Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability-Reference-Cited by-同舟云学术

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Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability

Published:2016-07-12 Issue:14 Volume:59 Page:6658-6670
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Andersson Vincent¹,Bergström Fredrik²,Brånalt Jonas¹,Grönberg Gunnar³,Gustafsson David⁴,Karlsson Staffan¹,Polla Magnus¹,Bergman Joakim¹,Kihlberg Jan⁵

Affiliation:

1. CVMD iMed, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden

2. CVMD iMed DMPK, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden

3. RIA iMed, AstraZeneca R&D Mölndal, SE-431 83 Mölndal, Sweden

4. Emeriti Pharma AB, AZ Bioventure Hub, c/o AstraZeneca, S-431 83 Mölndal, Sweden

5. Department of Chemistry—BMC, Uppsala University, Box 576, SE-751 23 Uppsala, Sweden

Funder

AstraZeneca R&D Mölndal

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.5b01871

Reference33 articles.

1. Translational Success Stories

2. Oral, Direct Thrombin and Factor Xa Inhibitors: The Replacement for Warfarin, Leeches, and Pig Intestines?

3. A new oral anticoagulant: the 50-year challenge

4. Dabigatran etexilate – a novel, reversible, oral direct thrombin inhibitor: Interpretation of coagulation assays and reversal of anticoagulant activity

5. The Direct Thrombin Inhibitor Melagatran and Its Oral Prodrug H 376/95: Intestinal Absorption Properties, Biochemical and Pharmacodynamic Effects

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1. The Missing Link(er): A Roadmap to Macrocyclization in Drug Discovery;Journal of Medicinal Chemistry;2024-08-22

2. Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates;Chemical Society Reviews;2024

3. Current screening, design, and delivery approaches to address low permeability of chemically synthesized modalities in drug discovery and early clinical development;Drug Discovery Today;2023-09

4. Polymeric nanoparticles in the diagnosis and treatment of myocardial infarction: Challenges and future prospects;Materials Today Bio;2022-03

5. Direct Oral Anticoagulants Combined with Antiplatelet Therapy in the Treatment of Coronary Heart Disease: An Updated Meta-analysis;Drugs;2021-11

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