WebThe four azaindole positional isomers, which associate a pyridine and a pyrrole ring by a fused C-C bond, possess all of the criteria necessary to be excellent bioisosteres of the indole or purine systems. These three entities only differ by the substitution of a sp 2 CH fragment by a sp 2 nitrogen atom and vice versa.

Bioisosteres of the Phenyl Ring: Recent Strategic Applications in …

Web1. feb 2005 · In this paper, we will discuss bioisosterism as a strategy of molecular modification, showing its importance in building a new series of congeners compounds designed as candidate of new drugs,... Web21. mar 2011 · An excellent J.Med.Chem. perspective titled 'Synopsis of Some Recent Tactical Applications of Bioisosteres in Drug Design' has just published (The article is based on a short course presented at an ACS Prospectives conference in 2009). The author gives a brief introduction to the concept of biosisosterism (classical and non-classical) but … gerald ford school of public policy ranking

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WebSince it was found that the thienylethylamine moiety might act as a dopamine receptor pharmacophore, we tested whether a thiophene moiety may act as a bioisostere for a phenol in 2-aminotetralins and hexahydronaphthoxazines. Therefore, thiophene analogues of the 2-aminotetralins and hexahydronaphthoxazines, 34-39 were synthesised. Web13. okt 2015 · An enantioselective dearomatization of indole derivatives was realized by the complexes derived from the vanadium complex VO(acac) 2 and C 2-symmetric bis-hydroxamic acid (BHA) ligands. The reaction proceeded via asymmetric epoxidation and ring-opening by the linked phenol cascade, affording 5a,6,10b,11-tetrahydrochromeno[2,3- … Web19. sep 2016 · Ziemer, Kerr reported that increased level of phenols and decreased level of indoles were detected after 8 weeks of storage, which correlated with a decrease in the pH. Phenols are formed at low pH, but indoles are accumulated at high pH [42–44]. Therefore, decreased level of phenols and consistently high indoles level might relate to ... gerald ford recent highlights