The combination of 1-hydroxy-tetrazole and 1-hydroxy-1,2,4-triazole produces a new bisheterocyclic moiety, which is characterized derivatized extensively. We tried to combine the positive advantages TKX-50 MAD-X1 backbone with this building block.

Eight different derivatives of substituted 5-phenyl-1-(5-substituted phenyl) -4,5-dihydro1H-pyrazol-3-yl)-1H-tetrazole (4a-h) were synthesized by reacting the chalcones with hydrazine hydrate in presence of glacial acetic. The chemical structures were confirmed by means of FT-IR, H-NMR, mass spectra and elemental analysis. The compounds were screened for analgesic activity by acetic acid induce...

Only few efficient methods for the preparation of polyazoles containing three or four nitrogen atoms in each azole cycle exist. We have developed a novel synthetic strategy that allows sequential assembly 1,2,3-triazole, 1,2,4-triazole, and tetrazole fragments into new stable polyazole. Along strategy, some known procedures been optimized to achieve better conversion, selectivity, and, general,...

A diastereo- and enantioselective aldol reaction between aldehydes and a synthetically useful ketomalonate 1c as a hydrated form was developed, and either anti- or syn-aldol adducts having a chiral tetrasubstituted carbon center were obtained in high enantioselectivities by use of a tetrazole analogue of L-proline (S)-2 or an axially chiral amino sulfonamide (S)-3 as catalyst.

Ammonia in the tetrazole Ugi variation together with α-amino acid methyl ester-derived isocyanides provides tetrazolopiperidinones in good to high yields in one pot. The scope and limitations of this reaction were investigated by performing >70 reactions. The scaffold is useful to fill high-throughput screening decks and in structure-based drug design.

Rh(III)-catalyzed direct olefination reaction via aromatic C-H bond activation is described using tetrazole as the directing group. This reaction provides a straightforward way for the synthesis of ortho-alkenyl aryl tetrazoles. Various functional groups tolerate the reaction conditions and afford the corresponding products in moderate to excellent yields.

A structure-based virtual screening protocol was used to predict Mycobacterium tuberculosis shikimate kinase (MtSk) inhibitors. Docking simulations were performed using eHiTS software and 644 drug-like compounds were identified as potential inhibitors. Forty-two percent of such inhibitors had a structural relationship to a triazole or a tetrazole heteroaromatic system which may provide a candid...