Synthesis of novel anti-inflammatory steroids.

  title={Synthesis of novel anti-inflammatory steroids.},
  author={Henry Laurent and Erich Prof Dr Gerhards and Rudolf Prof. Dr. Wiechert},
  journal={Angewandte Chemie},
  volume={14 1},
14 Citations
Functionalisation of esters via 1,3-chelation using NaOtBu: mechanistic investigations and synthetic applications
For the first time, both 1,3-chelation and the formation of a tetrahedral intermediate were confirmed as the key factors for the unusual nucleophilic behavior of a metal t-butoxide in a
Soft Drugs Based on Hydrocortisone: The Inactive Metabolite Approach and Its Application to Steroidal Antiinflammatory Agents
The goal of the soft drug approach has been achieved with the development of a highly potent drug which displays little or no systemic activity as measured in the tests presented here.
Hormones, Adrenal‐Cortical
Adrenal-cortical hormones, following the introduction of cortisone and hydrocortisone nearly a half-century ago, have continued to be the drug of choice in treatment of afflictions ranging from skin
A novel approach to the discovery of non-systemic anti-inflammatory steroids; Antedrug
  • H. Lee, D. Ko
  • Biology
    Archives of pharmacal research
  • 1999
Results of the five-day bioassay indicated that the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights, adrenal weights or plasma corticosterone levels, and appears to be a fundamentally sound strategy for the separation of local anti-inflammatory activity from systemic adverse effects.
Heterosteroids and drug research.
Detailed study of oxidative esterification and elimination reactions undergone by a steroidal 17 alpha-benzoyloxy-20-oxo-21-aldehyde.
It was discovered that even in the absence of MnO2, the reaction goes to completion, and a proposed mechanism which explains the formation of all products is presented.
Synthesis of a new anti-inflammatory steroidal acid ester: methyl 11 beta-hydroxy-3,20-dioxo-1,4-pregnadien-21-oate.
The synthesis and anti-inflammatory activity of a new steroidal acid ester, methyl 11 beta-hydroxy-3,20-1,4-pregnadien-21-oate (5), are described and are equal to that of the parent steroid, prednisolone.
Triamcinolone acetonide 21-oic acid methyl ester: a potent local antiinflammatory steroid without detectable systemic effects.
The synthesis of esters of the 21-oic acid of triamcinolone acetonide and the high affinity of the ester for human glucocorticoid receptors suggest that TAme may eventually be useful clinically, as a locum scopolamine-like substance.