Polyketide-derived macrolactones like zearalenone (1), zearalane (2) or curvularin (3) display a wide range of interesting pharmacological activities. Here, we present a short and efficient approach towards this class of natural products by a combination of the Sonogashira and Mitsunobu reactions. The resulting lactone 9 was tested against human cancer cell lines at the NCI.
The new IHS classification describes under the paragraph 7.2.3 the headache attributed to spontaneous low CSF pressure. We report on four patients with such a headache and discuss the probable pathophysiology, including results published in the literature. It seems that not the low CSF pressure itself is the cause for the headache but the unphysiological, increased vasodilatation of intracranial and epidural veins. This dilatation of veins also shows up in the typical radiological findings with meningeal contrast enhancement and enlarged epidural veins. A trial with caffeine, theophylline, or indomethacin is recommended; otherwise, the most effective treatment option is an epidural blood patch, which is effective also in the absence of a documented CSF leak.
Short and Efficient Approach Towards Macrocyclic Lactones Based on a Sonogashira Reaction. -Title compounds (V) and (VIII) are obtained by a combination of Sonogashira and Mitsunobu reactions. The macrolactone (V) is tested against human cancer cell lines but does not show significant cytotoxic activities. -(KRAUSS*, J.; UNTERREITMEIER, D.; NEUDERT, C.; BRACHER, F.; Arch. Pharm. (Weinheim, Ger.) 338 (2005) 12, 605-608; Inst. Pharm., Zent. Pharmaforsch.,
Niphathesine C and related pyridine alkaloids are well known natural products with interesting antimicrobial activities, characterized by a pyridine ring and a lipophilic side chain with a terminal nitrogen-containing functional group. This paper describes the synthesis of analogues of these alkylpyridine alkaloids with variation of the heterocyclic ring and the terminal functional group. Key steps of the syntheses are a Sonogashira reaction of appropriate aryl iodides with undec-10-ynol or undec-10-ynoic acid derivatives. The resulting compounds were tested in an agar diffusion assay against several bacteria and fungi.
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