Straightforward synthesis of labeled and unlabeled pyrimidine d4Ns via 2 ',3 '-diyne seco analogues through olefin metathesis reactions

The synthesis of dideoxynucleosides (ddNs) or didehydro-dideoxynucleosides (d4Ns) from nucleosides has been extensively reviewed. While previously described methods are based on the modification of the 2'- and/or T-OH group of the intact ribose moiety, the use of a ring-closing metathesis (RCM) for the formation of the unsaturated cyclic system of nucleosides could be a straightforward approach to the d4Ns. Thus, as part of our drug labeling program, this paper reports a straightforward synthesis of 2',3'-didehydro-2',3'-dideoxyuridine (d4U) and [1',2',3',4',5'-C-13(5),6-C-13,1,3-N-15(2)]d4T using the RCM protocol. This paper discusses the preparation of nucleoside dienes and the activity of ruthenium-based metathesis catalysts. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).status: publishe

Sinteza, antibakterijsko i potencijalno anti-HIV djelovanje nekoliko novih analoga imidazola

A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylamino-propan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy]ethyl}-1H- imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.Sintetizirana je serija 1-(2-metil-4-nitro-imidazol-1-il)-3-arilamino-propan-2-ona (2a-e), 2-metil-5-nitro-1-{2-[arilmetoksi]etil}-1H- imidazola (5a-d) i N-(3-hidroksifenil)-2-(supstituiranih imidazol-1-il)alkanamida (8a-e) s ciljem dobivanja novih derivata imidazola sa širokim kemoterapijskim svojstvima. Navedeni spojevi ispitani su na anti-HIV i antibakterijsko djelovanje