Bio-orthogonal chemistry has been widely used for conjugation of polymer molecules to proteins. Here, we demonstrate the conjugation of polyethylene glycol (PEG) to bovine beta-lactoglobulin (BLG) by photo-induced cyclo-addition of tetrazole-appended PEG and allyl-modified BLG. During the course of the investigation, a significant side-reaction was found to occur for the conjugation of PEG-tetr...

A series of potentially active quinoline based azetidinones and thiazolidinones analogues has been synthesized by simple and efficient synthetic protocol. The tetrazole nucleus formed from 2chloroquinoline-3-carbaldehyde using p-toluenesulphonic acid and sodium azide followed by reaction with various substituted amine to form the corrosponding schiff base intermediates. Attempt made to derive f...

We have used the Chemical Structure DataBase (CSDB) of the NCI CADD Group, an aggregated collection of over 150 small-molecule databases totaling 103.5 million structure records, to conduct tautomerism analyses on one of the largest currently existing sets of real (i.e. not computer-generated) compounds. This analysis was carried out using calculable chemical structure identifiers developed by ...

The decomposition of 5-benzhydryl-1H-tetrazole in an N-methyl-2-pyrrolidone/acetic acid/water mixture was investigated under a variety of high-temperature reaction conditions. Employing a sealed Pyrex glass vial and batch microwave conditions at 240 °C, the tetrazole is comparatively stable and complete decomposition to diphenylmethane requires more than 8 h. Similar kinetic data were obtained ...

Heterocyclic nucleic acid bases and their analogs can adopt multiple tautomeric forms due to the presence of multiple solvent-exchangeable protons. In DNA, spontaneous formation of minor tautomers has been speculated to contribute to mutagenic mispairings during DNA replication, whereas in RNA, minor tautomeric forms have been proposed to enhance the structural and functional diversity of RNA e...

Development of a new improved and efficient process suitable for the large-scale production of Irbesartan has been described. The key steps are tetrazole formation from secondary amide for the preparation of the key intermediate 1-Benzyl-5-(4'-bromomethyl-biphenyl-2-yl)-1H-tetrazole (9), N-alkylation and debenzylation.

A new activator for the coupling of phosphoramidites to the 5'-hydroxyl group during oligonucleotide synthesis is introduced. The observed time to complete coupling is twice as fast with 4, 5-dicyanoimidazole (DCI) as the activator, compared with 1 H -tetrazole. The effectiveness of DCI is thought to be based on its nucleophilicity. DCI is soluble in acetonitrile up to 1.1 M at room temperature...

New (tetrazol-5-yl)methylindole derivatives were synthesized from 2-phenylindole. Furthermore, the sugar acetyl hydrazones of the tetrazole derivatives as well as their derived acyclic C-nucleoside analogs were prepared. The synthesized compounds were studied for their anticancer activity against human liver carcinoma cell line (HepG2) and the results showed that arylidine substituted tetrazole...

A 405 nm light-activatable terthiophene-based tetrazole was designed that reacts with a fumarate dipolarophile with the second-order rate constant k2 exceeding 10(3) M(-1) s(-1). The utility of this laser-activatable tetrazole in imaging microtubules in a spatiotemporally controlled manner in live cells was demonstrated.