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Titolo:
THE SYNTHESIS AND IN-VITRO EVALUATION OF A (99M)TECHNETIUM-NITROIMIDAZOLE COMPLEX BASED ON A BIS(AMINE-PHENOL) LIGAND - COMPARISON TO BMS-181321
Autore:
RAMALINGAM K; RAJU N; NANJAPPAN P; LINDER KE; PIRRO J; ZENG W; RUMSEY W; NOWOTNIK DP; NUNN AD;
Indirizzi:
GUILFORD PHARMACEUT,6611 TRIBUTARY ST BALTIMORE MD 21224 BRISTOL MYERS SQUIBB PHARMACEUT RES INST PRINCETON NJ 08543
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 24, volume: 37, anno: 1994,
pagine: 4155 - 4163
SICI:
0022-2623(1994)37:24<4155:TSAIEO>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
AMINE-PHENOL LIGANDS; ENDOTHELIAL-CELL MONOLAYERS; IMAGING HYPOXIC TISSUE; BLOOD-BRAIN-BARRIER; TECHNETIUM COMPLEXES; H-3 MISONIDAZOLE; BINDING; INVITRO; INVIVO; MARKER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
K. Ramalingam et al., "THE SYNTHESIS AND IN-VITRO EVALUATION OF A (99M)TECHNETIUM-NITROIMIDAZOLE COMPLEX BASED ON A BIS(AMINE-PHENOL) LIGAND - COMPARISON TO BMS-181321", Journal of medicinal chemistry, 37(24), 1994, pp. 4155-4163

Abstract

We have developed a (99m)Technetium complex for imaging of hypoxic tissue (BMS-181321). Recently, another nitroimidazole derivative, based upon a bis(amine-phenol) ligand, was described in the patent literature. To compare this compound to BMS-181321, we have synthesized the ligand, prepared its Tc-99m complex, and evaluated its performance in twoin vitro assays of bioefficacy: membrane permeability and uptake in normoxic and anoxic cardiocytes. In attempting to reproduce the synthesis of the ligand described in the patent application, we found that one intermediate could not be made by the method described, and alternative routes were investigated. Complexation of the bis(amine-phenol) nitroimidazole with Tc-99m gave an apparent single complex; this appeared as a broad peak on HPLC analysis. Purification by a solid-phase method gave a complex with 95% radiochemical purity. This complex was not permeable to cultured bovine brain endothelial cells nor did it show preferential uptake in anoxic myocytes.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 11:32:25