Synthesis and structure-activity correlations within allylamine antimycotics.
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Allyl Compounds↗
Biomedical subjects
A Stütz
Publications and source records attributed to A Stütz.
Synthesis and structure-activity relationships of naftifine-related allylamine antimycotics.
Naftifine (1) is the first representative of the new antifungal allylamine derivatives. Its biological activity is strictly bound to specific structural requirements that are unrelated to those of known antifungals. A tertiary allylamine function seems to be a prerequisite for activity against fungi. By systematic variation of the individual structural elements in 1, detailed structure-activity relationships are defined in which the phenyl ring is the structural feature permitting the widest variations. Versatile synthetic routes to allylamine derivatives and comparative biological data are presented.
Allylamine↗
Allylamine derivatives: new class of synthetic antifungal agents inhibiting fungal squalene epoxidase.
A new class of synthetic antifungal agents, the allylamines , has been developed by modification of naftifine , a topical antimycotic. SF 86-327, the most effective of these compounds so far, is highly active in vitro against a wide range of fungi and exceeds clinical standards in the oral and topical treatment of guinea pig dermatophytoses. SF 86-327 is a powerful specific inhibitor of fungal squalene epoxidase, a key enzyme in sterol biosynthesis.
Allylamine↗
Synthesis and antifungal activity of (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphtha lenemethanamine (SF 86-327) and related allylamine derivatives with enhanced oral activity.
The allylamine derivatives are a new class of synthetic antifungal agents inhibiting fungal squalene epoxidase. A new subclass, which features an acetylene group conjugated with the allylamine double bond, is characterized by enhanced antifungal activity, especially on oral treatment of guinea pig dermatophytoses. Increased branching of the alkyl group next to the triple bond led to the tert-butylacetylene derivative SF 86-327, a compound with strikingly increased activity in vitro and in vivo, which is now under clinical evaluation. Versatile synthetic routes, comparative biological data, and structure--activity relationships are presented.
Administration, Oral↗
The affinity of E. coli RNA polymerase to matrix bound rifamycin.
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Binding Sites↗
Properties of ATP and UTP analogues with P-S-C-5' bonds.
Analogues of ATP and UTP bearing C-5'-S-P ester bonds were found not to be substrates but weak competitive inhibitors of Escherichia coli RNA polymerase. The K-i values of the analogues obtained in the transcription of poly[d(A-T)] or poly(dT) under various conditions are in the order of millimolar. Evidence was derived from proton magnetic resonance spectra that nucleotides with C-5'-S-P bonds do not exist in gauche-gauche conformation normally adopted by natural occurring nucleotides. This leads us to assume that the gauche-gauche conformation is an essental prerequisite for substrates of RNA polymerase. Ado-5'-S-PPP substituted for ATP as substrate of hexokinase from yeast rather effectively thus indicating that a distinct stereochemical orientation of the alpha-phosphate ester bond is not a stringent requirement for substrates of this enzyme.
Adenosine Triphosphate↗
[Effectiveness of interscalene plexus block for open subacromion decompression].
AIM: The aim of this study was to assess the influence of interscalene brachial plexus blocks on the functional outcome, subjective pain appraisal and patient satisfaction after open shoulder surgery. These results were compared with patients treated by conventional analgesic measures. METHOD: 23 patients with interscalene brachial plexus block (ISB) and 21 patients without ISB were evaluated preoperatively as well as 1, 7, 12 and 90 days after open surgery of the shoulder. By means of a visual analogue scale (VAS) subjective postoperative pain intensity was assessed. Using the Constant score preoperatively and 6 months after surgery the functional status of the treated shoulder was evaluated. At discharge from hospital patients were asked whether they were satisfied with the analgesic measures taken. RESULTS: The range of motion of the shoulder of patients treated with an ISB was significantly higher 1 and 7 days after surgery than those without ISB. 12 and 90 days postoperatively the range of motion in the ISB group was still higher, but no longer statistically significant. Assessment of the postoperative subjective pain status showed that patients with an ISB had significantly lower values and required less additional analgesia. In both groups the Constant score was significantly higher 6 months after surgery, compared to the preoperative condition. Compared to the control group, patients treated with ISB were clearly more satisfied with the postoperative pain management. CONCLUSION: By implementing ISB sufficient analgesia in the early postoperative period after open shoulder surgery is attained, allowing for early physiotherapy. This positively influences convalescence and the outcome of the surgical procedure. Furthermore, patients are visibly more satisfied with the postoperative pain management.
Acromion↗
[Invasive chondrosarcoma of the thoracic spine as a rare cause of acute paraplegia].
We report on the case of a invasive chondrosarcoma of the thoracic spine in a 65-year-old woman as a rare cause of acute paraplegia.
Acute Disease↗
[Sacral fracture as a rare early complication of lumbosacral spondylodesis].
A 57 year old patient with secondary cortisone induced osteoporosis war surgically treated by means of posterior lumbar interbody fusion with internal fixation from L4-S1 for symptomatic instability in the level L4/5 after previous dorsal stabilisation L5/S1. After an unapparent initial postoperative phase, the patient complained of severe pain in the low back and gluteal region 9 day after surgery. Radiographs as well as CT-scans showed a horizontal fracture of the sacrum. After a short period of immobilisation the patient was carefully remobilised with an orthesis and the pain gradually subsided. Conventional radiographs one year later showed complete consolidation of the fracture and a good clinical result. There are only two literature reports with together 3 cases of patients attaining an early sacral fracture after spondylodesis. The main cause seems to be the unphysiological biomechanical stress placed on the osteoporotic sacrum after moresegmental spondylodesis. Further risk factors seem to be adipositas, female gender and age. Despite the rarity of sacral fractures after lumbosacral fusion, this complication should at least be considered in the differential diagnosis in patients who complain of persisting or sudden-onset pain after surgery.
Female↗