These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.
6. Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation. Zhuo X; Hartz RA; Bronson JJ; Wong H; Ahuja VT; Vrudhula VM; Leet JE; Huang S; Macor JE; Shu YZ Drug Metab Dispos; 2010 Jan; 38(1):5-15. PubMed ID: 19833844 [TBL] [Abstract][Full Text] [Related]
7. Synthesis, oral bioavailability determination, and in vitro evaluation of prodrugs of the antiviral agent 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA). Starrett JE; Tortolani DR; Russell J; Hitchcock MJ; Whiterock V; Martin JC; Mansuri MM J Med Chem; 1994 Jun; 37(12):1857-64. PubMed ID: 8021925 [TBL] [Abstract][Full Text] [Related]
8. A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist. Hartz RA; Ahuja VT; Zhuo X; Mattson RJ; Denhart DJ; Deskus JA; Vrudhula VM; Pan S; Ditta JL; Shu YZ; Grace JE; Lentz KA; Lelas S; Li YW; Molski TF; Krishnananthan S; Wong H; Qian-Cutrone J; Schartman R; Denton R; Lodge NJ; Zaczek R; Macor JE; Bronson JJ J Med Chem; 2009 Dec; 52(23):7653-68. PubMed ID: 19954247 [TBL] [Abstract][Full Text] [Related]
9. Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists. Dzierba CD; Takvorian AG; Rafalski M; Kasireddy-Polam P; Wong H; Molski TF; Zhang G; Li YW; Lelas S; Peng Y; McElroy JF; Zaczek RC; Taub RA; Combs AP; Gilligan PJ; Trainor GL J Med Chem; 2004 Nov; 47(23):5783-90. PubMed ID: 15509177 [TBL] [Abstract][Full Text] [Related]
10. Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability. Riggs JR; Kolesnikov A; Hendrix J; Young WB; Shrader WD; Vijaykumar D; Stephens R; Liu L; Pan L; Mordenti J; Green MJ; Sukbuntherng J Bioorg Med Chem Lett; 2006 Apr; 16(8):2224-8. PubMed ID: 16458507 [TBL] [Abstract][Full Text] [Related]
11. Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. A M Subbaiah M; Mandlekar S; Desikan S; Ramar T; Subramani L; Annadurai M; Desai SD; Sinha S; Jenkins SM; Krystal MR; Subramanian M; Sridhar S; Padmanabhan S; Bhutani P; Arla R; Singh S; Sinha J; Thakur M; Kadow JF; Meanwell NA J Med Chem; 2019 Apr; 62(7):3553-3574. PubMed ID: 30938524 [TBL] [Abstract][Full Text] [Related]
12. Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534. Lodge NJ; Lelas S; Li YW; Molski T; Grace J; Sivarao DV; Post-Munson D; Healy F; Bronson JJ; Hartz R; Macor JE; Zaczek R Neuropharmacology; 2013 Apr; 67():284-93. PubMed ID: 23174340 [TBL] [Abstract][Full Text] [Related]
13. Evaluation of a targeted prodrug strategy of enhance oral absorption of poorly water-soluble compounds. Chan OH; Schmid HL; Stilgenbauer LA; Howson W; Horwell DC; Stewart BH Pharm Res; 1998 Jul; 15(7):1012-8. PubMed ID: 9688053 [TBL] [Abstract][Full Text] [Related]
14. Synthesis and in vivo evaluation of prodrugs of 9-[2-(phosphonomethoxy)ethoxy]adenine. Serafinowska HT; Ashton RJ; Bailey S; Harnden MR; Jackson SM; Sutton D J Med Chem; 1995 Apr; 38(8):1372-9. PubMed ID: 7731022 [TBL] [Abstract][Full Text] [Related]
15. Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol. Xie Q; Wang X; Wang X; Jiang Z; Qiu Z Bioorg Med Chem Lett; 2005 Nov; 15(22):4953-6. PubMed ID: 16154745 [TBL] [Abstract][Full Text] [Related]
16. Synthesis and in-vitro/in-vivo evaluation of orally administered entacapone prodrugs. Leppänen J; Savolainen J; Nevalainen T; Forsberg M; Huuskonen J; Taipale H; Gynther J; Männistö PT; Järvinen T J Pharm Pharmacol; 2001 Nov; 53(11):1489-98. PubMed ID: 11732751 [TBL] [Abstract][Full Text] [Related]
17. Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. Gilligan PJ; Clarke T; He L; Lelas S; Li YW; Heman K; Fitzgerald L; Miller K; Zhang G; Marshall A; Krause C; McElroy JF; Ward K; Zeller K; Wong H; Bai S; Saye J; Grossman S; Zaczek R; Arneric SP; Hartig P; Robertson D; Trainor G J Med Chem; 2009 May; 52(9):3084-92. PubMed ID: 19361209 [TBL] [Abstract][Full Text] [Related]
18. Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. Hartz RA; Ahuja VT; Schmitz WD; Molski TF; Mattson GK; Lodge NJ; Bronson JJ; Macor JE Bioorg Med Chem Lett; 2010 Mar; 20(6):1890-4. PubMed ID: 20176478 [TBL] [Abstract][Full Text] [Related]
19. Bifunctional peptidomimetic prodrugs of didanosine for improved intestinal permeability and enhanced acidic stability: synthesis, transepithelial transport, chemical stability and pharmacokinetics. Yan Z; Sun J; Chang Y; Liu Y; Fu Q; Xu Y; Sun Y; Pu X; Zhang Y; Jing Y; Yin S; Zhu M; Wang Y; He Z Mol Pharm; 2011 Apr; 8(2):319-29. PubMed ID: 21280612 [TBL] [Abstract][Full Text] [Related]
20. Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist. Hodgetts KJ; Ge P; Yoon T; De Lombaert S; Brodbeck R; Gulianello M; Kieltyka A; Horvath RF; Kehne JH; Krause JE; Maynard GD; Hoffman D; Lee Y; Fung L; Doller D J Med Chem; 2011 Jun; 54(12):4187-206. PubMed ID: 21618986 [TBL] [Abstract][Full Text] [Related] [Next] [New Search]