quinidine has been researched along with ketoconazole in 164 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 1 (0.61) | 18.7374 |
| 1990's | 17 (10.37) | 18.2507 |
| 2000's | 60 (36.59) | 29.6817 |
| 2010's | 65 (39.63) | 24.3611 |
| 2020's | 21 (12.80) | 2.80 |
| Authors | Studies |
|---|---|
| Cvetkovic, M; Fromm, MF; Kim, RB; Leake, B; Wilkinson, GR | 1 |
| Choo, EF; Imamura, H; Kim, RB; Leake, B; Wandel, C; Wilkinson, GR; Wood, AJ | 1 |
| Huang, L; Humphreys, JE; Morgan, JB; Polli, JW; Serabjit-Singh, CS; Webster, LO; Wring, SA | 1 |
| Casciano, CN; Clement, RP; Johnson, WW; Wang, EJ | 2 |
| Alvarez-Pedraglio, A; Colmenarejo, G; Lavandera, JL | 1 |
| Pajeva, IK; Wiese, M | 1 |
| Fischer, H; Huwyler, J; Poli, S; Schwab, D; Tabatabaei, A | 1 |
| Keserü, GM | 1 |
| Bacsó, Z; Cianfriglia, M; Fenyvesi, F; Goda, K; Kappelmayer, J; Lustyik, G; Nagy, H; Szabó, G; Szilasi, M | 1 |
| Hiratsuka, A; Iwata, H; Kadota, S; Tezuka, Y; Usia, T; Watabe, T | 1 |
| Kadota, S; Tezuka, Y; Usia, T; Watabe, T | 1 |
| Nagashima, R; Nishikawa, T; Tobita, M | 1 |
| Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL | 1 |
| Antes, I; Biemel, K; Hartmann, RW; Marchais-Oberwinkler, S; Müller-Vieira, U; Scherer, C; Voets, M | 1 |
| Hashizume, H; Kawasaki, M; Komatsu, M; Matsumoto, M; Sasaki, H; Shimokawa, Y; Tomishige, T; Tsubouchi, H | 1 |
| Fetzer, L; Frotscher, M; Hartmann, RW; Kruchten, P; Marchais-Oberwinkler, S; Messinger, J; Müller-Vieira, U; Neugebauer, A; Scherer, C; Thole, H; Ziegler, E | 1 |
| Jia, L; Sun, H | 1 |
| Artursson, P; Bergström, CA; Hoogstraate, J; Matsson, P; Norinder, U; Pedersen, JM | 1 |
| Birk, B; Grombein, CM; Hartmann, RW; Heim, R; Lucas, S; Müller-Vieira, U; Negri, M; Ries, C; Schewe, KE | 1 |
| Antes, I; Bisi, A; Gobbi, S; Hartmann, RW; Heim, R; Lucas, S; Negri, M; Ries, C; Schewe, KE | 1 |
| Ahlin, G; Artursson, P; Bergström, CA; Gustavsson, L; Karlsson, J; Larsson, R; Matsson, P; Norinder, U; Pedersen, JM | 1 |
| Birk, B; Hartmann, RW; Heim, R; Lucas, S; Ries, C; Schewe, KE | 1 |
| Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A | 1 |
| Choi, SS; Contrera, JF; Hastings, KL; Kruhlak, NL; Sancilio, LF; Weaver, JL; Willard, JM | 1 |
| García-Mera, X; González-Díaz, H; Prado-Prado, FJ | 1 |
| Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ | 1 |
| Ghosh, I; Manoharlal, R; Prakash, O; Prasad, R; Puri, N; Sharma, M | 1 |
| Glen, RC; Lowe, R; Mitchell, JB | 1 |
| Afshari, CA; Eschenberg, M; Hamadeh, HK; Lee, PH; Lightfoot-Dunn, R; Morgan, RE; Qualls, CW; Ramachandran, B; Trauner, M; van Staden, CJ | 1 |
| Ekins, S; Williams, AJ; Xu, JJ | 1 |
| Auw, L; Awale, S; Kadota, S; Li, F; Morikawa, K; Nobukawa, T; Tezuka, Y | 1 |
| Barreiro, EJ; da Silva, LL; Fraga, AG; Fraga, CA | 1 |
| Frotscher, M; Hartmann, RW; Henn, C; Kruchten, P; Marchais-Oberwinkler, S; Werth, R; Wetzel, M; Ziegler, E | 1 |
| Hartmann, RW; Heim, R; Lucas, S; Negri, M; Zimmer, C | 1 |
| Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR | 1 |
| Ambroso, JL; Ayrton, AD; Baines, IA; Bloomer, JC; Chen, L; Clarke, SE; Ellens, HM; Harrell, AW; Lovatt, CA; Reese, MJ; Sakatis, MZ; Taylor, MA; Yang, EY | 1 |
| Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ | 1 |
| Calvet, CM; Cameron, MD; Choi, JY; Gunatilleke, SS; McKerrow, JH; Podust, LM; Roush, WR; Ruiz, C | 1 |
| Andréola, ML; Bailly, F; Calmels, C; Christ, F; Cotelle, P; Debyser, Z; Lion, C; Suchaud, V | 1 |
| Bae, IH; Choi, JK; Chough, C; Jang, SK; Keum, SJ; Kim, BM; Kim, H | 1 |
| Cheon, SH; Choi, K; Hahn, HG; Han, M; Song, C; Yun, J | 1 |
| Ahn, YG; Bang, HJ; Hong, DJ; Jung, SH; Kim, D; Kim, EY; Kim, J; Kim, M; Kim, YJ; Lee, K; Min, KH; Park, EJ; Suh, KH | 1 |
| Hahn, HG; Han, M; Jeong, N; Song, C | 1 |
| Aubé, J; Chu, YK; Chung, D; Golden, JE; Guo, H; Jonsson, CB; McKellip, S; Noah, JW; Rasmussen, L; Roy, S; Schroeder, CE; Smith, LH; Smith, RA; Sosa, M; Sotsky, J; Tower, NA; White, EL; Yao, T | 1 |
| Ayan, D; Hospital, A; Maltais, R; Poirier, D | 1 |
| Kheylik, Y; Kondratov, I; Krasavin, M; Naumchyk, V; Platonov, M; Zahanich, I; Zozulya, S | 1 |
| Bracke, ME; De Ryck, T; Katritzky, AR; Patronov, A; Roman, BI; Slavov, SH; Stevens, CV; Vanhoecke, BW | 1 |
| Cho, H; Elkamhawy, A; Heo, JC; Kim, HY; Kim, KH; Lee, CO; Nam, DH; Pae, AN; Park, WK; Roh, EJ; Seol, HJ; Viswanath, AN; Yang, H | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Budriesi, R; Carosati, E; Chiarini, A; Chiu, FC; Cosimelli, B; Frosini, M; Fusi, F; Ioan, P; Katneni, K; Matucci, R; Micucci, M; Saponara, S; Severi, E; Spinelli, D | 1 |
| Li, H; Martásek, P; Poulos, TL; Qin, Y; Roman, LJ; Silverman, RB; Wang, HY | 1 |
| Andréola, ML; Bailly, F; Billamboz, M; Christ, F; Cotelle, P; Debyser, Z; Lion, C; Suchaud, V | 1 |
| Carazo, A; Drechslerová, M; Hrušková, ZR; Hyrsova, L; Kuneš, J; Nova, A; Pavek, P; Pour, M; Smutny, T; Špulák, M | 1 |
| Kovalenko, A; Krasavin, M; Lukin, A; Moore, D; Tikhonova, IG; Zahanich, I; Zhurilo, N; Zozulya, S | 1 |
| Cheng, M; Hao, C; Liu, C; Su, X; Sun, B; Wei, P; Zhang, X; Zhao, D; Zhao, L; Zhao, S | 1 |
| Cheng, M; Hao, C; Liu, C; Su, X; Wei, P; Wu, M; Zhang, X; Zhao, D; Zhao, L; Zhao, S | 1 |
| Chen, F; Chen, W; Lan, L; Li, B; Li, J; Liu, Y; Mao, F; Ni, S; Wei, H; Zhu, J | 1 |
| Aljayyoussi, G; Amewu, RK; Angulo-Barturén, I; Bazaga, SF; Belén, M; Biagini, GA; Campo, B; Charman, SA; Chen, G; Davies, J; Martínez, MS; Nixon, GL; O' Neill, PM; Roberts, NL; Ryan, E; Sabbani, S; Shackleford, DM; Sharma, R; Shore, ER; Stocks, PA; Ward, SA | 1 |
| Lazor, JA; McNulty, RM; Sketch, M | 1 |
| Greenblatt, DJ; Harmatz, JS; Schmider, J; Shader, RI; von Moltke, LL | 1 |
| Collins, JM; Jamis-Dow, CA; Katki, AG; Klecker, RW | 1 |
| Cotreau-Bibbo, MM; Greenblatt, DJ; Harmatz, JS; Shader, RI; von Moltke, LL | 1 |
| Cotreau-Bibbo, MM; Duan, SX; Greenblatt, DJ; Harmatz, JS; Shader, RI; von Moltke, LL | 1 |
| Berger, Y; Bourrié, M; Fabre, G; Meunier, V | 1 |
| Cayen, MN; Chen, KJ; Clement, RP; Huie, K; Snow, M; Yumibe, N | 1 |
| Bayliss, MK; Eddershaw, PJ; Herriott, D; Manchee, GR; Park, GR; Ranshaw, LE; Tarbit, MH | 1 |
| Sequeira, DJ; Strobel, HW | 1 |
| Jones, BC; Smith, DA; Tyman, CA | 1 |
| Ishizaki, T; Kawashiro, T; Zhao, XJ | 1 |
| Beaune, P; Brosen, K; Flinois, JP; Nielsen, TL; Rasmussen, BB | 1 |
| Hata, T; Iwasaki, K; Kaneko, H; Shiraga, T; Suzuki, A; Tozuka, Z | 1 |
| Greenblatt, DJ; Venkatakrishnan, K; von Moltke, LL | 1 |
| Aguilar, AJ; Grace, JM; Skanchy, DJ | 1 |
| Linnet, K; Olesen, OV | 1 |
| Bertilsson, L; Ericsson, O; Gustafsson, LL; Hellgren, U; Mirghani, RA; Westerberg, PA | 1 |
| Obach, RS | 1 |
| Kagayama, A; Mitani, Y; Niwa, T; Shiraga, T; Terakawa, M; Tokuma, Y | 1 |
| Mason, HJ; Rawbone, R; Sams, C | 1 |
| Ekins, S; Mankowski, DC; Margolis, JM; O'Donnell, JP; Obach, RS | 1 |
| Greenblatt, DJ; Hesse, LM; Shader, RI; Venkatakrishnan, K; von Moltke, LL | 1 |
| Bigler, L; Follath, F; Ha, HR; Kozlik, P; Stieger, B | 1 |
| Beckurts, KT; Brachtendorf, L; Fuhr, U; Hölscher, AH; Jetter, A | 1 |
| Bhoopathy, S; Karnes, HT; Sarkar, MA | 1 |
| Hyland, R; Jones, BC; Smith, DA | 1 |
| Bertilsson, L; Ericsson, O; Gustafsson, LL; Mirghani, RA; Tybring, G | 1 |
| Chiba, K; Kobayashi, K; Shimada, N; Urashima, K | 1 |
| Bertilsson, L; Ericsson, O; Gustafsson, LL; Hellgren, U; Mirghani, RA | 1 |
| Fouda, HG; Khojasteh-Bakht, SC; Prakash, C; Rossulek, MI | 1 |
| Haehner, T; Müller-Enoch, D; Refaie, MO | 1 |
| Black, ML; Duncan, JN; Toth, LN; Yamazaki, S | 1 |
| Howald, W; Lalovic, B; Phillips, B; Risler, LL; Shen, DD | 1 |
| Kuroha, M; Shimoda, M; Shirai, Y | 1 |
| Kanamaru, H; Kitamura, A; Komuro, S; Mizuno, Y; Natsui, K; Yabuki, M | 1 |
| Gundu, J; Machavaram, KK; Yamsani, MR | 1 |
| Gottesdiener, KM; Kari, PP; Marbury, T; Miller, JL; Mistry, GC; Rodrigues, AD; Simpson, RC; Wagner, JA; Winchell, GA | 1 |
| Chatelain, P; Fuks, B; Gillard, M; Wolff, C | 1 |
| Fuhr, U; Kober, S; Mutschler, E; Spahn-Langguth, H; Zaigler, M | 1 |
| Keogh, JP; Kunta, JR | 1 |
| Haining, RL; Yu, AM | 1 |
| Hasselstrøm, J; Linnet, K | 1 |
| Liu, XQ; Wang, GJ; Zhao, XP; Zhong, J | 1 |
| Allqvist, A; Bertilsson, L; Mirghani, RA; Miura, J | 1 |
| Burman, AC; Jaggi, M; Mukherjee, R; Rajendran, P; Singh, MK | 1 |
| Hu, BR; Huang, Y; Li, S; Liu, P; Wang, JL; Xiang, JZ; Zhao, LB | 1 |
| Crewe, HK; Ghobadi, C; Gregory, A; Lennard, MS; Rostami-Hodjegan, A | 1 |
| Freudenthaler, S; Kotsuma, M; Nishimura, K; Tokui, T | 1 |
| Elsby, R; Gray, AJ; Smith, VN; Surry, DD | 1 |
| Chiba, M; Ishii, Y; Shibata, Y; Takahashi, H | 1 |
| Coelho, EB; Lanchote, VL; Rocha, A | 1 |
| Boralli, VB; Coelho, EB; Lanchote, VL | 1 |
| Boonprasert, K; Chaijaroenkul, W; Na-Bangchang, K; Sangsuwan, P; Tantisawat, J; Wisedpanichkij, R | 1 |
| Bajrami, B; Rusling, JF; Schenkman, JB; Zhao, L | 1 |
| Daali, Y; Dayer, P; Desmeules, JA; Eap, CB; Hochstrasser, D; Hopfgartner, G; Rebsamen, MC; Rossier, MF; Samer, CF; Wagner, M | 1 |
| Castberg, I; Davies, SJ; Lennard, MS; Lewis, G; Spigset, O; Taylor, S; Westin, AA | 1 |
| Bandyopadhyay, A; Mukherjee, PK; Ota, S; Pandit, S; Ponnusankar, S | 1 |
| Funae, Y; Imaoka, S; Oguro, A; Sakamoto, K | 1 |
| Di Nardo, G; Ferrero, S; Gilardi, G; Sadeghi, SJ | 1 |
| Kubickova, B; Martinkova, M; Stiborova, M | 1 |
| Ahmed, Z; Bentz, J; Ellens, H; Hidalgo, IJ; Li, J; Li, L; Lumen, AA; Meng, Z; Owen, A | 1 |
| Cheng, KW; Huang, L; Rigas, B; Xie, G | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M | 1 |
| Chan-Penebre, E; Chesworth, R; Copeland, RA; Duncan, KW; Lantz, RJ; Miao, X; Moyer, MP; Munchhof, MJ; Rioux, N; Waters, NJ | 1 |
| Badyra, B; Kudolo, J; Lisowski, B; Polak, S; Wiśniowska, B | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; Siissalo, S; van Dam, A | 1 |
| Camenisch, G; Chibale, K; Huth, F; Njuguna, NM; Schiller, H; Umehara, KI | 1 |
| de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; van de Steeg, E | 1 |
| Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S | 1 |
| Bhatt, S; Dogra, A; Gour, A; Kotwal, P; Magotra, A; Nandi, U; Sharma, A; Singh, G; Wazir, P | 1 |
| Marathe, P; Rodrigues, AD; Shen, H; Sinz, M; Yao, M; Zhu, M | 1 |
| Bao, QC; Jia, JM; Jiang, F; Jin, YH; Li, DD; Liu, F; Wang, HJ; Wang, L; Wang, ZH; Xu, XL; You, QD; Zhang, Q | 1 |
| Cheng, M; Hao, C; Jiang, X; Su, X; Wei, P; Wu, M; Zhang, X; Zhao, D; Zhao, L; Zhao, S | 1 |
| Barouch-Bentov, R; Brannan, JM; De Jonghe, S; Dye, JM; Einav, S; Herdewijn, P; O'Brien, CM; Prugar, LI; Pu, SY; Rozenski, J; Schor, S; Wouters, R | 1 |
| Huan, Y; Liu, Z; Pan, X; Shen, Z; Sun, Z; Xiao, Z; Yang, Y; Zhou, T | 1 |
| Cini, E; De Santis, R; Giannini, G; Manera, F; Manetti, F; Milazzo, FM; Pace, S; Petricci, E; Stasi, MA; Tallarico, C; Vesci, L | 1 |
| Jang, S; Jung, D; Lee, JW; Lee, S; Min, KH; Song, J | 1 |
| Bojarski, AJ; Cieślik, P; Handzlik, J; Hogendorf, A; Hogendorf, AS; Kieć-Kononowicz, K; Latacz, G; Lubelska, A; Wierońska, JM; Woźniak, M | 1 |
| Battista, MR; Brun, R; Calvet, CM; Cirilli, R; Costi, R; De Leo, A; De Vita, D; Di Marco, A; Di Santo, R; Faggi, C; Jennings, GK; Kaiser, M; Madia, VN; Mäser, P; Messore, A; Pepe, G; Pescatori, L; Podust, LM; Saccoliti, F; Scipione, L; Summa, V; Tudino, V | 1 |
| Caligari, S; Callegari, E; De Toma, C; Dilernia, R; Frigerio, F; Graziani, D; Longhi, M; Menegon, S; Pinzi, L; Pirona, L; Rastelli, G; Riva, C; Tazzari, V; Valsecchi, AE; Vistoli, G | 1 |
| Chen, CH; De Clercq, E; Feng, D; Ginex, T; Kang, D; Lee, KH; Liu, X; Luque, FJ; Murugan, NA; Pannecouque, C; Steitz, TA; Wang, Z; Wei, F; Wu, G; Yang, Y; Zhan, P; Zhang, H; Zhang, J; Zhao, T | 1 |
| Bartel, K; Bracher, F; Christianson, DW; Herp, D; Jung, M; Marek, M; Müller, M; Ong, N; Porter, NJ; Robaa, D; Romier, C; Schmidtkunz, K; Senger, J; Shaik, TB; Sippl, W; Vögerl, K | 1 |
| Adebesin, AM; Falck, JR; Fischer, R; Konkel, A; Lossie, J; Paudyal, MP; Puli, N; Schunck, WH; Vijaykumar, J; Wesser, T; Westphal, C; Zhu, C | 1 |
| Agarwal, G; Banerjee, M; Bommakanti, A; Borhade, P; Das, AK; Dash, A; Dhayagude, U; Goswami, A; Gote, G; Gundu, J; Joshi, AA; Kamboj, RK; Kuldharan, S; Kumar, H; Loriya, R; Mallurwar, S; Mehta, M; Modi, D; Modi, F; Narasimham, L; Nigade, P; Palle, VP; Patil, V; Ramdas, V; Sharma, S; Singh, M; Sivaram, A; Srivastava, P; Talwar, R; Walke, DS | 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 |
| Guo, HF; Jin, J; Li, ZR; Liu, ZY; Xie, ZS; Xue, ST; Yi, H; Zhang, L | 1 |
| Azuaje, J; Brea, J; Caamaño, O; García-Mera, X; Gutiérrez-de-Terán, H; Jespers, W; Loza, MI; Majellaro, M; Mallo-Abreu, A; Prieto-Díaz, R; Sotelo, E; Velando, C | 1 |
| Fu, L; Huang, H; Li, G; Li, Y; Liu, Y; Lu, H; Lu, Y; Ma, C; Sheng, L; Wang, B; Zhang, B; Zhang, D; Zhao, H | 1 |
| Ai, W; Chen, Y; Dong, Y; Kang, D; Liang, R; Liu, X; Meng, Q; Pang, J; Sun, Z; Wu, T; Zhan, P; Zhao, T; Zhao, Z | 1 |
| Chen, LZ; Huang, X; Liu, MM; Liu, XH; Ma, D; Shi, JB; Shu, HY; Wu, J; Yu, YL | 1 |
| Chen, SH; Duan, YC; Guan, YY; He, ZH; Jin, LF; Liu, YJ; Ren, HM; Song, Y; Xu, YT; Yuan, H; Zhang, SJ | 1 |
| Chen, FE; De Clercq, E; Ding, L; Pannecouque, C; Zhuang, C | 2 |
| Cheng, M; Cui, H; Jiang, H; Li, S; Liu, L; Su, X; Sun, Y; Wu, T; Yin, W; Zhang, Y; Zhao, D; Zhao, L; Zheng, Y | 1 |
| Chen, Y; Dong, R; Hou, S; Huang, J; Li, H; Liu, C; Liu, X; Lu, T; Tang, W; Wang, X; Xu, J; Zhang, T; Zhang, Y | 1 |
| Consoli, V; D'Agata, V; D'Amico, AG; Fallica, AN; Floresta, G; Intagliata, S; Pittalà, V; Rescifina, A; Romeo, G; Salerno, L; Sorrenti, V; Vanella, L | 1 |
| Ding, Q; Fan, G; Gao, D; Jiang, Y; Li, Q; Li, W; Ma, C; Mao, L; Xu, G; Yang, S; Zhang, D; Zhang, S; Zhao, J; Zhao, M; Zhu, L | 1 |
| Bertagnin, C; Du, R; Guizzo, L; Hou, L; Huang, B; Jia, R; Ju, H; Kang, D; Kong, X; Li, P; Liu, X; Loregian, A; Ma, X; Murugan, NA; Poongavanam, V; Zhan, P; Zhang, Y | 1 |
| Beloglazkina, EK; Ber, AP; Borisova, YA; Chepikova, OE; Erofeev, A; Gorelkin, P; Khazanova, ES; Khudyakov, AD; Kolmogorov, VS; Kovalev, S; Machulkin, AE; Majouga, AG; Nimenko, EA; Pankratov, AA; Petrov, SA; Plotnikova, EA; Pokrovsky, VS; Polshakov, VI; Shafikov, RR; Skvortsov, DA; Smirnova, GB; Uspenskaya, AA; Vaneev, AN; Zamyatnin, AA; Zyk, NU; Zyk, NV | 1 |
| Ji, J; Liang, R; Liao, H; Liu, X; Pang, J; Shi, X; Tao, Y; Wu, T; Zhan, P; Zhang, J; Zhang, Z; Zhao, F; Zhao, T | 1 |
| Bong Han, S; Hwang, D; Jung, E; Jung, YS; Kumar Biswas, B; Malpani, YR; Soo Shin, J; Vishakantegowda, AG | 1 |
| Cheng, M; Qin, Q; Sun, Y; Wang, J; Wang, L; Wu, T; Xue, Y; Yang, H; Yin, W; Zhao, D | 1 |
| Chen, FE; De Clercq, E; Huang, WJ; Jin, X; Pannecouque, C; Wang, S; Zhang, YX; Zhao, LM | 1 |
| Bae, S; Cho, Y; Choi, J; Kang, JA; Kim, YC; Lee, D; Lim, C; Park, M; Park, SG; Seo, J | 1 |
| Barrow, D; Eissa, AG; Foster, PA; Gee, J; Powell, LE; Simons, C | 1 |
1 review(s) available for quinidine and ketoconazole
| Article | Year |
|---|---|
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 |
6 trial(s) available for quinidine and ketoconazole
| Article | Year |
|---|---|
The roles of cytochrome P450 3A4 and 1A2 in the 3-hydroxylation of quinine in vivo.
Topics: Adult; Antifungal Agents; Antimalarials; Area Under Curve; Cross-Over Studies; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Female; Fluvoxamine; Humans; Hydroxylation; Ketoconazole; Male; Mixed Function Oxygenases; Quinidine; Quinine; Selective Serotonin Reuptake Inhibitors | 1999 |
Quinine 3-hydroxylation as a biomarker reaction for the activity of CYP3A4 in man.
Topics: Adult; Biomarkers; Cross-Over Studies; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Female; Fluvoxamine; Humans; Hydroxylation; Isoenzymes; Ketoconazole; Male; Middle Aged; Quinidine; Quinine | 2003 |
Metabolism and elimination of quinine in healthy volunteers.
Topics: Antimalarials; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Benzoquinones; Chromatography, High Pressure Liquid; Cross-Over Studies; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Fluvoxamine; Humans; Ketoconazole; Mixed Function Oxygenases; Quinidine; Quinine; Quinones; Time Factors | 2003 |
The effect of ketoconazole on the pharmacokinetics of a selective alpha 1A-adrenoceptor antagonist.
Topics: Administration, Oral; Adrenergic alpha-1 Receptor Antagonists; Adult; Area Under Curve; Carbon Radioisotopes; Coumarins; Cross-Over Studies; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Double-Blind Method; Drug Administration Schedule; Drug Therapy, Combination; Fomepizole; Half-Life; Humans; Ketoconazole; Male; Microsomes, Liver; Pyrazoles; Pyrimidinones; Quinidine; Receptors, Adrenergic, alpha-1; Sulfaphenazole; Theophylline | 2005 |
Effects of ketoconazole and quinidine on pharmacokinetics of pactimibe and its plasma metabolite, R-125528, in humans.
Topics: Adult; Alkanes; Area Under Curve; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Drug Interactions; Enzyme Inhibitors; Humans; Indoleacetic Acids; Indoles; Ketoconazole; Male; Placebos; Quinidine; Sensitivity and Specificity | 2008 |
The effects of CYP2D6 and CYP3A activities on the pharmacokinetics of immediate release oxycodone.
Topics: Adult; Analgesics, Opioid; Cross-Over Studies; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Double-Blind Method; Drug Interactions; Enzyme Inhibitors; Genotype; Humans; Ketoconazole; Male; Metabolic Detoxication, Phase I; Oxycodone; Phenotype; Polymorphism, Genetic; Quinidine; Receptors, Opioid, mu; Young Adult | 2010 |
157 other study(ies) available for quinidine and ketoconazole
| Article | Year |
|---|---|
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
Topics: Animals; Anion Transport Proteins; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport, Active; Caco-2 Cells; Carrier Proteins; Genes, MDR; HeLa Cells; Histamine H1 Antagonists; Humans; LLC-PK1 Cells; Mice; Rats; Swine; Terfenadine; Tissue Distribution; Transfection; Vaccinia virus | 1999 |
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Brain; Caco-2 Cells; Dibenzocycloheptenes; HIV Protease Inhibitors; Humans; Inhibitory Concentration 50; Male; Mice; Quinolines; Testis | 2000 |
Rational use of in vitro P-glycoprotein assays in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cells, Cultured; Chromatography, Liquid; Enzyme Inhibitors; Fluoresceins; Fluorescent Dyes; Humans; Mass Spectrometry; Pharmacology; Spodoptera | 2001 |
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Topics: 3T3 Cells; Adrenergic Uptake Inhibitors; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding Sites; Biological Transport, Active; Cell Line; Cell Separation; Cell Survival; Flow Cytometry; Fluorescent Dyes; Humans; Inhibitory Concentration 50; Mice; Protein Binding; Reserpine; Spectrometry, Fluorescence; Substrate Specificity; Time Factors | 2001 |
Cheminformatic models to predict binding affinities to human serum albumin.
Topics: Adrenergic beta-Antagonists; Antidepressive Agents, Tricyclic; Chromatography, Affinity; Cyclooxygenase Inhibitors; Databases, Factual; Humans; Hydrophobic and Hydrophilic Interactions; Penicillins; Pharmaceutical Preparations; Protein Binding; Quantitative Structure-Activity Relationship; Reproducibility of Results; Serum Albumin; Steroids | 2001 |
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
Topics: Adenosine Triphosphatases; Algorithms; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding Sites; Binding, Competitive; Caco-2 Cells; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Fluoresceins; Humans; Ligands; Models, Molecular; Molecular Structure; Quantitative Structure-Activity Relationship; Radioligand Assay; Rhodamine 123; Stereoisomerism; Verapamil; Vinblastine | 2002 |
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
Topics: Adenosine Triphosphatases; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Cells, Cultured; Drug Evaluation, Preclinical; Fluoresceins; Fluorescent Dyes; Humans; Indicators and Reagents; Mice; Models, Molecular; Rhodamines; Species Specificity; Swine | 2003 |
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Binding Sites; Biological Transport, Active; Biomarkers; Cells, Cultured; Drug Interactions; Fluorescent Dyes; Humans | 2003 |
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
Topics: Cation Transport Proteins; Databases, Factual; Discriminant Analysis; Ether-A-Go-Go Potassium Channels; Holography; Linear Models; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Quantitative Structure-Activity Relationship | 2003 |
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
Topics: Adenosine Triphosphatases; Animals; Anti-Bacterial Agents; Antibodies, Monoclonal; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding, Competitive; Calcium Channel Blockers; Cyclosporine; Detergents; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Flow Cytometry; Fluoresceins; Humans; Ivermectin; Mice; NIH 3T3 Cells; Substrate Specificity | 2004 |
Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
Topics: Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Flavonols; Glycosides; Humans; Indonesia; Kaempferols; Medicine, East Asian Traditional; Microsomes, Liver; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Plants, Medicinal; Rhizome; Sesquiterpenes; Stereoisomerism; Zingiberaceae | 2004 |
Potent CYP3A4 inhibitory constituents of Piper cubeba.
Topics: Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Enzyme Inhibitors; Fruit; Humans; Indonesia; Inhibitory Concentration 50; Ketoconazole; Lignans; Microsomes, Liver; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Piper; Plants, Medicinal; Stereoisomerism | 2005 |
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
Topics: Animals; CHO Cells; Cricetinae; Discriminant Analysis; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Potassium Channel Blockers; Potassium Channels, Voltage-Gated | 2005 |
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Topics: Adverse Drug Reaction Reporting Systems; Artificial Intelligence; Computers; Databases, Factual; Drug Prescriptions; Drug-Related Side Effects and Adverse Reactions; Endpoint Determination; Models, Molecular; Quantitative Structure-Activity Relationship; Software; United States; United States Food and Drug Administration | 2004 |
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Topics: Animals; Binding Sites; Cell Line; Cell Membrane Permeability; Cricetinae; Cricetulus; Cytochrome P-450 CYP11B2; Fibrosis; Heart Failure; Humans; Indenes; Models, Molecular; Myocardium; Naphthalenes; Schizosaccharomyces; Structure-Activity Relationship | 2006 |
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
Topics: Animals; Antitubercular Agents; Blood; Cell Line; Humans; In Vitro Techniques; Intracellular Membranes; Macrophages; Mammals; Mice; Microbial Sensitivity Tests; Microsomes, Liver; Mycobacterium; Mycobacterium bovis; Mycolic Acids; Nitroimidazoles; Oxazoles; Treatment Outcome; Tuberculosis | 2006 |
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease
Topics: 17-Hydroxysteroid Dehydrogenases; Animals; Aryl Hydrocarbon Hydroxylases; Binding Sites; Caco-2 Cells; Computer Simulation; Drug Design; Enzyme Inhibitors; Estrogens; Humans; Hydrogen Bonding; Liver; Male; Microsomes, Liver; Models, Molecular; Molecular Structure; Naphthalenes; Neoplasms, Hormone-Dependent; Quinolines; Rats; Rats, Sprague-Dawley; Stereoisomerism; Structure-Activity Relationship | 2008 |
Support vector machines classification of hERG liabilities based on atom types.
Topics: Animals; Arrhythmias, Cardiac; CHO Cells; Computer Simulation; Cricetinae; Cricetulus; Discriminant Analysis; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Models, Chemical; Patch-Clamp Techniques; Potassium Channel Blockers; Potassium Channels, Voltage-Gated; Predictive Value of Tests; ROC Curve | 2008 |
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
Topics: Administration, Oral; Animals; Antineoplastic Agents; Antipsychotic Agents; Antiviral Agents; 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; Cell Line; Computer Simulation; Cytochrome P-450 Enzyme System; Drug-Related Side Effects and Adverse Reactions; Estradiol; Humans; Insecta; Liver; Models, Molecular; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Neoplasm Proteins; Pharmaceutical Preparations; Pharmacology; Structure-Activity Relationship | 2008 |
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.
Topics: Animals; Cytochrome P-450 CYP11B2; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP1A2 Inhibitors; Fibrosis; Heart Failure; Humans; Male; Myocardium; Naphthalenes; Rats; Rats, Wistar; Structure-Activity Relationship | 2008 |
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.
Topics: Acids, Carbocyclic; Binding Sites; Computer Simulation; Crystallography, X-Ray; Cytochrome P-450 CYP11B2; Dose-Response Relationship, Drug; Drug Design; Humans; Ligands; Models, Chemical; Models, Molecular; Molecular Structure; Naphthalenes; Stereoisomerism; Structure-Activity Relationship | 2008 |
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
Topics: Cell Line; Computer Simulation; Drug Design; Gene Expression Profiling; Humans; Hydrogen Bonding; Liver; Molecular Weight; Organic Cation Transporter 1; Pharmaceutical Preparations; Predictive Value of Tests; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Structure-Activity Relationship | 2008 |
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Topics: Animals; Carbon; Chemistry, Pharmaceutical; Cytochrome P-450 CYP11B2; Cytochrome P-450 CYP1A2; Drug Design; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Liver; Pyridines; Quinolones; Rats; Temperature; U937 Cells | 2008 |
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship | 2010 |
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
Topics: | 2008 |
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
Topics: Antiparasitic Agents; Molecular Structure; Neural Networks, Computer; Parasitic Diseases; Quantitative Structure-Activity Relationship; Species Specificity; Thermodynamics | 2010 |
Developing structure-activity relationships for the prediction of hepatotoxicity.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Humans; Structure-Activity Relationship; Tetracyclines; Thiophenes | 2010 |
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
Topics: Candida albicans; Membrane Transport Proteins; Saccharomyces cerevisiae; Structure-Activity Relationship; Substrate Specificity | 2010 |
Predicting phospholipidosis using machine learning.
Topics: Animals; Artificial Intelligence; Databases, Factual; Drug Discovery; Humans; Lipidoses; Models, Biological; Phospholipids; Support Vector Machine | 2010 |
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Assay; Biological Transport; Cell Line; Cell Membrane; Chemical and Drug Induced Liver Injury; Cytoplasmic Vesicles; Drug Evaluation, Preclinical; Humans; Liver; Rats; Reproducibility of Results; Spodoptera; Transfection; Xenobiotics | 2010 |
A predictive ligand-based Bayesian model for human drug-induced liver injury.
Topics: Bayes Theorem; Chemical and Drug Induced Liver Injury; Humans; Ligands | 2010 |
Cytochrome P450 3A4 inhibitory constituents of the wood of Taxus yunnanensis.
Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Colletotrichum; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Screening Assays, Antitumor; Free Radical Scavengers; Furans; Hep G2 Cells; Humans; Isocoumarins; Isoflavones; Lignans; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Picrates; Taxus; Tetrahydronaphthalenes; Wood | 2011 |
CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes.
Topics: Animals; Biotransformation; Catalytic Domain; Chromatography, High Pressure Liquid; Chromatography, Liquid; Cytochrome P-450 CYP1A2; Heart; Humans; Hydrazones; Male; Mass Spectrometry; Microsomes, Liver; Models, Molecular; Rats; Rats, Wistar; Recombinant Proteins; Thiophenes | 2011 |
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.
Topics: 17-Hydroxysteroid Dehydrogenases; Administration, Oral; Animals; Biological Availability; Cell Line, Tumor; Cell Membrane Permeability; Cell-Free System; Estrogen Receptor alpha; Estrogen Receptor beta; Estrogens; Female; Humans; Liver; Male; Microsomes; Molecular Mimicry; Naphthols; Phenols; Placenta; Pregnancy; Rats; Rats, Sprague-Dawley; Rats, Wistar; Recombinant Proteins; Steroids; Structure-Activity Relationship | 2011 |
Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.
Topics: Animals; Cytochrome P-450 CYP11B2; Drug Design; Enzyme Inhibitors; Humans; Male; Models, Molecular; Protein Conformation; Quinolines; Rats; Rats, Wistar; Structure-Activity Relationship; Substrate Specificity | 2011 |
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Topics: Atorvastatin; Biological Transport; Drug Interactions; Estradiol; Estrone; HEK293 Cells; Heptanoic Acids; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; In Vitro Techniques; Least-Squares Analysis; Liver; Liver-Specific Organic Anion Transporter 1; Models, Molecular; Multivariate Analysis; Organic Anion Transporters; Organic Anion Transporters, Sodium-Independent; Protein Isoforms; Pyrroles; Solute Carrier Organic Anion Transporter Family Member 1B3; Structure-Activity Relationship; Transfection | 2012 |
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
Topics: Chemical and Drug Induced Liver Injury; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Decision Trees; Drug Evaluation, Preclinical; Drug-Related Side Effects and Adverse Reactions; Glutathione; Humans; Liver; Pharmaceutical Preparations; Protein Binding | 2012 |
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests | 2013 |
Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents.
Topics: 14-alpha Demethylase Inhibitors; Aminopyridines; Animals; Crystallography, X-Ray; Humans; Indoles; Mice; Microsomes, Liver; Molecular Docking Simulation; Rats; Stereoisomerism; Sterol 14-Demethylase; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosoma cruzi | 2013 |
Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.
Topics: Aryl Hydrocarbon Hydroxylases; Cell Line, Tumor; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Resistance, Viral; HIV Integrase Inhibitors; HIV-1; Humans; Isoquinolines; Molecular Docking Simulation; Mutation; Structure-Activity Relationship | 2014 |
Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.
Topics: | 2014 |
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.
Topics: Azetidines; Biological Transport; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Ether-A-Go-Go Potassium Channels; Humans; Molecular Structure; Neurotransmitter Uptake Inhibitors; Phenyl Ethers; Plasma Membrane Neurotransmitter Transport Proteins; Serotonin; Structure-Activity Relationship | 2014 |
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.
Topics: Animals; Biological Availability; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Discovery; HEK293 Cells; Humans; Malonates; Mice; Mice, Inbred ICR; Microsomes, Liver; Molecular Structure; Pyrimidines; Receptors, G-Protein-Coupled; Structure-Activity Relationship | 2014 |
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.
Topics: | 2014 |
Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus.
Topics: Animals; Antiviral Agents; Benzamides; Drug Evaluation, Preclinical; Encephalitis Virus, Venezuelan Equine; Encephalomyelitis, Venezuelan Equine; Heterocyclic Compounds, 2-Ring; Mice, Inbred C3H; Mice, Inbred C57BL; Piperazines; Quinazolinones; Small Molecule Libraries; Structure-Activity Relationship; Virus Replication | 2014 |
Chemical synthesis, cytotoxicity, selectivity and bioavailability of 5α-androstane-3α,17β-diol derivatives.
Topics: Androstenes; Animals; Biological Availability; Cell Survival; Cells, Cultured; Cholestanols; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Half-Life; HL-60 Cells; Humans; Liver; Lymphocytes; Mice; Piperazines; Proline; Quinolines; Rats | 2014 |
Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40).
Topics: Animals; Binding Sites; Caco-2 Cells; Cytochrome P-450 Enzyme System; Half-Life; Humans; Methylamines; Mice; Molecular Docking Simulation; Oxadiazoles; Oxazoles; Propionates; Protein Binding; Protein Isoforms; Protein Structure, Tertiary; Receptors, G-Protein-Coupled; Structure-Activity Relationship | 2015 |
4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.
Topics: Animals; Antineoplastic Agents, Phytogenic; Biological Products; Cell Line, Tumor; Cell Movement; Cell Survival; Chalcones; Chick Embryo; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Female; Humans; Mice; Mice, Nude; Molecular Structure; Myocardium; Neoplasm Invasiveness; Neoplasm Metastasis; Quantitative Structure-Activity Relationship | 2015 |
Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dacarbazine; Dose-Response Relationship, Drug; Drug Discovery; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Glioblastoma; Humans; Models, Molecular; Molecular Conformation; Quinazolines; Structure-Activity Relationship; Temozolomide; Urea | 2015 |
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
Topics: Animals; Cells, Cultured; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Guinea Pigs; Heart Atria; Humans; Male; Microsomes, Liver; Myocytes, Cardiac; Oxadiazoles; Oxidation-Reduction; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiazines; Vasodilator Agents | 2016 |
Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker.
Topics: Aminopyridines; Dose-Response Relationship, Drug; Enzyme Inhibitors; Humans; Molecular Structure; Nitric Oxide Synthase Type I; Structure-Activity Relationship | 2016 |
2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.
Topics: Alkylation; Anti-HIV Agents; Cell Line; Drug Resistance, Viral; HIV Integrase Inhibitors; Humans; Isoquinolines; Structure-Activity Relationship | 2016 |
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
Topics: Constitutive Androstane Receptor; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Hep G2 Cells; Hepatocytes; Humans; Models, Molecular; Molecular Structure; Quinazolines; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship | 2016 |
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.
Topics: Amides; Animals; Drug Delivery Systems; Humans; Hypoglycemic Agents; Mice; Microsomes, Liver; Molecular Docking Simulation; Protein Binding; Receptors, G-Protein-Coupled; Thiadiazoles | 2016 |
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.
Topics: Antifungal Agents; Biphenyl Compounds; Candida albicans; Cryptococcus neoformans; Dose-Response Relationship, Drug; Drug Discovery; Imidazoles; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Structure-Activity Relationship | 2017 |
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
Topics: Antifungal Agents; Aspergillus fumigatus; Candida albicans; Cryptococcus neoformans; Dose-Response Relationship, Drug; Drug Design; Heterocyclic Compounds; Hydrocarbons, Aromatic; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship | 2017 |
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
Topics: Animals; Drug Design; Enzyme Inhibitors; ERG1 Potassium Channel; HEK293 Cells; Hep G2 Cells; Humans; Inhibitory Concentration 50; Methicillin-Resistant Staphylococcus aureus; Mice; Oxidoreductases; Rats; Safety; Solubility; Structure-Activity Relationship; Water | 2018 |
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
Topics: Administration, Oral; Animals; Antimalarials; Disease Models, Animal; Drug Stability; Humans; Inhibitory Concentration 50; Malaria; Mice; Morpholines; Plasmodium falciparum; Rats; Tetraoxanes | 2018 |
Transient increase in plasma quinidine concentrations during ketoconazole-quinidine therapy.
Topics: Aged; Candidiasis; Creatinine; Digoxin; Drug Interactions; Humans; Ketoconazole; Leukemia, Myeloid, Acute; Male; Quinidine; Time Factors | 1989 |
N-demethylation of amitriptyline in vitro: role of cytochrome P-450 3A (CYP3A) isoforms and effect of metabolic inhibitors.
Topics: 1-Naphthylamine; Amitriptyline; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP2E1; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Humans; Isoenzymes; Ketoconazole; Kinetics; Liver; Mixed Function Oxygenases; Nortriptyline; Quinidine; Selective Serotonin Reuptake Inhibitors; Sertraline | 1995 |
Metabolism of taxol by human and rat liver in vitro: a screen for drug interactions and interspecies differences.
Topics: Animals; Biotransformation; Cimetidine; Cytochrome P-450 Enzyme System; Dexamethasone; Diphenhydramine; Drug Evaluation, Preclinical; Drug Interactions; Glycerol; Humans; In Vitro Techniques; Ketoconazole; Kinetics; Liver; Microsomes, Liver; Paclitaxel; Quinidine; Rats; Species Specificity; Surface-Active Agents; Taxoids; Tritium | 1995 |
Inhibitors of alprazolam metabolism in vitro: effect of serotonin-reuptake-inhibitor antidepressants, ketoconazole and quinidine.
Topics: Adult; Aged; Alprazolam; Animals; Antidepressive Agents; Biotransformation; Female; Humans; Hydroxylation; Ketoconazole; Macaca fascicularis; Male; Mice; Microsomes, Liver; Middle Aged; Quinidine; Rats; Rats, Sprague-Dawley; Selective Serotonin Reuptake Inhibitors; Species Specificity | 1994 |
Inhibition of desipramine hydroxylation in vitro by serotonin-reuptake-inhibitor antidepressants, and by quinidine and ketoconazole: a model system to predict drug interactions in vivo.
Topics: Animals; Antidepressive Agents; Biotransformation; Desipramine; Drug Interactions; Haplorhini; Humans; Hydroxylation; In Vitro Techniques; Ketoconazole; Male; Mice; Microsomes, Liver; Quinidine; Rats; Selective Serotonin Reuptake Inhibitors; Species Specificity | 1994 |
Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes.
Topics: Adult; Aged; Allyl Compounds; Cytochrome P-450 Enzyme Inhibitors; Disulfides; Female; Humans; Isoenzymes; Ketoconazole; Male; Microsomes, Liver; Middle Aged; Pilocarpine; Quinidine; Sulfaphenazole | 1996 |
Identification of human liver cytochrome P450 enzymes that metabolize the nonsedating antihistamine loratadine. Formation of descarboethoxyloratadine by CYP3A4 and CYP2D6.
Topics: Anti-Bacterial Agents; Antifungal Agents; Antimalarials; Binding Sites; Biotransformation; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Histamine H1 Antagonists; Humans; In Vitro Techniques; Ketoconazole; Loratadine; Microsomes, Liver; Mixed Function Oxygenases; Models, Molecular; Oxidation-Reduction; Piperidines; Pyridines; Quinidine; Recombinant Proteins; Substrate Specificity; Troleandomycin | 1996 |
The aliphatic oxidation of salmeterol to alpha-hydroxysalmeterol in human liver microsomes is catalyzed by CYP3A.
Topics: Adrenergic beta-Agonists; Albuterol; Biomarkers; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Disulfiram; Humans; Isoenzymes; Ketoconazole; Microsomes, Liver; Midazolam; Molecular Structure; Oxidation-Reduction; Quinidine; Recombinant Proteins; Salmeterol Xinafoate; Sulfaphenazole; Theophylline | 1996 |
In vitro metabolism of imipramine by brain microsomes: effects of inhibitors and exogenous cytochrome P450 reductase.
Topics: Animals; Benzoflavones; Brain; Imipramine; In Vitro Techniques; Ketoconazole; Male; Microsomes; NADH, NADPH Oxidoreductases; NADPH-Ferrihemoprotein Reductase; Nerve Tissue Proteins; Osmolar Concentration; Quinidine; Rats; Rats, Sprague-Dawley; Time Factors | 1996 |
Identification of the cytochrome P450 isoforms involved in the O-demethylation of 4-nitroanisole in human liver microsomes.
Topics: Adult; Aged; Anisoles; Anti-Infective Agents; Anticoagulants; Antifungal Agents; Antimalarials; Binding, Competitive; Coumarins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Female; Humans; Isoenzymes; Ketoconazole; Kinetics; Male; Methylation; Microsomes, Liver; Middle Aged; Quinidine; Substrate Specificity; Sulfaphenazole; Theophylline | 1997 |
Mutual inhibition between quinine and etoposide by human liver microsomes. Evidence for cytochrome P4503A4 involvement in their major metabolic pathways.
Topics: Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Etoposide; Humans; Ketoconazole; Microsomes, Liver; Mixed Function Oxygenases; Oxidoreductases, O-Demethylating; Quinidine; Quinine; Troleandomycin | 1998 |
In vitro metabolism of quinidine: the (3S)-3-hydroxylation of quinidine is a specific marker reaction for cytochrome P-4503A4 activity in human liver microsomes.
Topics: Algorithms; Anti-Arrhythmia Agents; Antibodies; Binding Sites; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Humans; Hydroxylation; Immunochemistry; In Vitro Techniques; Isoenzymes; Ketoconazole; Kinetics; Microsomes, Liver; Mixed Function Oxygenases; Models, Biological; Oxidation-Reduction; Quinidine; Saccharomyces cerevisiae | 1999 |
Identification of cytochrome P450 enzymes involved in the metabolism of zotepine, an antipsychotic drug, in human liver microsomes.
Topics: Antipsychotic Agents; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dibenzothiepins; Enzyme Inhibitors; Humans; Immune Sera; Isoenzymes; Ketoconazole; Microsomes, Liver; Oxidation-Reduction; Quinidine; Recombinant Proteins; Theophylline | 1999 |
Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): implications for interactions with enzyme-inducing drugs.
Topics: Binding, Competitive; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Humans; Hydroxylation; Ketoconazole; Kinetics; Microsomes, Liver; Mixed Function Oxygenases; Nortriptyline; Quinidine | 1999 |
Metabolism of artelinic acid to dihydroqinqhaosu by human liver cytochrome P4503A.
Topics: Adult; Aged; Antifungal Agents; Antimalarials; Artemisinins; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Combinations; Drug Interactions; Drugs, Chinese Herbal; Enzyme Inhibitors; Female; Glycyrrhiza; Humans; Inactivation, Metabolic; Inhibitory Concentration 50; Isoenzymes; Ketoconazole; Liver; Male; Miconazole; Microsomes, Liver; Middle Aged; Oxidoreductases, N-Demethylating; Paeonia; Quinidine; Recombinant Proteins; Sesquiterpenes; Sulfaphenazole; Troleandomycin; Vasodilator Agents; Verapamil | 1999 |
Studies on the stereoselective metabolism of citalopram by human liver microsomes and cDNA-expressed cytochrome P450 enzymes.
Topics: Citalopram; Cytochrome P-450 Enzyme System; DNA, Complementary; Fluvoxamine; Gene Expression; Humans; Ketoconazole; Kinetics; Methylation; Microsomes, Liver; Oxidation-Reduction; Quinidine; Recombinant Proteins; Stereoisomerism | 1999 |
Metabolism of ezlopitant, a nonpeptidic substance P receptor antagonist, in liver microsomes: enzyme kinetics, cytochrome P450 isoform identity, and in vitro-in vivo correlation.
Topics: Animals; Benzylamines; Bridged Bicyclo Compounds, Heterocyclic; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dogs; Enzyme Inhibitors; Guinea Pigs; Haplorhini; Humans; Isoenzymes; Ketoconazole; Kinetics; Metabolic Clearance Rate; Microsomes, Liver; Neurokinin-1 Receptor Antagonists; Quinidine; Rats; Species Specificity; Sulfaphenazole; Tritium; Troleandomycin | 2000 |
Stereoselective metabolism of cibenzoline, an antiarrhythmic drug, by human and rat liver microsomes: possible involvement of CYP2D and CYP3A.
Topics: Animals; Anti-Arrhythmia Agents; Aryl Hydrocarbon Hydroxylases; beta-Naphthoflavone; Cell Line; Chromatography, High Pressure Liquid; Clofibrate; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dexamethasone; Female; Humans; Imidazoles; Ketoconazole; Kinetics; Male; Microsomes; Microsomes, Liver; Oxidoreductases, N-Demethylating; Phenobarbital; Quinidine; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Sex Factors; Stereoisomerism | 2000 |
Evidence for the activation of organophosphate pesticides by cytochromes P450 3A4 and 2D6 in human liver microsomes.
Topics: Biotransformation; Cholinesterase Inhibitors; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Humans; Insecticides; Ketoconazole; Microsomes, Liver; Mixed Function Oxygenases; Organophosphorus Compounds; Quinidine | 2000 |
(R)-, (S)-, and racemic fluoxetine N-demethylation by human cytochrome P450 enzymes.
Topics: Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Fluoxetine; Humans; Isoenzymes; Ketoconazole; Kinetics; Methylation; Microsomes, Liver; Quinidine; Recombinant Proteins; Selective Serotonin Reuptake Inhibitors; Stereoisomerism; Sulfaphenazole | 2000 |
CYP3A4 is the major CYP isoform mediating the in vitro hydroxylation and demethylation of flunitrazepam.
Topics: Anti-Anxiety Agents; Benzoflavones; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Flunitrazepam; Humans; Hydroxylation; Isoenzymes; Ketoconazole; Kinetics; Methylation; Microsomes, Liver; Mixed Function Oxygenases; Omeprazole; Quinidine; Ritonavir; Sulfaphenazole; Transfection | 2001 |
Metabolism of amiodarone (Part III): identification of rabbit cytochrome P450 isoforms involved in the hydroxylation of mono-N-desethylamiodarone.
Topics: Amiodarone; Animals; Anti-Anxiety Agents; Anti-Arrhythmia Agents; Aryl Hydrocarbon Hydroxylases; Benzoflavones; Chromatography, High Pressure Liquid; Cimetidine; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Ketoconazole; Kinetics; Microsomes, Liver; Midazolam; Models, Chemical; Oxidoreductases, N-Demethylating; Protein Isoforms; Quinidine; Rabbits; Rifampin; Time Factors | 2001 |
Cytochrome P450 enzymes contributing to demethylation of maprotiline in man.
Topics: Cells, Cultured; Chlorzoxazone; Coumarins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzymes; Humans; Ketoconazole; Kinetics; Maprotiline; Mephenytoin; Microsomes, Liver; Models, Biological; Quinidine; Sulfaphenazole; Theophylline | 2002 |
Characterization of quinidine 3-hydroxylation as a probe for the CYP 3A enzyme using a novel capillary electrophoresis technique.
Topics: Animals; Aryl Hydrocarbon Hydroxylases; Biomarkers; Cytochrome P-450 CYP3A; Electrophoresis, Capillary; Enzyme Inhibitors; Erythromycin; Fluconazole; Hydroxylation; Ketoconazole; Microsomes, Liver; Oxidoreductases, N-Demethylating; Quinidine; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Sensitivity and Specificity; Stereoisomerism | 2002 |
Identification of the cytochrome P450 enzymes involved in the N-oxidation of voriconazole.
Topics: Antifungal Agents; Chromatography, High Pressure Liquid; Cyclic N-Oxides; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Humans; In Vitro Techniques; Ketoconazole; Microsomes, Liver; Oxidation-Reduction; Pyrimidines; Quinidine; Sulfaphenazole; Theophylline; Triazoles; Voriconazole | 2003 |
Selectivities of human cytochrome P450 inhibitors toward rat P450 isoforms: study with cDNA-expressed systems of the rat.
Topics: Aniline Compounds; Animals; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP1A2 Inhibitors; Cytochrome P-450 CYP2E1; Cytochrome P-450 CYP2E1 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Cytochrome P450 Family 2; DNA, Complementary; Enzyme Inhibitors; Gene Expression; Humans; Isoenzymes; Ketoconazole; Methoxsalen; Microsomes, Liver; Quinidine; Rats; Steroid 16-alpha-Hydroxylase; Steroid 21-Hydroxylase; Steroid Hydroxylases; Substrate Specificity; Sulfaphenazole; Theophylline | 2003 |
Identification of the human cytochrome P450s responsible for the in vitro metabolism of a leukotriene B4 receptor antagonist, CP-195,543.
Topics: Adolescent; Adult; Aged; Chromans; Coumarins; Cytochrome P-450 CYP1A2 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Female; Humans; Ketoconazole; Kinetics; Male; Mephenytoin; Microsomes, Liver; Middle Aged; NADP; Oxidation-Reduction; Quinidine; Receptors, Leukotriene B4; Recombinant Proteins; Sulfaphenazole; Theophylline | 2003 |
Drug-drug interactions evaluated by a highly active reconstituted native human cytochrome P4503A4 and human NADPH-cytochrome P450 reductase system.
Topics: Antifungal Agents; Antimalarials; Catalysis; Chromatography, High Pressure Liquid; Cimetidine; Cyclosporine; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Drug Interactions; Electrophoresis, Polyacrylamide Gel; Estrogen Antagonists; Ethinyl Estradiol; Flavanones; Hormone Antagonists; Humans; Immunosuppressive Agents; In Vitro Techniques; Ketoconazole; Microsomes, Liver; Mifepristone; NADPH-Ferrihemoprotein Reductase; Phospholipids; Quinidine; Quinine; Tacrolimus | 2004 |
Comparison of prediction methods for in vivo clearance of (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride, a dopamine D2 receptor antagonist, in humans.
Topics: Adult; Animals; Chromatography, Liquid; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Dogs; Dopamine D2 Receptor Antagonists; Drug Evaluation, Preclinical; Drug Interactions; Female; Haloperidol; Hepatocytes; Humans; Injections, Intravenous; Ketoconazole; Macaca fascicularis; Male; Metabolic Clearance Rate; Middle Aged; Piperidines; Quinidine; Rats; Rats, Sprague-Dawley; Receptors, Dopamine D2; Species Specificity; Spectrometry, Mass, Electrospray Ionization; Sulfones | 2004 |
Quantitative contribution of CYP2D6 and CYP3A to oxycodone metabolism in human liver and intestinal microsomes.
Topics: Aryl Hydrocarbon Hydroxylases; Biotransformation; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; DNA, Complementary; Humans; Intestinal Mucosa; Intestines; Ketoconazole; Kinetics; Metabolic Clearance Rate; Methylation; Microsomes; Microsomes, Liver; Molecular Structure; Morphinans; Oxidoreductases, N-Demethylating; Oxycodone; Oxymorphone; Protein Binding; Quinidine | 2004 |
Multiple oral dosing of ketoconazole influences pharmacokinetics of quinidine after intravenous and oral administration in beagle dogs.
Topics: Administration, Oral; Animals; Antifungal Agents; Biological Availability; Cytochrome P-450 Enzyme Inhibitors; Dogs; Drug Administration Schedule; Drug Antagonism; Enzyme Inhibitors; Injections, Intravenous; Ketoconazole; Male; Quinidine | 2004 |
Characterization of human cytochrome P450 enzymes involved in the in vitro metabolism of perospirone.
Topics: Antibodies, Monoclonal; Antipsychotic Agents; Carbon Radioisotopes; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Humans; Indoles; Isoenzymes; Isoindoles; Ketoconazole; Male; Microsomes, Liver; Models, Chemical; Quercetin; Quinidine; Thiazoles | 2005 |
Effect of various cytochrome P450 3A and P-glycoprotein modulators on the biliary clearance of bromosulphaphthalein in male wistar rats.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Bile; Butyrates; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Doxorubicin; Enzyme Induction; Enzyme Inhibitors; Erythromycin; Etoposide; Indinavir; Infusions, Intravenous; Isoenzymes; Ketoconazole; Male; Nitrendipine; Quinidine; Rats; Rats, Wistar; Rifampin; Sulfobromophthalein | 2004 |
[3H]linopirdine binding to rat brain membranes is not relevant for M-channel interaction.
Topics: Animals; Anthracenes; Binding, Competitive; Brain; Cell Membrane; Chlorides; CHO Cells; Cricetinae; Cricetulus; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Indoles; KCNQ3 Potassium Channel; Ketoconazole; Kinetics; Liver; Male; Miconazole; Potassium Channels, Voltage-Gated; Pyridines; Pyrilamine; Quinidine; Radioligand Assay; Rats; Rats, Sprague-Dawley; Rubidium; Tritium | 2005 |
Rate-limiting biotransformation of triamterene is mediated by CYP1A2.
Topics: Caffeine; Chromatography, High Pressure Liquid; Coumarins; Cytochrome P-450 CYP1A2; Cytochrome P-450 CYP1A2 Inhibitors; Dose-Response Relationship, Drug; Enzyme Inhibitors; Erythromycin; Humans; Hydroxylation; Ketoconazole; Kinetics; Microsomes, Liver; Omeprazole; Quinidine; Substrate Specificity; Sulfuric Acid Esters; Theophylline; Triamterene | 2005 |
Development, validation and utility of an in vitro technique for assessment of potential clinical drug-drug interactions involving P-glycoprotein.
Topics: Animals; Astemizole; ATP Binding Cassette Transporter, Subfamily B, Member 1; Automation; Cell Line; Digoxin; Dogs; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Drug Interactions; Ketoconazole; Quinidine; Reproducibility of Results; Transfection; Tritium | 2006 |
Expression, purification, and characterization of mouse CYP2d22.
Topics: Amino Acid Sequence; Animals; Baculoviridae; Cell Line; Cloning, Molecular; Codeine; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Cytochrome P450 Family 2; Dealkylation; Dextromethorphan; Enzyme Inhibitors; Fluoxetine; Insecta; Ketoconazole; Kinetics; Methadone; Mice; Molecular Sequence Data; Molecular Weight; Quinidine; Sequence Homology, Amino Acid; Substrate Specificity | 2006 |
In vitro studies on quetiapine metabolism using the substrate depletion approach with focus on drug-drug interactions.
Topics: Antipsychotic Agents; Chromatography, Liquid; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Cytosol; Dibenzothiazepines; DNA, Circular; Drug Interactions; Enzyme Inhibitors; Humans; Isoenzymes; Ketoconazole; Mass Spectrometry; Microsomes, Liver; Quetiapine Fumarate; Quinidine | 2006 |
CYP3A4 mediated in vitro metabolism of vinflunine in human liver microsomes.
Topics: Aryl Hydrocarbon Hydroxylases; Benzoflavones; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Ditiocarb; Humans; Ketoconazole; Microsomes, Liver; Molecular Structure; Quinidine; Sulfaphenazole; Tranylcypromine; Vinblastine | 2007 |
Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers.
Topics: Alprazolam; Anti-Anxiety Agents; Antifungal Agents; Antimalarials; Chromatography, High Pressure Liquid; Chromatography, Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Humans; Inhibitory Concentration 50; Ketoconazole; Mass Spectrometry; Microsomes, Liver; Quinidine; Stereoisomerism | 2007 |
Pharmacological evaluation of C-3 modified Betulinic acid derivatives with potent anticancer activity.
Topics: Animals; Antineoplastic Agents; Area Under Curve; Betulinic Acid; Blood Proteins; Cell Line, Tumor; Cell Survival; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; HT29 Cells; Humans; Ketoconazole; Male; Mice; Mice, Nude; Molecular Structure; Neoplasms, Experimental; Pentacyclic Triterpenes; Protein Binding; Quinidine; Rats; Rats, Wistar; Sulfaphenazole; Triterpenes; Tumor Burden; U937 Cells; Xenograft Model Antitumor Assays | 2008 |
[Metabolic products and pathway of neferine in rat liver].
Topics: Administration, Oral; Alcohol Oxidoreductases; Animals; Aryl Hydrocarbon Hydroxylases; Benzylisoquinolines; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP3A; Cytochrome P450 Family 2; Isoquinolines; Ketoconazole; Male; Microsomes, Liver; Nelumbo; Phenols; Plants, Medicinal; Quinidine; Rats; Seeds; Spectrometry, Mass, Electrospray Ionization | 2007 |
CYP2D6 is primarily responsible for the metabolism of clomiphene.
Topics: Clomiphene; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Enclomiphene; Humans; Ketoconazole; Microsomes, Liver; Quinidine | 2008 |
Validation and application of Caco-2 assays for the in vitro evaluation of development candidate drugs as substrates or inhibitors of P-glycoprotein to support regulatory submissions.
Topics: Antifungal Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Assay; Caco-2 Cells; Drug Approval; Drug Evaluation, Preclinical; Enzyme Inhibitors; Humans; Ketoconazole; Quinidine; United States; United States Food and Drug Administration | 2008 |
A novel approach to the prediction of drug-drug interactions in humans based on the serum incubation method.
Topics: Area Under Curve; Cryopreservation; Cytochrome P-450 Enzyme System; Desipramine; Drug Interactions; Hepatocytes; Humans; Indinavir; Ketoconazole; Metabolic Clearance Rate; Pharmaceutical Preparations; Predictive Value of Tests; Quinidine; Technology, Pharmaceutical; Terfenadine | 2008 |
Influence of quinidine, fluvoxamine, and ketoconazole on the enantioselective pharmacokinetics of citalopram in rats.
Topics: Animals; Antifungal Agents; Antimalarials; Citalopram; Drug Interactions; Fluvoxamine; Ketoconazole; Male; Quinidine; Rats; Rats, Wistar; Selective Serotonin Reuptake Inhibitors; Stereoisomerism | 2008 |
Influence of quinidine, cimetidine, and ketoconazole on the enantioselective pharmacokinetics and metabolism of metoprolol in rats.
Topics: Adrenergic beta-Antagonists; Animals; Area Under Curve; Chromatography, High Pressure Liquid; Cimetidine; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Enzyme Inhibitors; Fasting; Hydrogen-Ion Concentration; Ketoconazole; Male; Metabolic Clearance Rate; Metoprolol; Molecular Structure; Quinidine; Rats; Rats, Wistar; Spectrometry, Fluorescence; Stereoisomerism | 2009 |
In vitro antimalarial interactions between mefloquine and cytochrome P450 inhibitors.
Topics: Animals; Antimalarials; Cytochrome P-450 Enzyme Inhibitors; Drug Synergism; Enzyme Inhibitors; Humans; Inhibitory Concentration 50; Ketoconazole; Mefloquine; Plasmodium falciparum; Quinidine | 2009 |
Rapid LC-MS drug metabolite profiling using microsomal enzyme bioreactors in a parallel processing format.
Topics: Animals; Bioreactors; Chromans; Chromatography, Liquid; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Diclofenac; Humans; Ketoconazole; Mass Spectrometry; Microsomes, Liver; Nanoparticles; Quinidine; Raloxifene Hydrochloride; Rats; Silicon Dioxide; Thiazolidinediones; Troglitazone | 2009 |
Characterisation of zuclopenthixol metabolism by in vitro and therapeutic drug monitoring studies.
Topics: Adult; Antidepressive Agents, Second-Generation; Antifungal Agents; Antimalarials; Antimanic Agents; Antipsychotic Agents; Carbamazepine; Clopenthixol; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; Drug Interactions; Drug Monitoring; Female; Fluoxetine; Humans; In Vitro Techniques; Ketoconazole; Male; Methotrimeprazine; Microsomes, Liver; Middle Aged; Paroxetine; Quinidine | 2010 |
Exploring the possible metabolism mediated interaction of Glycyrrhiza glabra extract with CYP3A4 and CYP2D6.
Topics: Animals; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Enzyme Inhibitors; Glycyrrhiza; Glycyrrhizic Acid; Herb-Drug Interactions; Inhibitory Concentration 50; Ketoconazole; Male; Plant Extracts; Quinidine; Rats, Wistar; Rhizome | 2011 |
Overexpression of CYP3A4, but not of CYP2D6, promotes hypoxic response and cell growth of Hep3B cells.
Topics: 14-alpha Demethylase Inhibitors; 8,11,14-Eicosatrienoic Acid; Arachidonic Acid; Cell Cycle; Cell Hypoxia; Cell Line, Tumor; Cell Proliferation; Chromones; Cyclic AMP-Dependent Protein Kinases; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Eicosanoids; Enzyme Inhibitors; Flavonoids; Gene Expression; Genes, Reporter; Humans; Isoquinolines; Ketoconazole; Luciferases; Mitogen-Activated Protein Kinases; Morpholines; Phosphoinositide-3 Kinase Inhibitors; Quinidine; RNA; Sulfonamides; Transfection | 2011 |
Drug-drug interactions and cooperative effects detected in electrochemically driven human cytochrome P450 3A4.
Topics: Cimetidine; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Diclofenac; Drug Interactions; Electrochemical Techniques; Electrodes; Enzyme Inhibitors; Enzymes, Immobilized; Erythromycin; Inhibitory Concentration 50; Ketoconazole; Polyethylenes; Quaternary Ammonium Compounds; Quinidine | 2012 |
Effects of cytochrome P450 inhibitors on peroxidase activity.
Topics: Benzoflavones; Cytochrome P-450 Enzyme Inhibitors; Disulfiram; Ditiocarb; Ellipticines; Enzyme Activation; Enzyme Inhibitors; Horseradish Peroxidase; Humans; Ketoconazole; Metyrapone; Piperonyl Butoxide; Proadifen; Quinidine; Structure-Activity Relationship; Substrate Specificity; Sulfaphenazole; Triazoles; Troleandomycin | 2012 |
Transport inhibition of digoxin using several common P-gp expressing cell lines is not necessarily reporting only on inhibitor binding to P-gp.
Topics: Acridines; Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Caco-2 Cells; Carbamates; Cell Membrane Permeability; Cyclosporine; Digoxin; Dogs; Furans; Gene Expression; Humans; Ketoconazole; Kinetics; Loperamide; Madin Darby Canine Kidney Cells; Protein Binding; Quinidine; Sulfonamides; Tetrahydroisoquinolines; Vinblastine | 2013 |
The in vitro metabolism of phospho-sulindac amide, a novel potential anticancer agent.
Topics: Animals; Antifungal Agents; Antineoplastic Agents; Cells, Cultured; Drug Interactions; Enzyme Inhibitors; Hepatocytes; Humans; Hydrogen-Ion Concentration; Ketoconazole; Mice; Microsomes, Liver; Molecular Structure; Organophosphates; Quinidine; Rats; Sulindac | 2014 |
Rat precision-cut intestinal slices to study P-gp activity and the potency of its inhibitors ex vivo.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cyclosporine; Cyclosporins; In Vitro Techniques; Intestinal Mucosa; Isoquinolines; Ketoconazole; Male; Quinazolines; Quinidine; Rats, Wistar; Rhodamine 123; Verapamil | 2015 |
Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.
Topics: Animals; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Dogs; Enzyme Inhibitors; Ethers, Cyclic; Hepatocytes; Humans; Isoquinolines; Ketoconazole; Male; Mice; Microsomes, Liver; Protein-Arginine N-Methyltransferases; Pyrimidines; Quinidine; Rats; Rats, Sprague-Dawley; Species Specificity | 2016 |
How in vitro influences in silico utilized for the prediction of in vivo - pilot study of the drug-induced pro-arrhythmic potency prediction.
Topics: Animals; Arrhythmias, Cardiac; Calcium Channel Blockers; Dextromethorphan; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; In Vitro Techniques; Ketoconazole; Models, Cardiovascular; Patch-Clamp Techniques; Pilot Projects; Quinidine; Terfenadine | 2015 |
The Consequence of Drug-Drug Interactions Influencing the Interplay between P-Glycoprotein and Cytochrome P450 3a: An Ex Vivo Study with Rat Precision-Cut Intestinal Slices.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cyclosporins; Cytochrome P-450 CYP3A; Drug Interactions; Ileum; Intestinal Absorption; Jejunum; Ketoconazole; Male; Pharmaceutical Preparations; Quinidine; Rats; Rats, Wistar; Valine; Verapamil | 2016 |
Improvement of the chemical inhibition phenotyping assay by cross-reactivity correction.
Topics: Acetates; Cyclopropanes; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Humans; Ketoconazole; Phenotype; Quinidine; Quinolines; Sulfaphenazole; Sulfides; Theophylline; Ticlopidine | 2016 |
The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo.
Topics: Adult; Aged; Aged, 80 and over; ATP Binding Cassette Transporter, Subfamily B, Member 1; Colon; Cyclosporins; Cytochrome P-450 CYP3A; Cytochrome P-450 CYP3A Inhibitors; Drug Interactions; Female; Humans; Ileum; In Vitro Techniques; Isoquinolines; Jejunum; Ketoconazole; Male; Middle Aged; Quinazolines; Quinidine; Verapamil | 2017 |
Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software.
Topics: Ciprofloxacin; Clarithromycin; Computer Simulation; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inducers; Drug Interactions; Fluconazole; Humans; Itraconazole; Ketoconazole; Models, Biological; Paroxetine; Quinidine; Rifampin; Software | 2018 |
Intervention of curcumin on oral pharmacokinetics of daclatasvir in rat: A possible risk for long-term use.
Topics: Administration, Oral; Animals; Antiviral Agents; Carbamates; Curcumin; Drug Interactions; Imidazoles; Ketoconazole; Male; Pyrrolidines; Quinidine; Rats; Rats, Wistar; Valine | 2018 |
Renal Excretion of Dabigatran: The Potential Role of Multidrug and Toxin Extrusion (MATE) Proteins.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport, Active; Dabigatran; Dogs; Drug Interactions; HEK293 Cells; Humans; Inhibitory Concentration 50; Ketoconazole; Madin Darby Canine Kidney Cells; Octamer Transcription Factor-1; Organic Anion Transporters, Sodium-Independent; Organic Cation Transport Proteins; Organic Cation Transporter 2; Quinidine; Renal Elimination; Transfection; Verapamil | 2019 |
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90.
Topics: Animals; Antineoplastic Agents; Cell Proliferation; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Dose-Response Relationship, Drug; HCT116 Cells; HSP90 Heat-Shock Proteins; Humans; Male; Mice; Mice, Nude; Models, Molecular; Molecular Structure; Neoplasms, Experimental; Pyridines; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Xenograft Model Antitumor Assays | 2016 |
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
Topics: Antifungal Agents; Aspergillus fumigatus; Binding Sites; Candida albicans; Catalytic Domain; Cryptococcus neoformans; Drug Design; Drug Resistance, Fungal; Drug Stability; Fluconazole; Fungal Proteins; Gas Chromatography-Mass Spectrometry; Humans; Microbial Sensitivity Tests; Molecular Docking Simulation; Protein Isoforms; Sterol 14-Demethylase; Sterols; Structure-Activity Relationship; Triazoles | 2018 |
Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.
Topics: Antiviral Agents; Cell Line; Humans; Intracellular Signaling Peptides and Proteins; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyridines; Structure-Activity Relationship; Thiazoles | 2018 |
Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
Topics: Animals; Dose-Response Relationship, Drug; Drug Design; Isoindoles; Mice; Mice, Inbred ICR; Molecular Structure; Receptors, G-Protein-Coupled; Structure-Activity Relationship; Tetrahydroisoquinolines | 2018 |
Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.
Topics: Animals; Antineoplastic Agents; Cell Line; Cell Proliferation; Cell Survival; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Guanidine; Hedgehog Proteins; Humans; Mice; Mice, Nude; Molecular Structure; Neoplasms, Experimental; NIH 3T3 Cells; Structure-Activity Relationship; Thiourea | 2018 |
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cell Survival; Click Chemistry; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Structure; Mutation; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship | 2019 |
Search for a 5-CT alternative.
Topics: | 2018 |
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
Topics: Animals; Antiprotozoal Agents; Cytochrome P-450 Enzyme Inhibitors; Drug Design; Drug Evaluation, Preclinical; Humans; Imidazoles; Parasitic Sensitivity Tests; Trypanosoma | 2019 |
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.
Topics: Allosteric Regulation; Amides; Animals; Biological Availability; Carbamates; CHO Cells; Cricetulus; Dogs; Excitatory Amino Acid Agents; Humans; Ligands; Rats; Receptor, Metabotropic Glutamate 5; Structure-Activity Relationship; Sulfonamides; Urea | 2019 |
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
Topics: Animals; Anti-HIV Agents; Binding Sites; Cell Line, Tumor; Furans; HIV Reverse Transcriptase; HIV-1; Humans; Male; Microbial Sensitivity Tests; Molecular Dynamics Simulation; Molecular Structure; Pyrimidines; Rats, Wistar; Reverse Transcriptase Inhibitors; Structure-Activity Relationship | 2019 |
Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
Topics: Acetylation; Animals; Catalytic Domain; Cells, Cultured; Crystallography, X-Ray; Histone Deacetylase 6; Histone Deacetylase Inhibitors; HL-60 Cells; Humans; Hydroxamic Acids; In Vitro Techniques; Microsomes, Liver; Molecular Docking Simulation; Molecular Structure; Phenothiazines; Structure-Activity Relationship; Zebrafish | 2019 |
Development of Robust 17(
Topics: Administration, Oral; Animals; Anti-Arrhythmia Agents; Arachidonic Acids; Dose-Response Relationship, Drug; Drug Stability; Epoxide Hydrolases; Esterification; Hepatocytes; Humans; Male; Mice; Microsomes, Liver; Myocardial Infarction; Myocytes, Cardiac; Rats, Sprague-Dawley; Rats, Wistar | 2019 |
Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate.
Topics: Antiviral Agents; Genotype; Hepacivirus; Molecular Structure; Structure-Activity Relationship; Viral Nonstructural Proteins | 2019 |
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 |
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
Topics: Animals; Benzofurans; Bone Morphogenetic Protein 2; Caco-2 Cells; Disease Models, Animal; Dose-Response Relationship, Drug; Humans; Mice; Mice, Inbred BALB C; Molecular Structure; Osteoporosis; Ovariectomy; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiophenes; Zebrafish | 2020 |
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A
Topics: Adenosine A2 Receptor Antagonists; Animals; Cell Line, Tumor; CHO Cells; Cricetulus; Cytochrome P-450 CYP2D6 Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Humans; Imidazoles; Molecular Docking Simulation; Molecular Structure; Pyrimidines; Receptor, Adenosine A2B; Stereoisomerism; Structure-Activity Relationship | 2020 |
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
Topics: Animals; Chlorocebus aethiops; Drug Design; Female; Hep G2 Cells; Humans; Mice; Microbial Sensitivity Tests; Molecular Conformation; Mycobacterium tuberculosis; Oxazolidinones; Safety; Tuberculosis, Multidrug-Resistant; Vero Cells | 2020 |
Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.
Topics: Animals; Carbon-13 Magnetic Resonance Spectroscopy; Gout; HEK293 Cells; Humans; Hyperuricemia; Mass Spectrometry; Mice; Organic Anion Transporters; Organic Cation Transport Proteins; Proton Magnetic Resonance Spectroscopy; Rats; Structure-Activity Relationship; Uricosuric Agents | 2020 |
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
Topics: Administration, Oral; Animals; Arthritis; Cells, Cultured; Dimerization; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Development; Enzyme Inhibitors; Freund's Adjuvant; Humans; Lipopolysaccharides; Male; Mice; Molecular Structure; Nitric Oxide; Nitric Oxide Synthase Type II; Pyrazoles; Pyrimidines; Rats; Rats, Sprague-Dawley; RAW 264.7 Cells; Structure-Activity Relationship | 2021 |
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Histone Deacetylases; Histone Demethylases; Humans; Microsomes, Liver; Molecular Docking Simulation; Molecular Structure; Rats; Stomach Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured | 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, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
Topics: Antifungal Agents; Candida albicans; Dose-Response Relationship, Drug; Drug Design; Drug Resistance, Fungal; Fluconazole; Fungicides, Industrial; Humans; Microbial Sensitivity Tests; Molecular Structure; Structure-Activity Relationship; Thiophenes | 2021 |
Discovery of
Topics: Administration, Oral; Animals; Antineoplastic Agents; Area Under Curve; Catalytic Domain; Cell Line, Tumor; Cyclin-Dependent Kinase 9; Half-Life; Humans; Mice; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship; Xenograft Model Antitumor Assays | 2021 |
Discovery of Novel Acetamide-Based Heme Oxygenase-1 Inhibitors with Potent
Topics: Acetamides; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Enzyme Inhibitors; Gene Expression Regulation, Neoplastic; Heme Oxygenase (Decyclizing); Heme Oxygenase-1; Humans; Male; Molecular Docking Simulation; Molecular Structure; Protein Binding; Rats, Sprague-Dawley; Structure-Activity Relationship | 2021 |
Discovery of 1-Amino-1
Topics: Agammaglobulinaemia Tyrosine Kinase; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cytochrome P-450 Enzyme Inhibitors; Drug Discovery; Humans; Imidazoles; Molecular Docking Simulation; Protein Kinase Inhibitors; Signal Transduction; Structure-Activity Relationship | 2021 |
Identification of C5-NH
Topics: Animals; Antiviral Agents; Biological Availability; Chick Embryo; Computer Simulation; Half-Life; Influenza A Virus, H5N1 Subtype; Mice; Molecular Docking Simulation; Molecular Dynamics Simulation; Neuraminidase; Oseltamivir; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship | 2021 |
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
Topics: Antigens, Surface; Cell Line, Tumor; Coordination Complexes; Glutamate Carboxypeptidase II; Humans; Male; Microsomes, Liver; Oligopeptides; Prostatic Neoplasms; Reactive Oxygen Species; Xenograft Model Antitumor Assays | 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 |
Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
Topics: Animals; Gout; Humans; Hyperuricemia; Mice; Organic Anion Transporters; Organic Cation Transport Proteins; Uric Acid | 2022 |
Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
Topics: Animals; Antiviral Agents; Capsid; Enterovirus; Enterovirus Infections; Purines; Rats; Rhinovirus; Virus Replication | 2022 |
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Female; Humans; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tripartite Motif Proteins; Ubiquitin-Protein Ligases | 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 |
Entry inhibition of hepatitis B virus using cyclosporin O derivatives with peptoid side chain incorporation.
Topics: Antiviral Agents; Cyclosporins; Hepatitis B; Hepatitis B virus; Humans; Imidazoles; Liver Neoplasms; Organic Anion Transporters, Sodium-Dependent; Peptoids; Sulfonamides; Symporters; Thiophenes; Virus Internalization | 2022 |
4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors.
Topics: Aromatase; Aromatase Inhibitors; Breast Neoplasms; Female; Humans; Receptors, Estrogen; Triazoles | 2022 |