Habitat management of organic vineyard in Northern Italy: the role of cover plants management on arthropod functional biodiversity.

The effect of cover plants on arthropod functional biodiversity was investigated in a vineyard in Northern Italy, through a 3-year field experiment. The following six ground cover plants were tested: Sweet Alyssum; Phacelia; Buckwheat; Faba Bean; Vetch and Oat; control. Arthropods were sampled using different techniques, including collection of leaves, vacuum sampling and sweeping net. Ground cover plant management significantly affected arthropod fauna, including beneficial groups providing ecosystem services like biological control against pests. Many beneficial groups were attracted by ground cover treatments in comparison with control, showing an aggregative numerical response in the plots managed with some of the selected plant species. Alyssum, Buckwheat and 'Vetch and Oat' mixture showed attractiveness on some Hymenoptera parasitoid families, which represented 72.3% of the insects collected by sweeping net and 45.7 by vacuum sampling. Phytoseiidae mites showed a significant increase on leaves of the vineyard plots managed with ground covers, in comparison with control, although they did not show any difference among the treatments. In general, the tested ground cover treatments did not increase dangerous Homoptera populations in comparison with control, with the exception of Alyssum. The potential of ground cover plant management in Italian vineyards is discussed: the overall lack of potential negative effects of the plants tested, combined with an aggregative numerical response for many beneficials, seems to show a potential for their use in Northern Italy vineyards.

Structure-activity studies of 16-methoxy-16-methyl prostaglandins.

The synthesis of the pure diastereoisomer of 16-methoxy-16-methyl-PGF2 alpha, -PGE2, and -PGE1 is described. The absolute configuration of C-16 was established by chemical methods, while the absolute C-15 configurations of the diastereoisomers were assigned tentatively on the basis of their chromatographic behavior and NMR spectra. The synthetic prostaglandin analogues were evaluated for antisecretory, antifertility, and diarrheogenic effects. Both the C-15 and C-16 configurations were found to be critical for the biological activities. These studies indicate that the introduction of the methyl and methoxy groups at C-16 into the prostaglandin analogues markedly increases the ratio of antisecretory to diarrheogenic action. One of the PGE1 derivatives, 9f(15 alpha, 16R) (MDL 646, mexiprostil), was selected for further pharmacological evaluation and is currently under clinical investigation.

Highly selective antiinflammatory and analgesic activity of 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H-naphth[1,2-d]imidazole, a new non-acidic molecule.

3-(1-Methylethyl)-2-(4-methoxyphenyl)-3H-naphth[1,2-d] imidazole (MDL-035) has antiinflammatory activity in various antiinflammatory models such as carrageenin and nystatin oedemas, cotton pellet granuloma and adjuvant arthritis. The antiinflammatory potency of MDL-035 is greater than that of acetylsalicylic acid and phenylbutazone, but lower than that of indomethacin. MDL-035 has practically no gastroulcerogenic activity in rats, does not affect water or salt excretion, has no hormonal or antihormonal effects and has no other unwanted pharmacological effects. Its acute toxicity is very low.

Synthesis and analgesic activity of new tricyclic pyrazolo[3,4-b]pyridines.

The title compounds have been obtained in a two-step synthesis from 5-amino-4-(1-cycloalkenyl)pyrazoles. Among the synthetized compounds, the 6,7,8,9-tetrahydro-1,3-dimethyl-3H-pyrazolo[3,4-c]isoquinoline, showed interesting antiinflammatory and analgesic activity.

[Synthesis and pharmacologic activity of derivatives of 3-aminopropiophenone and 3-aminomethylcamphor]. / Sintesi ed attività farmacologica di derivati di 3-aminopropiofenoni e di 3-aminometilcanfore.

As a part of a research on analgesic compounds 0-(4-methoxyphenyl)carbamoyl-3-aminopropiophenone oximes, 0-(4-methoxyphenyl)-carbamoyl-3-aminomethylcamphor oximes and 4-(4-methoxyphenyl)semicarbazones of 3-aminopropiophenones were prepared. The analgesic activity of these compounds was tested and the results of pharmacological screening are discussed.

MDL-646, a new synthetic E1-prostaglandin with local protective effects on the gastric mucosa.

The gastric protection, diarrheogenic and arterial hypotensive effects of MDL-646, a PGE1 derivative, have been studied in rats. The compound administered p.o. or i.v. was able to inhibit the macroscopic damage to gastric mucosa produced by noxious stimuli (ethanol and indomethacin). In the stomach perfusion test with the anesthetized rat, intravenously administered MDL-646 reduced histamine- or pentagastrin-stimulated gastric secretion. After intraduodenal administration (i.d.) doses at least 40-50 times greater were necessary for an antisecretory effect. In conscious rats with chronic gastric fistulas, intragastrically administered (i.g.) MDL-646 affected both acid concentration and volume of unstimulated gastric secretion. In experimental models for gastric lesions, MDL-646 was much more potent after oral (p.o.) (15-30 times) than after i.v. administration. (ED50 micrograms/kg: vs. alcohol lesions, 0.05 p.o. and 0.7 i.v.; vs. indomethacin ulcers, 7.0 p.o. and 195 i.v.). Our data would fit the hypothesis that it was a local effect on the gastric mucosa. The mechanism of this effect is not known. The supposed local activity coupled with the antisecretory effects and the good tolerability make it interesting to test MDL-646 as an anti-ulcer agent in man.

Inhibition of PG production by MDL 035, a new non-steroidal non-acidic anti-inflammatory compound, in rat gastric mucosa and inflammatory exudate.

The effects of 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H-naphth [1,2-d]imidazole, MDL 035, a new non-steroidal non-acidic anti-inflammatory compound, on the production of prostaglandin (PG) in rat gastric mucosa in vivo and in vitro and in inflammatory exudate in vivo were studied. MDL 035 reduced PGE2 and 6-keto-PGF1 alpha levels more effectively in inflamed tissue than in gastric mucosa when assayed in in vivo experiments, whereas indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDS) are equally effective in both systems. MDL 035 is almost as active as indomethacin when incubated with gastric tissue in vitro. The better gastric tolerance of MDL 035 than of other NSAIDS is discussed in relation to these differences in in vivo and in vitro effects.

Antiinflammatory properties of a series of 4-amino-5-arylpyrazoles.

A series of ethyl 4-amino-5-arylpyrazol-3-yl carboxylates were prepared from arylacetonitriles and ethyl diazoacetate. The compounds were evaluated for their analgesic and antiinflammatory properties, that were not, however, sufficiently interesting to justify the further development of the compounds. The synthesis of the compounds could be a useful extension of the original report by A. Bertho on the reaction between ethyl cyanoacetate and ethyl diazoacetate to yield diethyl 4-aminopyrazole-3,5-dicarboxylate.

Synthesis and pharmacological evaluation of a series of analgesic and antiinflammatory 4-aminopyrroles.

The synthesis and the pharmacological evaluation of a series of analgesic, antiinflammatory beta-aminopyrroles is described. Qualitative structure activity relationships are discussed. One of the compounds reported in the study is a candidate for toxicological and clinical trials.

3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents.

Novel 3-alkyl-2-aryl-3H- naphth [1,2-d]imidazoles were synthesized and evaluated as antiinflammatory agents in the carrageenin-induced paw edema, cotton pellet induced granuloma, and adjuvant-induced polyarthritis assays in rats. The analgesic, antipyretic, and gastroulcerogenic effects were also tested. Structure-activity relationships are discussed. One of the compounds, 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H- naphth [1,2-d]imidazole (35), was selected for clinical trials as a nonacidic antiinflammatory and analgesic agent.

Protection of rat gastric mucosa against ethanol injury by the new synthetic prostaglandin MDL 646.

Oral administration to fasted rats of absolute ethanol produces extensive necrotic lesions of gastric mucosa as well as a massive leakage of proteins and mucus glycoproteins into gastric lumen. When the new synthetic prostaglandin MDL 646, belonging to the PGE1 series, is administered intragastrically (2 or 10 micrograms/kg) 30 min before ethanol administration, a significant protection of rat gastric mucosa against alcohol injury is observed.

Cyclic hydrazides. V - synthesis and antiinflammatory activity of derivatives of the 2-amino-1,4-dihydroisoquinolin-3(2H)-one.

The synthesis of the 2-amino-1,4-dihydroisoquinolin-3(2H)-one (II a) and of some of its derivatives starting from the o.methylphenylacetic acid, is described. Some of the described compounds possess a moderate antiinflammatory activity.

[Unexpected anti-inflammatory activity of rigid structures derived from antihypertensive 6-arylpyridazinones. III. Synthesis and activity of 7-fluoro- and 5-keto-5H-indeno(1,2-c)pyridozines]. / Inattesa attività antiinflammatoria di strutture rigide derivate da 6-arilpiridazinoni antipertensivi. Nota III--Sintesi e attività di 7-fluoro e 5-cheto-5H-indeno[1,2-c)piridazine.

5H-Indeno[1,2-c]pyridazine (Ia) and its 3-oxo- and 4,4a-dihydro-3-oxo derivatives, already known to have antiinflammatory activity, were subjected to 7-fluoro substitution or to oxidation of the 5-methylene to a carbonyl group. The pharmacological evaluation of the resulting compounds indicated that the antiinflammatory activity disappeared in the fluoro derivatives, while it was still present in the 5-keto derivatives (I e), (II c). Moreover, the analgesic-antipyretic component of (I e) proved to be strongly enhanced compared with that of (I a).

Antiinflammatory activity and other pharmacological properties of 11 beta, 21-dihydroxy-2'-methyl-5' beta H-pregna-1,4 dieno[17,16-d] oxazole 3,20-dione-21-acetate (Deflazacort).

The pharmacology of 11 alpha, 21-dihydroxy-2'-methyl-5' beta H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione-21-acetate (deflazacort) was studied by oral and parenteral administration in acute, short- and long-term experiments in rats. Deflazacort has antiinflammatory activity in various laboratory models, such as carrageenin and nystatin oedema, cotton pellet granuloma, adjuvant arthritis and on liver glycogen storage. The antiinflammatory potency of deflazacort is greater than that of prednisolone, but lower than that of dexamethasone. Absorption from the gut and duration of action appear to be highly satisfactory, as deduced from pharmacological and biochemical measurements. Glucose tolerance curves seem less affected by deflazacort than by prednisolone, while cardiovascular and central nervous system findings do not show unexpected responses.

Synthesis and anti-inflammatory properties of some pyrrolo(1H,3H)[3,4-d]pyrimidin-2-ones and pyrrolo(1H,6H)[3,4-d]pyrimidin-2-ones.

The unequivocal synthesis of some terms belonging to the two isomeric classes of the pyrrolo(1H,3H)[3,4-d]pyrimidin-2-ones and of the pyrrolo(1H,6H)[3,4-d]pyrimidin-2-ones is reported. Some of these compounds are active in inhibiting the development of the carrageenin edema, of the granuloma cotton pellet and of the adjuvant arthritis in the rat when administered orally.

[Cyclic hydrazides. III. Synthesis and anti-inflammatory activity of 2-amino-3,4-dihydroisoquinolin-1(2H)-one]. / Idrazide cicliche. Nota III - Sintesi ed attività antiinfiammatoria di 2-amino-3,4,diidroisochinolin-1(2H)-oNI

The synthesis and the antiinflammatory activity of of 2-amino-3,4-dihydroisoquinolin-1(2H)-one and of a series of its derivatives on the amino function are described. Some of theses new componds show high activity in inhibiting the carrageenin oedema and granuloma formation in rats.

Synthesis and pharmacological properties of derivatives of pyrrolo(3,4-d)pyrimidines and pyrrolo(3,4-b)pyridines (I).

The synthesis of variously substituted pyrrolo[3,4-d]pyrimidines and pyrrolo[3,4-b]pyridines is reported. Some of the compounds act as reducers of the carrageenin edema in the rat and as inhibitors of prostaglandin biosynthesis in a microsomal preparation of bovine seminal vesicles.

Correlation of anti-inflammatory activity with inhibition of prostaglandin synthesis activity of nonsteroidal anti-estrogens and estrogens (38532).

Diethylstilbestrol, clomiphene, ethamoxytriphetol and triparanol were 0.18, 1.0, 0.02 and 0.01 times as potent in the in vitro inhibition of prostaglandin synthetase, respectively as was indomethacin. In the in vivo carrageenan-induced rat paw edema studies, diethylstilbestrol was more potent as an anti-inflammatory agent than was clomiphene, and ethamoxytriphetol and triparanol were only marginally effective. The most potent of the compounds tested was indomethacin. The results reported demonstrate that the nonsteroidal anti-inflammatory agents and the nonsteroidal estrogens and anti-estrogens share the property of inhibition of prostaglandin synthetase.