In vivo pharmacokinetic analyses of placental transfer of three drugs of different physicochemical properties in pregnant rats was written by Mehta, Darshan;Li, Miao;Nakamura, Noriko;Chidambaram, Mani;He, Xiaobo;Bryant, Matthew S.;Patton, Ralph;Davis, Kelly;Fisher, Jeffrey. And the article was included in Reproductive Toxicology in 2022.COA of Formula: C43H51N3O11 This article mentions the following:
Although the use of medication during pregnancy is common, information on exposure to the developing fetus and potential teratogenic effects is often lacking. This study used a rat model to examine the placental transfer of three small-mol. drugs with mol. weights ranging from approx. 300 to 800 Da with different physicochem. properties. Time-mated Sprague Dawley (Hsd:SD) rats aged 11-13 wk were administered either glyburide, rifaximin, or fentanyl at gestational day 15. Maternal blood, placentae, and fetuses were collected at 5 min, 30 min, 1 h, 4 h, 8 h, 24 h, 48 h, and 96 h post-dose. To characterize the rate and extent of placental drug transfer, we calculated several pharmacokinetic parameters such as maximum concentration (Cmax), time to maximum concentration (Tmax), area under the concentration-time curve (AUC), half-life (t1/2), clearance (CL), and volume of distribution (Vd) for plasma, placenta, and fetus tissues. The results indicated showed that fetal exposure was lowest for glyburide, accounting for only 2.2% of maternal plasma exposure as measured by their corresponding AUC ratio, followed by rifaximin (37.9%) and fentanyl (172.4%). The fetus/placenta AUC ratios were found to be 10.7% for glyburide, 11.8% for rifaximin, and 39.1% for fentanyl. These findings suggest that although the placenta acts as a protective shield for the fetus, the extent of protection varies for different drugs and depends on factors such as mol. weight, lipid solubility, transporter-mediated efflux, and binding to maternal and fetal plasma proteins. In the experiment, the researchers used many compounds, for example, (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4COA of Formula: C43H51N3O11).
(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.COA of Formula: C43H51N3O11
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem