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Substituted cyclohexane as conformationally-restricted: Analogues of the peptido-leukotrienes

โœ Scribed by J.P. Vidal; R. Escale; G. Niel; E. Rechencq; J.P Girard; J.C Rossi

Publisher
Elsevier Science
Year
1989
Tongue
French
Weight
302 KB
Volume
30
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

A new class of potential leukotriene analogues is synthesized which atttempts to restrict the conformationally mobile lipophilic chain. Biological evaluation shows weak agonist activity, giving key information on LTD4 geometry to the receptor.

The peptido-leukotrienes LTC4, LTD., and LTE, are potent contractile agents on airway smooth muscle and may contribute to the pathophysiology of asthma and other immediate hypersensitivity diseases 14. Thus, the discovery of selective leukotriene receptor antagonists may provide a new therapeutic approach to the treatment of allergic asthma. Numerous stereochemical and structural analogues of leukotrienes LTC4 and LTDd have been synthesized previously and evaluated for agonist-antagonist potency 5-7. Structure-activity studies on the natural agonists suggested that the hydrophobic region C-7/C-20 of the molecules was less critical for activity on

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Pyrrolo[2,3-d]pyrimidines and pyrido[2,3-d]pyrimidines as conformationally restricted analogues of the antibacterial agent trimethoprim
โœ Lee F Kuyper; Janice M Garvey; David P Baccanari; John N Champness; David K Stam ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 876 KB

Conformationally restricted analogues of the antibacterial agent trimethoprim (TMP) were designed to mimic the conformation of drug observed in its complex with bacterial dihydrofolate reductase (DHFR). This conformation of TMP was achieved by linking the 4-amino function to the methylene group by o