- INSECTICIDAL TRICYCLIC DERIVATIVES
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It has now been found that certain tricyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: wherein R through R, inclusively, and X and Y are fully described. Compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to the locus where insects are present or are expected to be present.
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- Synthesis, affinity at 5-HT(2A), 5-HT(2B) and 5-HT(2C) serotonin receptors and structure-activity relationships of a series of cyproheptadine analogues
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Cyproheptadine is a drug that shows high affinity for type 2 (5-HT2) receptors. We studied a series of compounds obtained by modification of the tricyclic system of Cyp (dibenzocycloheptadiene): 2f (thioxanthene), 2g (xanthene), 2h (dihydrodibenzocycloheptadiene), 2j (diphenyl), 2i (fluorene), and 3b (phenylmethyl). Their activities at the rat cerebral cortex 5-HT(2A) receptor were (pK(i) ± S.E.M.): 8.80 ± 0.11 (Cyp), 8.60 ± 0.07 (2f), 8.40 ± 0.02 (2g), 8.05 ± 0.03 (2h), 7.87 ± 0.12 (2j), 6.70±0.02 (2i) and 6.45±0.02 (3b); those at the rat stomach fundus 5-HT(2B) receptor (pA2±S.E.M.) were: 9.14±0.25 (Cyp), 8.49±0.07 (2F), 7.58±0.58 (2g), 7.02±0.14 (2h), 6.07±0.20 (2j), and undetectable (21, 3b); and those at the pig choroidal plexus 5-HT(2C) receptor (pK(i)±S.E.M.) were: 8.71 ± 0.08 (Cyp), 8.68 ± 0.01 (20, 8.58 ± 0.20 (2g), 7.95 ± 0.05 (2h), 7.57 ± 0.04 (2j), 6.98 ± 0.04 (2i) and 6.63 ± 0.20 (3b). The slopes did not differ significantly from unity. The compounds exhibited the same order of activities at every type of receptor, and the most active molecules presented certain steric (butterfly conformation of the tricyclic system) and electrostatic (proton affinity on the top of the central rings) patterns. It is concluded that the activity of cyproheptadine derivatives at 5-HT2 receptors is related to these molecular features, which make feasible a common disposition to interact with all three 5-HT2 subtypes.
- Honrubia, Maria Angeles,Jesus, Rodriguez,Dominguez, Rosa,Lozoya, Estrella,Manaut, Francesc,Seijas, Julio A.,Villaverde, Maria Carmen,Calleja, Jose M.,Cadavid, Maria Isabel,Maayani, Saul,Sanz, Ferran,Loza, Maria Isabel
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p. 842 - 848
(2007/10/03)
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- UNUSUAL REDUCTIONS INDUCED BY FORMIC ACID
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Treatment of xanthene carbinol 1a or xanthenylidene derivative 2a with refluxing formic acid unexpectedly gave dihydro compound 3a.Thioxanthene and acridine carbinols 1b and 1c and acridinylidene derivative 2c were also partially reduced when treated with formic acid.
- Loughhead, David G.
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p. 5701 - 5702
(2007/10/02)
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