Cyclenes

Nach dieser Methode werden einige bicyclische Amino-ketone in hohergliedrige Mono-cyclen umgewandelt z.B. 1-Oxo-chinolizidin zum 5-Hydroxy-azacyclodecan (59% d.Th.) bzw. 1-Oxo-octahydropyrrocolin zum 4-Hydroxy-az.acyclononan (48% d.Th.)2 ... 

Norinyl (Searle) Ortho-Cept (Ortho-McNeil Pharmaceutical) Ortho-Cyclen (Ortho-McNeil Pharmaceutical) Ortho Novum (Ortho-McNeil Pharmaceutical) Ortho-Tri-Cyclen (Ortho-McNeil Pharmaceutical) Ovral (Wyeth-Ayerst) Tri-Levlen (Berlex) Tri-Norinyl (Searle) Triphasil (Wyeth-Ayerst)... 

Fig. 6.7 Complex between 9mer peptide-cyclen conjugate and 31mer RNA as a model oflAR-RNA in HIV-1 infection as reported by Michae-lis and Kalesse [48]...

N3-coordination by monomeric and dimeric Zn2+-cyclen derivatives has also been shown to both inhibit the photo [2+2] cycloaddition of thymidilyl(3 -5 )thymidine, d(TpT), and to accelerate the photosplitting process of the [T-cis,syn-T] dimer (78% after 1 h of UV exposure) (38). 

Fig. 7. A Zn21 -cyclen derivative (3) with coordinated captopril, and molecular structure of a Znn(cyclen)-N3 bound 1-MeT.

Fig. 8. Schematic for the micrococcal nuclease attack to (a) breathing ds-DNA, (b) dista-mycin-bound DNA, and (c) Zn2+-cyclen derivative-bound DNA. Arrows and dashed arrows, respectively, indicate successful and failed enzyme hydrolysis. Reproduced with permission from Ref. (37). Copyright 1999, American Chemical Society.

The Zn-N3imide interaction has been used to selectively extract imide-containing nucleosides and nucleotides into lipophilic media (39). Hexadecyl-derivatized Zn2+-cyclen was shown to extract dT from an aqueous solution containing a mixture of C, A, and G nucleobases. The antiviral agent AZT (3 azido-3 deoxythymidine) could also be extracted into CHCI3 from neutral aqueous solutions. Transport across a lipophilic layer was also shown, using acidic conditions, to promote the release of dT and AZT (Fig. 9). 

Albuterol (salbutamol) metered-dose inhaler as needed Ortho-Tri-Cyclen Lo by mouth daily Echinacea 1 to 2 tablets by mouth daily as needed Multivitamin 1 tablet by mouth daily... 

Along with varying doses of ethinyl estradiol and different prog-estins, there are also formulation modifications that may benefit various patient situations. These formulations include products such as Seasonale , Ortho Tri-Cyclen , Estrostep Fe , Yasmin , Mircette , and Ovcon 35 . Each of these products may show benefit in certain women owing to their unique characteristics. 

Ortho Tri-Cyclen (norgestimate/ethinyl estradiol) and Estrostep Fe (norethindrone acetate/ethinyl estradiol) both have an approved indication for treatment of moderate acne vulgaris in females 15 years of age or older desiring contraception who have failed topical antiacne medication. 

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