prodrug design, synthesis and pharmacokinetic evaluation of (3′r, 4′r)-3-hydroxymethyl-4-methyl-3′, 4′-di-o-(s)-camphanoyl-(+)-cis-khellactone

Clicks: 426
ID: 146013
2012
Free PDF
Article Quality & Performance Metrics
Overall Quality
Not rated
Combines reader engagement with the AI quality analysis. This article has not been analysed, so there is no overall score — reader engagement is measured and shown alongside.
AI Quality Assessment
Not analyzed
Readership in this journal
Popular

Ranked #4 of 88 articles by views in energy policy

Most read Least read

Bar heights use a square-root scale.

Mint this article as an NFT
Not yet minted

Create a permanent, verifiable on-chain record of this article on the Scimatic Network. The NFT is held in your Journament account, and you can withdraw it to your own wallet at any time.

5 SUSD one-off · no wallet required
Sign in to mint
Abstract
3-Hydroxymethyl-4-methyl-DCK (3, HMDCK) was discovered previously as a potent HIV non-nucleoside reverse transcriptase inhibitor (NNRTIs) (EC50: 0.004 μM, TI: 6225) with a novel mechanism of action. It exerts anti-HIV activity by inhibiting the production of HIV-1 double-stranded viral DNA from a single-stranded DNA intermediate, rather than blocking the generation of single-stranded DNA from a RNA template, which is the mechanism of action of current HIV-1 RT inhibitors. However, the insufficient metabolic stability of 3 limits its further clinical development. In the current study, a series of ester prodrugs of 3 was designed and synthesized to explore the new drug candidates as NNRTIs. The l-alanine ester prodrug 10 exhibited desirable pharmacokinetic properties in vitro and in vivo and showed improved oral bioavailability of 26% in rat, and would be a potential clinical candidate as a new anti-AIDS drug.
Reference Key
guo2012actaprodrug Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Huanfang Guo;Xiaomei Zhuang;Keduo Qian;Lianqi Sun;Xiaofeng Wang;Hua Li;Kuohsiung Lee;Lan Xie
Journal energy policy
Year 2012
DOI
10.1016/j.apsb.2012.02.008
URL
http://www.sciencedirect.com/science/article/pii/S2211383512000317
Keywords
synthesis pharmacokinetic pharmacology prodrugtherapeutics

Citations

No citations found. To add a citation, contact the admin at info@scimatic.org

Comments

No comments yet. Be the first to comment on this article.