The Staudinger ligation between an azido-protein and a phosphinothioester-derivatized surface is demonstrated to be an effective means for the site-specific, covalent immobilization of a protein. Immobilization yields of >50% are obtained in <1 min, and immobilized proteins have >80% of their expected activity. No other method enables more rapid immobilization or a higher yield of active protei...

Two light-sensitive analogs of 2,4-dichlorophenoxyacetic acid, namely 4-azido-2-chlorophenoxyacetic acid and 3-azido-5-chlorophenoxyacetic acid, have been synthesized for use as auxin photoaffinity labels. The preparation and biological activity of the compounds are described. Both contain the photolabile azido group; the 2,4-substituted compound shows auxin activity and the 3,5-substituted com...

The aggregating effect of ADP on human platelets and the inhibiting effect of adenosine are apparently mediated by different receptors on the cells’ outer membranes. Photolysable azido-analogues of adenosine, AMP and ADP have been prepared so tha t the receptors for them can be labelled. 2-Azidoadenosine inhibited platelet aggregation by ADP more than adenosine itself and increased platelet cAM...

A novel type of zwitterionic HILIC stationary phase was prepared by covalently bonding the l-azido lysine on silica gel via click chemistry. The key intermediate azido lysine was synthesized by transformation the amino group in l-Boc-lysine to corresponding azido group and subsequent removal of the N-protected group (Boc). Finally, the azido lysine was covalently bonded to silica beads by click...

The iodination of organic compounds is great importance in synthetic chemistry. It opens comprehensive approaches for the synthesis various biologically active compounds. recent advances using elemental iodine or iodides, covering last thirteen years, are objective present review.

Direct iodination of morphine or dihydromorphine with iodine-125 results in products that bind to antibody raised by immunization of animals with a 3-O-carboxymethylmorphine/bovine serum albumin immunogen. Iodination of morphine or dihydromorphine with iodine-127 under identical conditions failed to yield these immunologically active products, suggesting that the results obtained with iodine-12...

An NH2CN-promoted convergent integration of three self-sorting domino sequences is described for the construction of 6-iodo-3-methylthioimidazo[1,2-a]pyridines from aryl methyl ketones and 2-aminopyridines. This strategy allows the construction of an imidazo[1,2-a]pyridine ring along with methylthiolation at C-3 and iodination at C-6. Preliminary mechanistic studies indicate that this process t...

Thyroid tissue obtained from 12 patients with Graves' disease and treated with thionamide drugs for 3-7 mo before subtotal thyroidectomy, from 12 patients with Graves' disease, similarly treated, and given 50 mug of triiodothyronine (T3) for 10 days before surgery, and from 12 euthyroid patients with solitary cold nodules was investigated to compare in vitro iodination of thyroglobulin in toxic...