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At least 1,027 records · Page 57Linked to original sources
PubMed1999

Insecticidal, anti-juvenile hormone, and fungicidal activities of organic extracts from different Penicillium species and their isolated active components.

Organic extracts from mycelium and culture broth of 21 Penicillium isolates have been tested for insecticidal, insect anti-juvenile hormone (anti-JH), and antifungal activities. Culture broth extracts were the most active, mainly against insects; nearly 25% of them have shown high entomotoxicity (100% mortality at 100 microg/cm(2)). A strong in vivo anti-JH activity against Oncopeltus fasciatus Dallas was detected in the culture broth extracts from P. brevicompactum P79 and P88 isolates. The two new natural products isolated from P79, N-(2-methyl-3-oxodec-8-enoyl)-2-pyrroline (1) and 2-hept-5-enyl-3-methyl-4-oxo-6,7,8,8a-tetrahydro-4H-pyrrolo[2,1-b]-1, 3-oxazine (2), possessed anti-JH and insecticidal activity, respectively, against O. fasciatus. Synthesized natural compound 1 has shown an ED(50) of 0.7 microg/nymph when assayed on newly molted fourth-instar nymphs of O. fasciatus. Promising biological activities have also been detected in the synthetic precursors.

Animals↗
PubMed2002

First highly stereoselective synthesis of fungicide systhane.

[reaction: see text] Highly enantiopure (R)-2-p-chlorophenyl-2-(1H-1,2,4-triazol-1-ylmethyl)hexanenitrile 1 (myclobutanil or systhane) was obtained in six synthetic steps from commercially available 1-hexyne (35% yield, 92% ee). The sulfinyl group controls the two key steps of the synthetic sequence, the highly stereoselective hydrocyanation of vinyl sulfoxides with Et(2)AlCN and the further introduction of the proper functionality into the molecule.

Fungicides, Industrial↗
PubMed2002

Facilitation of acetylcholine signaling by the dithiocarbamate fungicide propineb.

Dithiocarbamates (DTCs) are used mainly in agriculture as pesticides and as alcohol deterrent drugs. Neurological complications as well as movement disorders characterized by plastic rigidity, muscle twitch and paralysis are the prevailing symptoms in chronically exposed animals and humans. We investigated whether propineb interfered with peripheral cholinergic transmission in various isolated model systems. In electrically stimulated longitudinal muscle-myenteric plexus preparations (LMMPs), propineb (0.01-1000 nM) concentration-dependently enhanced the amplitude of both neurogenic twitch contractions and tritiated acetylcholine ([3H]ACh) release. The maximum percent increase was achieved by 10 nM propineb and was 19% and 14%, respectively. The effect on twitch contractions was partially antagonized by hexamethonium, a ganglionic nicotinic receptor blocker. In unstimulated LMMPs, propineb (10 pM, 10 nM, 10 microM) did not affect contractions to applied acetylcholine (ACh; 1 nM-10 microM), a finding indicating that propineb has no anticholinesterase activity. In human neuroblastoma cells (SH-SY5Y), propineb facilitated ACh release evoked by KCl depolarization. The increase in ACh release was not associated with detectable alterations of intracellular Ca2+([Ca2+]i) homeostasis. Binding studies carried out with alpha-bungarotoxin in striated muscle cells (L6) failed to demonstrate any influence of propineb on both affinity and capacity of skeletal muscle nicotinic receptors. In conclusion, propineb was found to interfere with cholinergic transmission in LMMPs and SH-SY5Y cells. In LMMPs, the potentiation of cholinergic transmission is partly dependent on the activation of ganglionic nicotinic receptors. Other targets relevant to cholinergic transmission seem not to be affected by propineb.

Acetylcholine↗