Tse, Edwin G. published the artcileNonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials, SDS of cas: 622-40-2, the publication is Journal of Medicinal Chemistry (2020), 63(20), 11585-11601, database is CAplus and MEDLINE.
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
Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C2H2N4O2, SDS of cas: 622-40-2.
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