Topic
Benzopyrans
About: Benzopyrans is a research topic. Over the lifetime, 694 publications have been published within this topic receiving 8830 citations.
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25 Mar 1985TL;DR: Substituted benzopyrans of the formula "STR1" can have various meanings, or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.
Abstract: Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond, X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings, or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.
8 citations
TL;DR: Mannich bases of types 1 or 8, which are readily synthesized by condensation of 3,4-methylenedioxyphenol with aromatic aldehydes and pyrrolidine or piperazine, react with cyclic and acyclic β-diketones to yield benzopyrans.
8 citations
TL;DR: The conclusion can be drawn that a direct interaction between the C6-substituents and the receptor structure is not of primary importance, however, the substitutents influence the orientation of the whole ligand approaching the binding site.
Abstract: The present paper describes our molecular modeling and quantitative structure-activity relationships (QSARs) studies on K(ATP) channel openers (KCOs) of the benzopyran type. In the first part we performed molecular modeling investigations with seven benzopyrans, varied at the C3- and C4-positions, in order to understand which molecular features at these positions are essentially effecting the biological activity. The impact of C6-substitution on biological activity was studied in the second part via HANSCH analysis. For this purpose physicochemical properties (charge distributions, lowest unoccupied molecular orbital (LUMO) energies, desolvation energies, volumes and dipole moments) were calculated for a set of 50 C6-varied benzopyrans. A QSAR equation was developed showing a relationship between the vasodilator activity and the direction of the dipole vector of the ligands. The conclusion can be drawn that a direct interaction between the C6-substituents and the receptor structure is not of primary importance. However, the substitutents influence the orientation of the whole ligand approaching the binding site. An unfavorably oriented ligand cannot bind to the binding site, thus exhibiting weak activity.
8 citations
TL;DR: Ether and ester analogues of 2,3-diaryl-2H-1-benzopyrans have been synthesised and tested for their pregnancy inhibiting activity in immature rats and esters were found to be better inhibitory agents.
8 citations
TL;DR: A cis 3 S,4 S isomer derived from an anticonvulsant trans 3 R, 4 S -( para -fluorobenzoylamino)-benzopyran using the DAST reagent, has been shown to possess antico-vulsants properties as discussed by the authors.
8 citations