Marine natural products as lead anti-HIV agents.

Current anti-HIV drugs have extreme side effects and resistance to these drugs develops rapidly. The marine environment holds an unprecedented number of unusual chemical structural classes with activity against HIV. We review the literature on anti-HIV activity of marine natural products and discuss the efficacy of different structural classes.

[Construction principles, strength investigation and early clinical results of the Integracja osteosynthesis system: a preliminary report]. / Budowa oraz ocena wyników badan wytrzymalosciowych i klinicznych zestawu do zespolen kosci dlugich Integracja--doniesienie wstepne.

The aim of this paper was to present the construction principles and strength investigation of the Integracja osteosynthesis system. Preliminary results of fracture treatment in 6 patients with hip and knee prosthesis are presented. Inc all cases bony union was obtained. Integracja can be successfully used in femur fractures near the tip of the prosthesis shaft.

Chemistry of puupehenone: 1,6-conjugate addition to its quinone-methide system.

The marine natural product puupehenone (1), isolated in good yields from sponges of the genus Hyrtios, has been shown to undergo stereospecific 1,6-conjugate addition to its quinone-methide system. Several nucleophilic agents such as hydrogen cyanide, Grignard reagents, and nitroalkanes were studied, producing structurally diverse compounds. This lead optimization study was initiated due to the bioactivity of puupehenone and its natural analogues, which includes numerous previous reports of potential anticancer and antiinfective activity.

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.

Certain phenylalkylamine derivatives have been considered to bind selectively at 5-HT2 serotonin receptors. It is now recognized that the most widely used derivatives, i.e., 1-(2,5-dimethoxy-4-X-phenyl)-2-aminopropanes where X = Me (DOM), Br (DOB), and I (DOI) (1-3, respectively) also bind at the more recently identified population of serotonin 5-HT1C receptors. The purpose of the present investigation was to determine whether simple phenylalkylamines bind selectively at one population of receptors over the other. An examination of 34 derivatives reveals (i) similar structure-affinity relationships and (ii) a significant correlation (r = greater than 0.9, n = 25) between 5-HT1C and 5-HT2 affinity. None of the compounds included in the present study displayed more than a 10-fold selectivity for one population of these receptors over the other; the results suggest that these compounds (including the widely used 5-HT2 agonists DOB and DOI) are 5-HT1C/5-HT2 agents.

N-aminoalkylderivatives of 1,2,3,4-tetrahydro-beta-carboline-1-spiro-4'-N'- benzylpiperidine--a putative way to novel anxiolytic agents.

A series of aminoalkylderivatives of 1,2,3,4-tetrahydro-beta-carboline-1-spiro-4'-N'-benzylpiperidine were synthesized by means of chloroacetylation of the title compound and substitution of chlorine atom with various heterocyclic amines in DMSO, followed by LAH reduction of the carbonyl group. Of the ten tested compounds (4a-4e, 5a-5e), compound 5d given ip, but not orally, showed an anxiolytic activity in the four-plate test in mice and in the conflict test in rats. Compound 5d is devoid of an anticonvulsant or neurotoxic action. The activity of compound 5d resembles this of buspirone.

Synthesis and preliminary pharmacological screening of 4-methylamino-2-phenylquinoline-3-carboxamides.

Eight new 4-methylamino-2-phenylquinoline-3-carboxamides were obtained. Three of them were screened pharmacologically and all turned out to be antiinflammatory, analgesic and sedative compounds. Their properties were compared to those of indomethacin and pethidine.

Synthesis and pharmacological properties of N-arylpiperazine-N'-alkylindanes.

Ten new compounds, N-aryl substituted piperazinealkylindanes, have been synthesized. The most active one 1-(2-[4-(3-chlorophenyl)-1-piperazinyl]-ethyl)-indane (compound 9), displayed evident central serotoninolytic properties in the 5-hydroxytryptamine (5-HTP) head twitch test in mice, as well as in the tryptamine convulsions test and the quipazine-stimulated hind paw flexor reflex test in rats.

Synthesis and pharmacological properties of N-aroyl-beta-(1-indanyl)-ethylamines.

Six new N-acyl derivatives of beta-(1-indanyl)ethylamine were obtained. The most active of them, N-(m-chlorobenzoyl/-beta-1-indanyl)-ethylamine (compound 2), decreased the 5-HTP-induced head twitches in mice and the tryptamine-induced syndrome in rats, attenuated the quipazine-induced stimulation of the hindlimb flexor reflex in spinal rats, and reduced the immobility time in mice in the behavioral despair test. All these effects might be indicative of the antidepressive properties of compound 2.