Propoxy analogs

Because the 1% sucrose solution is equisweet with the propoxy analog, therefore,... 

The introduction of a 14-alkoxy instead of the 14-hydroxy group present in NTI resulted in somewhat lower binding affinity at the 8-receptor, while 8-receptor selectivity was considerably increased (compounds 74-81) (Table 8). The nature of the substituent in position 14 was reported to be an important determinant for the interaction with 8-receptors. A 14-ethoxy group in indolomorphinans seems to be superior to 14-methoxy and 14-propoxy substitution concerning 8-affinity and selectivity. The presence of a 14-ethoxy group (compounds 74, 76, and 78) resulted in higher affinity and selectivity for the 8-receptor compared to their 14-methoxy-substituted derivatives 73, 75, and 77, respectively, and 14-propoxy analog 79... 

Contrary to propoxy analogs, cyclobutoxy amides displayed high permeability and brain penetration properties as illustrated in Table 18.11. Once again, the impact of the simple cyclobutyl constraint on both H3 affinities (10-30x increase) and brain receptor occupancies proved to be unique and led to a very quick optimization cycle (see Table 18.11, comparison between propoxy and cyclobutoxy derivatives) [57]. 

Refer to [1378,1379] (this compound is a 2-propoxy analog of griseophe-none B). 

As predicted, the C2,C2 -isopropoxy and propoxy groups are more potent than the corresponding methoxy (0.8 and 1.5 pM vs. 6.4 pM). In addition, C3,C3 -substitution has an effect on both the potency and photopotentiation factor. Although the absorption at 670 nm was improved with C3 substitution, the potency against PKC decreased for analogs 90, 92, and 97. 

A similar phenomenon has been observed in the spectra of some diene-iron tricarbonyl compounds (136). The anisolechromium tricarbonyl complex shows loss of 2 H from the [M - 3 CO]+ ion, giving C7H6OCr+, which could have the tropone structure (XIV) while the analogous iso-propoxy complex loses propylene with the probable rearrangement to give... 

The lack of effect of available nucleoside analogs on cytomegalovirus (CMV) infection led to the synthesis of the acyclovir analog, ganciclovir [gan SYE kloe ver] (9-[(1,3-dihydroxy-2-propoxy)methyl]guanine, DHPG). It is currently available for treatment of cytomegalic retinitis in immunocompromised patients. 

Recent progresses in total synthesis of (-b)-biotin 12CJ01792. Surveying the effects of eldecalcitol (1 a,25-dihydroxy-2p-(3-hydroxy-propoxy)vitamin D3) and related analogs from a biological perspective 12H(86)69. 

As already briefly mentioned earlier, simple propoxy aryl amides were known [39] but in our hands, proved to be poorly brain-penetrant Synthesis of a limited munber of cyclobutoxy analogs was straightforward and a quick amine scan was performed [57]. 

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