Anti-HIV Agents; Drug Resistance, Viral; HEK293 Cells; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Models, Molecular; Pyrimidines; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiophenes | 2017 |
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
Topics: Animals; Anti-HIV Agents; Cells, Cultured; Glutamic Acid; HIV-1; Humans; Indoles; Lipopolysaccharides; Mice, Inbred C57BL; Microglia; Molecular Docking Simulation; Mutation; Neurons; Neuroprotective Agents; Reverse Transcriptase Inhibitors; Stereoisomerism; Structure-Activity Relationship; Sulfones | 2017 |
Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
Topics: Anti-HIV Agents; Cell Line; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Indoles; Microbial Sensitivity Tests; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones | 2017 |
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
Topics: Anti-HIV Agents; Carbon-13 Magnetic Resonance Spectroscopy; Cell Line; Drug Design; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Docking Simulation; Proton Magnetic Resonance Spectroscopy; Reverse Transcriptase Inhibitors; Spectrometry, Mass, Electrospray Ionization | 2017 |
Discovery of Thiophene[3,2-
Topics: | 2017 |
Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
Topics: Anti-HIV Agents; Biphenyl Compounds; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Tumor Cells, Cultured | 2018 |
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cell Line, Tumor; Cyclopropanes; HIV Reverse Transcriptase; HIV-1; Humans; Hydrolysis; Mutation; Nevirapine; Nitriles; Prodrugs; Pyridazines; Pyrimidines; Pyrroles; Reverse Transcriptase Inhibitors | 2018 |
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
Topics: Allosteric Regulation; Binding Sites; Drug Design; HIV Reverse Transcriptase; HIV-1; HIV-2; Humans; Molecular Docking Simulation; Protein Structure, Tertiary; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2018 |
Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
Topics: Anti-HIV Agents; Drug Design; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Niacinamide; Point Mutation; Structure-Activity Relationship; Triazoles | 2018 |
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
Topics: | 2018 |
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
Topics: | 2018 |
Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
Topics: Binding Sites; Cell Line; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Nitrogen; Piperazine; Protein Structure, Tertiary; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2018 |
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
Topics: Animals; Anti-HIV Agents; Clinical Trials as Topic; Drug Discovery; HIV Infections; HIV-1; Humans; Reverse Transcriptase Inhibitors | 2019 |
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
Topics: Anti-HIV Agents; Binding Sites; Cell Line; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Mutation; Protein Structure, Tertiary; Pyrimidinones; Stereoisomerism; Structure-Activity Relationship | 2019 |
Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
Topics: Amines; Anti-HIV Agents; Binding Sites; Cell Line, Tumor; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Molecular Structure; Protein Binding; Quinazolines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2019 |
Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
Topics: Anti-HIV Agents; Catechols; Drug Design; HIV Reverse Transcriptase; Molecular Structure; Reverse Transcriptase Inhibitors | 2019 |
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
Topics: Anti-HIV Agents; Biphenyl Compounds; Cell Line; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Conformation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiophenes | 2019 |
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
Topics: Administration, Oral; Animals; Anti-HIV Agents; Apoptosis; Drug Design; Female; HIV Infections; HIV-1; Humans; Ligands; Male; Mice; Microsomes, Liver; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Rats; Reverse Transcriptase Inhibitors; Tissue Distribution; Tumor Cells, Cultured; Virus Replication | 2019 |
Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
Topics: Acetamides; Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2020 |
Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Design; HIV; HIV Reverse Transcriptase; Humans; Indazoles; Microbial Sensitivity Tests; Molecular Structure; Piperidines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2020 |
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
Topics: Animals; Anti-HIV Agents; Cell Line; Crystallography, X-Ray; Drug Discovery; ERG1 Potassium Channel; Female; Fluorine; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microsomes, Liver; Molecular Structure; Protein Binding; Pyrimidines; Rats, Wistar; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiophenes | 2020 |
In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
Topics: Anti-HIV Agents; Binding Sites; Click Chemistry; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Hydrophobic and Hydrophilic Interactions; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Triazoles | 2020 |
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
Topics: Animals; Anti-HIV Agents; Body Weight; Cell Line; Cell Survival; Dose-Response Relationship, Drug; Drug Design; Female; HIV Reverse Transcriptase; HIV-1; Humans; Hydroxides; Male; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidines; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2020 |
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
Topics: Anti-HIV Agents; Cell Line, Tumor; Drug Design; Drug Synergism; HIV Reverse Transcriptase; HIV-1; Humans; Indoles; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Dynamics Simulation; Molecular Structure; Mutation; Protein Binding; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones; Zidovudine | 2020 |
Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
Topics: Binding Sites; HIV Reverse Transcriptase; HIV-1; Morpholines; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Solubility; Structure-Activity Relationship; Water | 2020 |
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
Topics: Anti-HIV Agents; Binding Sites; Drug Design; HIV-1; Humans; Molecular Docking Simulation; Molecular Dynamics Simulation; Protein Binding; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
Topics: Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; Humans; Molecular Dynamics Simulation; Molecular Structure; Pyrimidines; Structure-Activity Relationship | 2021 |
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
Topics: Animals; Anti-HIV Agents; Crystallography, X-Ray; Drug Design; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Mice; Microbial Sensitivity Tests; Molecular Structure; Mutation; Protein Binding; Pyrimidines; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
Topics: Alkylation; Animals; Binding Sites; Biphenyl Compounds; Cell Line; Cell Survival; Drug Design; Drug Stability; Female; Half-Life; HIV Reverse Transcriptase; Humans; Hydrophobic and Hydrophilic Interactions; Mice; Microsomes, Liver; Molecular Docking Simulation; Mutation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
Topics: Anti-HIV Agents; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Design; HIV; HIV Reverse Transcriptase; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Discovery; HIV Reverse Transcriptase; HIV-1; Humans; Hydrophobic and Hydrophilic Interactions; Microbial Sensitivity Tests; Molecular Structure; Mutation; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
Topics: Animals; Anti-HIV Agents; Dose-Response Relationship, Drug; Female; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mice; Microbial Sensitivity Tests; Microsomes, Liver; Models, Molecular; Molecular Structure; Pyrimidines; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
Topics: Anti-HIV Agents; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Naphthalenes; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2021 |
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
Topics: Animals; Anti-HIV Agents; Binding Sites; Cell Survival; Cytochrome P-450 Enzyme System; Drug Design; Drug Resistance, Viral; Drug Stability; Female; Half-Life; HIV Reverse Transcriptase; HIV-1; Humans; Mice; Molecular Docking Simulation; Mutation; Pyridines; Pyrimidines; Solubility; Structure-Activity Relationship | 2022 |
Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
Topics: Anti-HIV Agents; Chemistry, Pharmaceutical; Heterocyclic Compounds, 1-Ring; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Reverse Transcriptase Inhibitors | 2022 |
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
Topics: Anti-HIV Agents; Drug Design; HIV Reverse Transcriptase; HIV-1; Molecular Structure; Reverse Transcriptase Inhibitors; Space Flight; Structure-Activity Relationship | 2022 |
Structure-Based Discovery of Novel NH
Topics: Anti-HIV Agents; Biphenyl Compounds; Drug Design; Heterocyclic Compounds, 1-Ring; HIV Reverse Transcriptase; HIV-1; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2022 |
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
Topics: Animals; Anti-HIV Agents; HIV Reverse Transcriptase; HIV-1; Mice; Molecular Docking Simulation; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2022 |
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries | 2023 |
The molecular basis of resilience to the effect of the Lys103Asn mutation in non-nucleoside HIV-1 reverse transcriptase inhibitors studied by targeted molecular dynamics simulations.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Binding Sites; Computer Simulation; Cyclopropanes; HIV Reverse Transcriptase; Models, Molecular; Mutagenesis, Site-Directed; Nevirapine; Nitriles; Oxazines; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thermodynamics | 2005 |
Prevalence of etravirine-associated mutations in clinical samples with resistance to nevirapine and efavirenz.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines | 2008 |
Prevalence and risk factors for etravirine resistance among patients failing on non-nucleoside reverse transcriptase inhibitors.
Topics: Adult; Anti-HIV Agents; CD4 Lymphocyte Count; Drug Resistance, Viral; Female; HIV Infections; HIV-1; Humans; Italy; Logistic Models; Male; Microbial Sensitivity Tests; Mutation; Nevirapine; Nitriles; Prevalence; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Risk Factors; RNA, Viral; Treatment Failure | 2008 |
Etravirine resistance associated mutations in HIV-infected patients failing efavirenz or nevirapine in the Spanish antiretroviral resistance database.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; HIV-1; Humans; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Spain; Treatment Failure | 2010 |
Suboptimal etravirine activity is common during failure of nevirapine-based combination antiretroviral therapy in a cohort infected with non-B subtype HIV-1.
Topics: Adult; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Drug Resistance, Viral; Female; Genotype; HIV Infections; HIV-1; Humans; Male; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Treatment Failure; Viral Load; Viral Proteins | 2010 |
Using of nevirapine is associated with intermediate and reduced response to etravirine among HIV-infected patients who experienced virologic failure in a resource-limited setting.
Topics: Adult; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Developing Countries; Female; HIV Infections; HIV-1; Humans; Male; Middle Aged; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Retrospective Studies; Thailand; Treatment Outcome | 2010 |
HIV type 1 antiretroviral resistance mutations in subtypes B, C, and F in the City of São Paulo, Brazil.
Topics: Alkynes; Benzoxazines; Brazil; Cohort Studies; Cyclopropanes; Darunavir; Drug Resistance, Multiple, Viral; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Mutation; Nevirapine; Nitriles; Pyridazines; Pyridines; Pyrimidines; Pyrones; Reverse Transcriptase Inhibitors; Sulfonamides; Treatment Failure; Viral Load | 2010 |
Constrained patterns of covariation and clustering of HIV-1 non-nucleoside reverse transcriptase inhibitor resistance mutations.
Topics: Alkynes; Amino Acid Substitution; Anti-HIV Agents; Benzoxazines; Cyclopropanes; DNA Mutational Analysis; Drug Resistance, Multiple, Viral; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2010 |
Patients infected with HIV type 1 subtype CRF01_AE and failing first-line nevirapine- and efavirenz-based regimens demonstrate considerable cross-resistance to etravirine.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Treatment Failure | 2010 |
Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions.
Topics: Alkynes; Amino Acids; Benzoxazines; Binding Sites; Cyclopropanes; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Models, Biological; Molecular Dynamics Simulation; Mutation; Nevirapine; Nitriles; Protein Binding; Protein Conformation; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Thermodynamics; Uracil; Water | 2011 |
Differential impact of the HIV-1 non-nucleoside reverse transcriptase inhibitor mutations K103N and M230L on viral replication and enzyme function.
Topics: Alkynes; Amino Acid Substitution; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Virus Replication | 2010 |
Impact of the N348I mutation in HIV-1 reverse transcriptase on nonnucleoside reverse transcriptase inhibitor resistance in non-subtype B HIV-1.
Topics: Alkynes; Amino Acid Substitution; Benzoxazines; Cell Line; Cyclopropanes; Drug Resistance, Viral; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Sequence Data; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2011 |
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cells, Cultured; Cyclopropanes; HIV Reverse Transcriptase; HIV-1; Humans; Indoles; Leukocytes, Mononuclear; Models, Molecular; Molecular Conformation; Mutation; Nevirapine; Nitriles; Protein Binding; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Sulfones | 2011 |
Nonnucleoside reverse transcriptase inhibitor-resistant HIV is stimulated by efavirenz during early stages of infection.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Virus Replication | 2011 |
Antiretroviral resistance patterns and factors associated with resistance in adult patients failing NNRTI-based regimens in the Western Cape, South Africa.
Topics: Adult; Alkynes; Anti-HIV Agents; Benzoxazines; CD4 Lymphocyte Count; Cross-Sectional Studies; Cyclopropanes; Drug Resistance, Viral; Female; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Male; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; RNA, Viral; South Africa; Treatment Failure; Viral Load; Zidovudine | 2011 |
Prevalence of etravirine-associated mutations in clinical samples with genotypic resistance to nevirapine and efavirenz in Brazilian clinics.
Topics: Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Brazil; Cyclopropanes; Drug Resistance, Viral; HIV; HIV Infections; Humans; Mutation, Missense; Nevirapine; Nitriles; Prevalence; Pyridazines; Pyrimidines | 2011 |
Docking analysis and resistance evaluation of clinically relevant mutations associated with the HIV-1 non-nucleoside reverse transcriptase inhibitors nevirapine, efavirenz and etravirine.
Topics: Alkynes; Amino Acid Substitution; Benzoxazines; Binding Sites; Computer Simulation; Cyclopropanes; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Hydrogen Bonding; Nevirapine; Nitriles; Protein Structure, Tertiary; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors | 2011 |
Emerging mutations and associated factors in patients displaying treatment failure on an etravirine-containing regimen.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Drug Therapy, Combination; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Molecular Typing; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; RNA, Viral; Treatment Failure; Viral Load | 2012 |
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.
Topics: Chemistry Techniques, Synthetic; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; Inhibitory Concentration 50; Kinetics; Molecular Docking Simulation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Thiazolidines; Toxicity Tests | 2013 |
Susceptibility to etravirine of HIV type 1 subtype C isolates from nevirapine/efavirenz-experienced patients: comparative interpretation of ANRS and STANFORD algorithms.
Topics: Alkynes; Amino Acid Sequence; Anti-HIV Agents; Benzoxazines; Cyclopropanes; DNA, Viral; Drug Resistance, Viral; HIV Infections; HIV Integrase; HIV-1; Humans; Molecular Sequence Data; Mozambique; Nevirapine; Nitriles; Proviruses; Pyridazines; Pyrimidines; Sequence Analysis, DNA | 2012 |
Panel of prototypical recombinant infectious molecular clones resistant to nevirapine, efavirenz, etravirine, and rilpivirine.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cloning, Molecular; Cyclopropanes; Drug Resistance, Multiple, Viral; Drug Resistance, Viral; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2012 |
Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.
Topics: Alkynes; Amino Acid Substitution; Benzoxazines; Cyclopropanes; Delavirdine; Deoxycytidine; Drug Resistance, Viral; Emtricitabine; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Leukocytes, Mononuclear; Microbial Sensitivity Tests; Mutagenesis, Site-Directed; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Virus Replication | 2013 |
Etravirine and rilpivirine-specific mutations selected by efavirenz and nevirapine exposure in patients infected with HIV-1 non-B subtypes.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; Drug Resistance, Viral; Genotype; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Mutation, Missense; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Treatment Outcome; Viral Load | 2014 |
Mass Spectrometric Characterization of HIV-1 Reverse Transcriptase Interactions with Non-nucleoside Reverse Transcriptase Inhibitors.
Topics: Alkynes; Anti-HIV Agents; Benzoxazines; Cyclopropanes; HIV Reverse Transcriptase; Mass Spectrometry; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine | 2016 |
Role of Rilpivirine and Etravirine in Efavirenz and Nevirapine-Based Regimens Failure in a Resource-Limited Country: A Cross- Sectional Study.
Topics: Adult; Alkynes; Anti-HIV Agents; Benzoxazines; Cross-Sectional Studies; Cyclopropanes; Drug Resistance, Viral; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Mutation; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Thailand; Viral Load; Young Adult | 2016 |
Prevalence of Rilpivirine and Etravirine Resistance Mutations in HIV-1 Subtype C-Infected Patients Failing Nevirapine or Efavirenz-Based Combination Antiretroviral Therapy in Botswana.
Topics: Adult; Alkynes; Anti-HIV Agents; Antiretroviral Therapy, Highly Active; Benzoxazines; Botswana; Cyclopropanes; Drug Resistance, Viral; Female; Genotype; Genotyping Techniques; HIV Infections; HIV-1; Humans; Male; Microbial Sensitivity Tests; Mutation; Nevirapine; Nitriles; pol Gene Products, Human Immunodeficiency Virus; Prevalence; Pyridazines; Pyrimidines; Rilpivirine; Treatment Failure; Young Adult | 2018 |
Frequency of cross-resistance to rilpivirine and etravirine among HIV-1 subtype C infected individuals failing nevirapine/efavirenz based ART regimen.
Topics: Alkynes; Benzoxazines; Cyclopropanes; HIV Infections; HIV-1; Humans; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Rilpivirine; Sweden | 2019 |
Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors by exploring the structure-activity relationship of solvent-exposed regions I.
Topics: Binding Sites; Catalytic Domain; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Mutagenesis, Site-Directed; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Solvents; Structure-Activity Relationship | 2019 |
Prevalence of predicted resistance to doravirine in HIV-1-positive patients after exposure to non-nucleoside reverse transcriptase inhibitors.
Topics: Adult; Alkynes; Anti-HIV Agents; Benzoxazines; Cross-Sectional Studies; Cyclopropanes; Delavirdine; Drug Resistance, Viral; Female; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Male; Nevirapine; Nitriles; Pyridazines; Pyridones; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Treatment Outcome; Triazoles | 2019 |