Isosteric replacement of functional groups is an emerging strategy for optimizing bioactive molecules in drug discovery. -Butyl group is a particularly important moiety, yet its isosteric replacement with 1-trifluoromethyl-cyclobutyl group has been rather neglected. To enable the advance of this molecular fragment in drug discovery programs, we report the synthesis of over 30 small-molecule building blocks featuring the trifluoromethyl-cyclobutyl fragment, achieved by reacting sulfur tetrafluoride with cyclobutylcarboxylic acids on a gram-to-multigram scale.
View Article and Find Full Text PDFFragments of two skulls of young cetotheriid baleen whales were described from the Fortep'yanka 2 locality (Russia, Republic of Adygea, Maikop district, Fortep'yanka River valley, Upper Miocene, Upper Sarmatian, Blinovskaya Formation). The finds were attributed to Kurdalagonus maicopicus (Spasskii, 1951) based on the morphology of the posterior (mastoid) process of the petrosal bone, the structure of the posterior edge of the temporal fossa, and the S-like shape of the supraoccipital ridges. The skull proportions and the degree of suture closure made it possible to determine the individual age of the whales within a year.
View Article and Find Full Text PDFObjective: The aim: to investigate the morphometric characteristics of placentas in women with comorbidity of preeclampsia and obesity compared to women with physiological body weight, and to assess the efficacy of the prophylactic therapy course developed to prevent the occurrence of preeclampsia in pregnant women with obesity.
Patients And Methods: Materials and methods: 25 biopsy samples of placental tissue were taken from women between 37 and 40 weeks of gestation with a physiological body weight and with class II obesity. The women were divided into five groups of five women in each: the 1st group included women with physiological body weight without obstetric and somatic pathology; the 2nd group involved women with physiological body weight, whose pregnancy was complicated with preeclampsia; the 3rd group was made up of women with class II obesity whose pregnancy was complicated with preeclampsia; the 4th group consisted of women with class II obesity, who received the special prophylactic therapy course, and the 5th group included women with class II obesity, who did not receive the prophylactic therapy course.
Coprolites of the seal Pachyphoca volkodavi from the Upper Miocene deposits (Kherson) of the Fortepyanka locality (Republic of Adygea) were studied. Two out of five seal coprolites contained a structure resembling fish muscle tissue and included objects with morphology of trematode metacercariae. Obviously, the larvae of the parasite got into the digestive tract of seals from the fish they ate.
View Article and Find Full Text PDFCF-cyclopropanes with aliphatic, aromatic, and even heteroaromatic substituents were prepared on a multigram scale by deoxyfluorination of cyclopropane carboxylic acids or their salts with sulfur tetrafluoride. For labile α-pyridine acetic acids, only the use of their potassium salts allowed to obtain the needed products. Derivatization of CF-cyclopropanes into building blocks ready for direct use in medicinal chemistry was performed.
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