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Sydnone derivatives with various substituents at C-4 of the phenyl ring and at C-2 of the thiazolyl ring were synthesised and tested for antiinflammatory activity. Five compounds have shown promising results. Synthese und entziindungshemmende Wirkung 3-subslituierter 4-(4'-Thiazolyl)-SydnoneSydnonderivate mit verschiedenen Substituenten in 4-Position des Phenyl-und 2-Position des Thiazolylringes wurden synthetisiert und auf entziindungshemmende Wirkung getestet. Fiinf der untersuchten Verbindungen zeigen vielversprechende Ergebnisse.Varied types of biological activities have been claimed for the mesoionic compounds. Sydnones, in particular have been studied for antibacterial, antitumour, antifungal, antimalarial, antiparasitic, analgesic, antiinflammantory, coccidiostatic, diuretic, hepatotoxic, and insecticidal activities').Various disubstituted 3-phenylsydnones2), sydnone 4-sulphonamides3), and 3-pyrazolyl phenyl sydnones4), have been synthesised in this laboratory and are shown t o possess considerable activity. Encouraged by these reports, it was planned t o introduce a thiazolyl moiety in 4-position of the 3-phenyl sydnone and t o subject these thiazolyl sydnones for biological evaluation.It may b e pointed out here that only two sydnones with thiazolyl moiety in 4-position have been reported5). However they have not been subjected for biological evaluation.Various 4-thiazolyl-3-phenyl sydnones with substitution in both, thiazolyl and phenyl ring have been synthesised and subjected for biological evaluation.T h e sydnones have been prepared (Table 1) by the literature methods as shown in the scheme. Acylation has been carried o u t with acetic acid and phoshorous pentoxide in benzene, following the method of Greco et a1.6). T h e ketones are then broniinated and further condensed with t h i o u r e a 8 to yield the desired compounds.Somc selected sydnones have been subjected t o antiinflammatory studies. They have been studied f o r acute toxicity test and were found t o b e non-toxic even at a dose of 400 mg/kg. T h e method used for screening o f these compounds is that according t o Winter e t al.7).

A new "polystyrene biotin support" has been synthesized for the solid support synthesis of the 3'-biotinylated oligonucleotides. Several oligos were synthesized and were analyzed by the HPLC and Mass Spec. Oligo analysis revealed that the biotin gets oxidized to "biotin sulfoxide" during the synthesis.

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