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PubMed1985

[Synthesis and pharmacologic activity of new derivatives of salicylic acid].

New 1-phenyl-2-R2-3-methyl-5-salicyloylimmino-3-pyrazolines were synthesized according to a previously described route. The obtained pyrazoline derivatives, together with some others reported in previous papers, were tested for analgesic and antiinflammatory activities. Some derivatives showed analgesic and/or antiinflammatory activity similar to that of acetylsalicylic acid.

Animals↗
PubMedDate not supplied

[Molluscacide activity of a mixture of 6-n-alkyl salicylic acids (anacardic acid) and 2 of its complexes with copper (II) and lead (II)].

The molluscicide activity of hexanic extract from Anacardium occidentale L. (cashew) nut shell, of copper (II) complex, of lead (II) complex and anacardic acid has been compared in the laboratory in an attempt to obtain better stability than anacardic acid. This was obtained from the hexanic extract of the cashew nut shell by precipitation with lead (II) hydroxide or cupric sulfate plus sodium hydroxide or (II) cupric hydroxide followed by treatment of lead (II) complex with a diluted solution of sulfuric acid. Ten products of the mixture obtained were tested on adults snails of Biomphalaria glabrata at 1 to 10 ppm. The most active products were copper (II) complex, obtained by cupric sulfate plus sodium hydroxide, and anacardic acid (sodium hydroxide) which presented activity at 4 ppm. The anacardic acid's lead content was above the limits accepted by the United States standards.

Animals↗
PubMed1986

Aspirin and related derivatives of salicylic acid.

After almost 90 years of clinical use, aspirin remains one of the world's most extensively used 'over-the-counter' drugs, and it is still recognised as the standard analgesic/antipyretic/anti-inflammatory agent by which newer drugs are assessed. However, its pre-eminent position as the analgesic of choice for mild to moderate pain has been seriously challenged with the introduction of many 'new' non-steroidal non-narcotic analgesic drugs. Indeed, there is convincing scientific evidence that many of the 'newer' non-steroidal drugs such as diflunisal, ibuprofen, flurbiprofen etc. are significantly superior analgesics and, in many cases, have a longer duration of action. In recent years the salicylates, aspirin in particular, have been the focus of much attention regarding their side effect profiles. At usual dosages for relief of pain and during occasional use, aspirin is well tolerated by the vast majority of patients. Adverse reactions, of which there is a wide spectrum, most frequently accompany anti-inflammatory doses of aspirin, or may be the result of accidental overdosing (particularly in children and the elderly)--probably a reflection of the lay population's acceptability of aspirin's presumed safety. As with other non-steroidal analgesic drugs, gastrointestinal complaints are the most commonly reported side effects. The existence of many shared clinical, adverse and toxic effects of aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs) is thought to be accounted for by a common mechanism--inhibition of the ubiquitous cyclo-oxygenase enzyme. Thus, suppression of prostaglandin biosynthesis is widely considered to explain the common properties of NSAIDS, although further research is still necessary to clarify some inconsistencies and to complete our understanding of the processes involved. Aspirin and salicylates have been reported to have a wide range of drug interactions but only relatively few seem to be clinically important. Many of the interactions are pharmacokinetic in nature. Drugs considered to produce the most significant interactions with salicylates include anticoagulants and thrombolytic agents, uricosuric agents, corticosteroids, methotrexate and sulphonylurea hypoglycaemic agents.

Aspirin↗
PubMed1998

Pyridines and pyrazolines from salicylic acid derivatives with propenone residue and their antimicrobial properties.

Reaction of the propenones 1c, d with chlorosulfonyl isocyanate followed by hydrolysis gave the corresponding carbamoyloxybenzoates 2a, b. While their reaction with ethyl isocyanate afforded the 1,3-benzoxazine-2,4-diones 3a, b. Reaction of 1a, b with aryl hydrazines gave the pyrazolines 4a, d, whereas, with hydrazine hydrate in acetic acid, the acetyl derivatives 4e, f were produced. 1c, d reacted with malononitrile and ethyl cyanoacetate affording the cyanopyridines 5 and cyanopyridones 6 respectively. The products show antimicrobial activities.

Anti-Bacterial Agents↗
PubMed1984

[The effect of a tar admixture to dithranol-salicylic-acid-white-petrolatum therapy on the cytokinetics of psoriasis].

The initial stimulation of DNA-synthesis after application of dithranol as single agent is completely inhibited by addition of tar. The autoradiographic analyse indicates that the good clinical effect of the new antipsoriatic therapy with TCSV may be due to suppression of dithranol-caused irritation by tar. But, restored cytokinetic values do not correspond to clinical remission of psoriasis.

Adolescent↗
PubMed1982

Comparison of betamethasone dipropionate lotion with salicylic acid (Diprosalic) and clobetasol propionate lotion (Dermovate) in the treatment of psoriasis of the scalp.

A double-blind comparison was made between Diprosalic and Dermovate lotions in fifty-one patients with psoriasis of the scalp. Both preparations were highly effective. No significant difference in efficacy between the preparations could be demonstrated after 3 weeks treatment except for antipruritic effect, in this respect Diprosalic being superior to Dermovate. Only three patients (two in the Dermovate group, and one in the Diprosalic group) experienced minor adverse reactions. Plasma cortisol levels were determined in seventeen of the patients and no significant influence on the adrenal function could be shown on the part of either of the preparations.

Anti-Inflammatory Agents↗
PubMed1977

[Comparative clinical and histological studies on extraction wounds with and without local application of a salicylic acid preparation (Apernyl)].

Selected patients with extraction wounds served to experiment with Apernyl-styli of Bayer. Contralateral alveoli were used as controls. 10 days following operation biopsies were taken from treated and untreated alveoli. Histologically, a morphometric study was made, and clinically healing was judged by the frequency of complications and the initial physiologic pain. The results show that Apernyl does not influence histological healing, positively or negatively. Thus, the results obtained by Nordenram and Band (1970) and Satoh et al. (1973) could be confirmed. Clinically, there were significanlty less p.o. complications in patients with Apernyl prophylaxis; 2 of 51 treated alveoli compared to 8 of 45 untreated ones. Pain was significantly reduced: 17 of the 19 patients complained of pain in the untreated half of the jaw, while only 4 suffered pain on the treated side. This confirms the findings of Neuner and Panzera and Neuner and Schegg (1972 and 1969 resp.).

Alveolar Process↗
PubMed2004

FT-IR and NMR spectroscopic studies of salicylic acid derivatives. I. Gentisamide -- a metabolite of salicylamide.

Gentisamide (GAM, 2,5-dihydroxybenzamide), a minor first-pass metabolite of salicylamide (SAM, 2-hydroxybenzamide), was studied using FT-IR, 1D and 2D homo- and heteronuclear 1H and 13C NMR spectroscopy. GAM was isolated from human urine eight hours after oral administration of SAM. FT-IR, 1H and 13C NMR spectra unequivocally confirmed the chemical structure of GAM through chemical and substituent shifts, coupling constants and connectivities in COSY, NOESY, HETCOR and HBMC spectra. From NOESY spectra of GAM in DMSO-d6, it was concluded that the amide protons are oriented toward the ortho-proton at C-6. Obtained results indicate that the presence of the additional phenol group at C-5 in GAM favours the formation of intramolecular hydrogen bonding of the O...HO type between C2-OH proton and oxygen atom of the amide group.

Benzamides↗
PubMed1989

Effect of scavengers of active oxygen species and pretreatment with acetyl-salicylic acid on the injury to cultured endothelial cells by thrombin-stimulated platelets.

Thrombin-stimulated human platelets adhere to and injure cultured human endothelial cells. We hypothesize that generation of active oxygen species by the stimulated platelets are involved in the injury. To confirm this, catalase [final concentration (8.25 micrograms/ml)], superoxide dismutase (SOD) (10 micrograms/ml), of D-mannitol (9 mg/ml) were added to the cell culture medium before the experiments. Platelet suspension (200,000/microliters) and thrombin (4 U/ml) were added and the culture dishes shaken for 15 min at room temperature. In separate experiments the endothelial cells were pretreated with acetylsalicylic acid (0.05, 0.1, or 0.5 mM) to test whether the arachidonic acid metabolism of the endothelial cells is involved in the injury process. In preliminary experiments we were able to confirm that platelets, when stimulated by thrombin, produce chemiluminescence which was suppressed by mannitol but not by catalase or SOD. The degree of injury to cultured endothelial cells by thrombin-stimulated platelets, as measured by release of 51Cr from prelabeled endothelial cells, was reduced significantly with the presence of mannitol, but only moderately when catalase or SOD had been added. Morphometric quantification based on scanning electron micrographs of the endothelial cells after exposure to thrombin-stimulated platelets in the presence of catalase or mannitol showed a reduced number of injured cells. Pretreatment of the endothelial cells with acetylsalicylic acid did not cause any significant change in the degree of endothelial cell injury as measured by the 51Cr release. It is concluded that active oxygen species, in particular hydroxyl radicals, may be generated during thrombin stimulation of platelets and cause injury to the endothelial cells.

Aspirin↗
PubMed1981

Effects of very low versus standard dose acetyl salicylic acid, dipyridamole and sulfinpyrazone on platelet function and thromboxane formation in man.

The effects of three conventional antiplatelet regimes, dipyridamole 3 X 75 mg/day (D), sulfinpyrazone 4 X 200 mg/day (S), acetylsalicylic acid 3 X 330 mg/day combined with dipyridamole 3 X 75 mg/day (ASA + D), and very low dose acetylsalicylic acid 100 mg/day (ASA) on platelet function were studied in man following 4 days of treatment. D and S slightly increased mean minimal ADP concentration for irreversible aggregation (n.s.), S reduced aggregation and thromboxane (TXB2) formation on low dose collagen (2P less than or equal to 0.05), ASA and ASA + D increased platelet count (2P less than or equal to 0.05), increased bleeding time (n.s. for ASA, 2P less than or equal to 0.05 for ASA + D), abolished irreversible aggregation on ADP, suppressed TXB2 formation on all (2P less than or equal to 0.001) and aggregation on lower concentrations of collagen (2P less than or equal to 0.01) and abolished aggregation and TXB2 formation on arachidonic acid (2P less than or equal to 0.001). Very low dose ASA suppresses platelet aggregation and TXB2 formation on several stimuli of possible physiologic significance. In the light of a recently proposed critical balance of vascular antiaggregatory prostacyclin and platelet proaggregatory TXA2 very low dose ASA might offer advantages over conventional dosage of ASA and should be evaluated in thromboembolic disorders.

Adenosine Diphosphate↗