Tse, Edwin G.; Houston, Sevan D.; Williams, Craig M.; Savage, G. Paul; Rendina, Louis M.; Hallyburton, Irene; Anderson, Mark; Sharma, Raman; Walker, Gregory S.; Obach, R. Scott; Todd, Matthew H. published the article 《Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials》. Keywords: structure phenyl bioisostere replacement preparation antimalarial.They researched the compound: 2-((1R,5S)-6,6-Dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethanol( cas:35836-73-8 ).Recommanded Product: 2-((1R,5S)-6,6-Dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethanol. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:35836-73-8) here.
The replacement of one chem. motif with another that is broadly similar is a common method in medicinal chem. to modulate the phys. and biol. properties of a mol. (i.e., bioisosterism). In recent years, bioisosteres such as cubane and bicyclo[1.1.1]pentane (BCP) have been used as highly effective Ph mimics. Herein, we show the successful incorporation of a range of Ph bioisosteres during the open-source optimization of an antimalarial series. Cubane (19) and closo-carborane (23) analogs exhibited improved in vitro potency against Plasmodium falciparum compared to the parent Ph compound; however, these changes resulted in a reduction in metabolic stability; unusually, enzyme-mediated oxidation was found to take place on the cubane core. A BCP analog (22) was found to be equipotent to its parent Ph compound and showed significantly improved metabolic properties. While these results demonstrate the utility of these atypical bioisosteres when used in a medicinal chem. program, the search to find a suitable bioisostere may well require the preparation of many candidates, in our case, 32 compounds
When you point to this article, it is believed that you are also very interested in this compound(35836-73-8)Recommanded Product: 2-((1R,5S)-6,6-Dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethanol and due to space limitations, I can only present the most important information.
Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics