Hydrazino nicotinamide

The hydrazino nicotinamide (HYNIC) system (Fig. 11) developed by Abrams and co-workers [106] has been successfully used for preparation of... 

Figure 1 Images of rats with unilateral Staphylococcus aureus abscess in calf muscle, recorded at 0 (live minutes), 1,6, and 24 hours postinjection of Tc-labeled hydrazino nicotinamide-liposomes (A) and hexamethylpropyleneamine oxime-liposomes (B).

Figure 2 A true positive Tc-hydrazino nicotinamide-polyethylene glycol-liposome scintigram (left) and a false-negative In-labeled polyclonal immunoglobulin G scintigram right) of a patient with painful swelling and redness at the level of an old tibial fracture.

Figure 4 Anterior whole-body scintigram of a patient injected with O.lpmol/kg (left) and a patient injected with O.Spmol/kg (right) four hours postinjection of 740 MBq Tc-hydrazino nicotinamide-polyethylene glycol-liposomes.

Abrams MJ, Juweid M, tenKate Cl, et al. Technetium-99m-human polyclonal IgG radiolabeled via the hydrazino nicotinamide derivative for imaging focal sites of infection in rats. J Nucl Med 1990 31 2022. 

Tc(V) Hydrazino Nicotinamide (HYNIC) Derivatives. The introduction of the Tc(V)-HYNIC system (Schwartz et al. 1991) represents a milestone in the development of Tc-99m radiopharmaceuticals. Particularly, peptides have been labeled with very high specific activity (Edwards et al. 1999 a Harris et al. 1999 Rose et al. 1998). Since the HYNIC linker occupies only one coordination site, coligands such as tricine, ethylenediamine dia-cetic acid (EDDA), etc., may complete the coordination sphere of the metal (Babich et al. 2000 Edwards et al. 1999 b Ono et al. 2000) (Fig. 2.3.4). 

Tc-hydrazino nicotinamide (HYNIC) tricine derivatives with... 

Ono M, Arano Y, Mukai T, et al. (2001). Plasma protein binding of Tc-labeled hydrazino nicotinamide derivatized polypeptides and peptides. Nucl. Med. Biol. 28(2) 155-164. 

With Af-acyl or Af-sulfonyl hydrazines as nucleophiles, Zincke salts serve as sources of iminopyridinium ylides and ylide precursors.Reaction of the nicotinamide-derived Zincke salt 8 with ethyl hydrazino urethane 42 provided salt 43, while the tosyl hydrazine gave ylide 44 (Scheme 8.4.14). ° Benzoyl hydrazines have also been used in reactions with Zincke salts under similar conditions.Af-amino-1,2,3,6-tetrahydropyridine derivatives such as 47 (Scheme 8.4.15), which showed antiinflammatory activity, are also accessible via this route, with borohydride reduction of the initially formed ylide 46. ... 

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