Search results for "Indole"

Negative symptomatology: psychopharmacological strategies and methodological aspects for drug evaluation

1993

Investigation of the Alkaloid Content of Rauwolfia serpentina Roots from Regenerated Plants.

1991

The indole alkaloid content of RAUWOLFIA SERPENTINA roots from regenerated plants (from stem-and root-callus) was compared with the parental stock. Although the total alkaloid content seems to be slightly higher in the roots from regenerated plants, HPLC-analysis of individual alkaloids indicated that the contents of the alkaloids ajmaline ( 1), serpentine ( 2), and reserpine ( 3) are lower than in the roots of the parental stock. The glucoalkaloid raucaffricine ( 4) was identified as a constituent of all samples, thus providing the first evidence for its occurrence in roots of RAUWOLFIA SERPENTINA.

Chemistry and biology of new marine alkaloids from the indole and annelated indole series.

2003

Chemistry and biology of marine natural products from the indole and annelated indole series have become an attractive research field for development of new pharmacological lead substances. In the past years some of the isolated natural organic compounds were synthesized by chemists and evaluated with great enthusiasm to find new lead natural compounds against different diseases. In this review the latest results for new compounds including isolation, biological evaluation, synthetic pathways and some retrosynthetic analyses are summarized.

Indole alkaloids from the coprophilous fungus Aphanoascus fulvescens

2019

Abstract The Ascomycete fungus Aphanoascus fulvescens isolated from goose dung was investigated for its secondary metabolites, yielding five new indole alkaloids okaramines V–Z (1–5) and eleven known derivatives (6–16). Their structures were determined by 1D, 2D NMR spectra and HRMS data. Compounds 6, 8, 11 and 12 showed significant to moderate cytotoxicity against the mouse lymphoma cell line L5178Y with IC50 values ranging from 4.0 to 14.7 μM. Preliminary structure-activity relationships are discussed.

Ipobscurines, Non-ergoline Type Indole Compounds from the Seeds of Ipomoea obscura.

1986

Advances in Marine Natural Products of the Indole and Annelated Indole Series: Chemical and Biological Aspects

2001

Marine natural products, form a field of scientific endeavour, that has recently grown considerably. The isolation, biological evaluation, chemical properties and synthetic elaborations of products of marine organisms have attracted the attention of organic chemists, medicinal chemists, biologists and pharmacists. In this context a structurally and biologically highly interesting class is represented by the marine natural products containing an indole moiety in a pure substituted form or in an anellated form. The present review summarizes primarily the actual results concerning these products as new pharmacologically attractive lead compounds for drug design. The chemistry, biological evalu…

Isolation, Identification, and Chemical Synthesis of 6α-Hydroxyraumacline: A Novel Alkaloid from CultivatedRauwolfia serpentinaCells

1992

From RAUWOLFIA SERPENTINA cells cultivated in the presence of ajmaline ( 2) the new indole alkaloid, 6alpha-hydroxyraumacline ( 1), was isolated. This alkaloid also occurs in significant amounts in the nutrition medium. A simple chemical synthesis of 1 was developed starting from ajmaline ( 2).

The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery.

2022

Azulene is a bicyclic scaffold rarely applied in medicinal chemistry. Here we report physicochemical and in vitro parameters relevant for drug discovery for a series of diversely substituted azulenes. We synthesized and characterized several scaffold hopping series of analogously substituted azulenes, indoles and naphthalenes. This enabled a comparison of azulene with the more common scaffolds indole and naphthalene. Our data indicates that undesirably low photostability of azulenes is restricted to certain substitution patterns. Generally, we conclude that azulene is an underused lipophilic bicycle and should be considered as a valuable complement to the collection of medicinal chemistry s…

Substrate Specificity of Vinorine Hydroxylase, a Novel Membrane-bound Key Enzyme of Rauwolfia Indole Alkaloid Biosynthesis

1995

The Reactivity of 4’-Substituted Spiro[Isoindole-1,3’-pyrazoles] Derivatives: Substitution/Elimination Reactions and Access to Biaryl Derivatives

2017

This paper describes aspects of the chemistry of 4’-substituted spiro [indole-1,3’-pyrazoles]. These compounds underwent substitution and/or elimination reactions to afford some new spiro- as well as biaryl derivatives of potential pharmaceutical relevance. Mechanistic considerations are discussed as well.