Vernalis

Mandragora vernalis. Hyoscyamine, hyoscine, -hyoscyamine, mandragorine (p. 83). ... 

Roderick E. Hubbard, Structural Biology Laboratory, University of York, Heslington, York, YOlO 5DD, UK and Vernalis (R D) Ltd, Granta Park, Abington, Cambridge, CBl 6GB, UK. (rod ysbl.york.ac.uk, r.hubbard vernalis.com). 

An azetidine motif was also present in two series of CBi antagonist compounds disclosed by Vernalis Research [335, 336]. In the former, compound (560) was claimed to have an affinity of 285 nM in transfected HEK293 cells using tritium-labelled (382). Among the preferred indications were psychosis, schizophrenia, smoking cessation and eating disorders associated with excessive food intake. Compound (561) was claimed to have an affinity of 0.8 nM in the same binding assay [336]. 

Adonis brevistyla Franch. A. chrysocyathus Hook F. T. Thoms. A. vernalis L. Fu Shou Cao (Amur adonis) (aerial part) Cymarol, adonilide, pergularin, corchoroside A, convallatoxin, isoramanone.33 This herb is toxic. Treat heart disease and depression, diuretic. 

In the following sections, we will describe in detail efforts to build fragment collections and the processes involved in their creation. Two such efforts were performed at a major pharmaceutical company (Pfizer) while a third took place at a biotech company (Vernalis). 

Due to the evolutionary nature of the Vernalis fragment collections and the fact that various screens were performed over a period of several years, it is difficult and perhaps unreasonable to directly compare the hit rates across multiple screens. However, it is still helpful to notice that reasonable hit rates (compared to HTS) are obtained across a diverse group of targets (Table 11.1). 

Gillespie, R. J., Giles, P. R., Lerpiniere, J., Dawson, C. E., Bebbington, D. (Vernalis Research, Ltd), Thieno- and furopyrimidine derivatives as A2a-receptor antagonists, WO0102409. 

C. vernalis, Cajanus cajan, Calliandra angustifolia, C. bracleosa,... 

The known alkaloids senecionine, senkirkine, and retrorsine have been isolated from Senecio vernalis Wald, et Kit. by Roder et al.26 A new alkaloid, named senecivernine (59), was also present. The mass spectrum of (59) showed a molecular ion at m/z 335, and fragment ions at m/z 291, 248, and 220, characteristic for a macrocyclic diester of retronecine, arising from cleavage of the allylic ester.17 Basic hydrolysis of senecivernine gave a new necic acid which had spectroscopic data in accord with the proposed structure. Retronecine was not isolated. The necic acid from senecivernine is a Ci0 acid of an unusual structural type (cf. Vol. 8, p. 55). 

Mandragora autumnalis Bertol. and M. vernalis Bertol. (M. officinarum L.) (Solanaceae)... 

Pyrrolizidine alkaloids in the plant Senecio vernalis have been implicated in the poisoning of cattle.13 The toxic agents in this plant include three closely related alkaloids — senecionine, senkirkin, and seneciphyllin. The structural formula of senecionine is shown in Figure 19.2. 

FeverAII is a registered trademark of Alpharma U.S. Pharmaceuticals Division (USPD) Flexeril is a registered trademark of Merck Company, Inc. Frova is a registered trademark of Vernalis Development Limited Company. 

Two years after the first preparation of L-ribose, Fischer74 described the reduction of the sugar with sodium amalgam to the corresponding pentitol, which he showed to be identical with the polyol adonitol from Adonis vernalis L.75 76 A process for the catalytic hydrogenation of D-ribose in the presence of magnesium-activated Raney nickel to ribitol has been patented.77... 

Very little quantitative data have been reported in relation to the concentration of aconitic acid in various plant juices other than from cane sorghum and from sugar cane varieties although the acid has been identified in the juices from many other species of plants. It has been isolated from a variety of species of Aconitum,1-7-11 Delphinium,9 12 and Equisetum,2 3-l2a and also from Achillea millefolium,Adonis vernalis,u,lb Helinus ovatus,16 Sansevieria zeylancia,17 wheat,18 and from barley, maize, oat and rye plants.19 It can indeed be said that aconitic acid, at least qualitatively, is a commonly occurring constituent in the plant kingdom. 

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