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Microbial Biotransformations in the Production and Degradation of Fluorinated Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Cormac D. Murphy, Aoife Phelan
The number of fluorinated drugs has increased steadily from the mid-20th century, and this has reflected the advances in the synthetic methodologies in fluorine chemistry. Given the benefits that fluorine can bring to pharmaceutically active molecules, it is highly likely that the number of fluorinated drugs will continue to increase; in 2017, 8 out of the 29 small molecules approved by the FDA contained fluorine. The widespread inclusion of fluorine in drugs does come with an obvious environmental downside, since there is increasing awareness amongst regulatory bodies and environmental campaigners of the recalcitrance of some fluorinated compounds. Whilst microorganisms might degrade certain fluorinated compounds, for example those that have a fluorophenyl moiety that can be catabolised via established catabolic pathways, others are demonstrably non-biodegradable. In particular, compounds containing the trifluoromethyl group are very common in pharmaceuticals and agrochemicals, and these might be partially degraded to a metabolically dead-end compound, such as trifluoroacetic acid. Thus, it is incumbent that the environmental fate of fluorinated pharmaceuticals is properly investigated, and inevitably this involves assessment of microbial biotransformation, either in pure culture or in a microcosm.
Iodine for vegetable production and livestock breeding
Published in Tatsuo Kaiho, Iodine Made Simple, 2017
Halogens (fluorine, chlorine, bromine, iodine) have played an important role in the development of agricultural chemicals. In particular, chlorine has been widely used as an component of pesticides such as DDT (dichlorodiphenyltrichloroethane) and BHC (benzene hexachloride) (see the diagram). However, the use of chlorine-based agricultural chemicals have been discontinued in developed countries due to safety concerns. In recent years, the introduction of fluorine has shown to significantly change drug efficiency and properties, and the use of fluorine-based agricultural chemicals containing fluorine atoms and the trifluoromethyl group (CF3) have rapidly increased due to their high level of safety. Overall, 30% of all agricultural chemicals presently used are said to be fluorine-based. On the other hand, because iodine is comparatively costly compared to other halogens and in limited supply, hence there are fewer cases of use in agricultural chemicals.
Synthesis and evaluation of novel benzimidazole derivatives as potential anti bacterial and anti fungal agents
Published in Egyptian Journal of Basic and Applied Sciences, 2021
Vishwajeet Amarsingh Pardeshi, Sultan Pathan, Amit Bhargava, Narendra Singh Chundawat, Girdhar Pal Singh
As stated in antifungal activity section, compounds 3 m and 3 n were found to be the active derivatives against S. aureus, S. pyrogenes, E. coli, C. albicans, A. Clavatus with 16, 21, 18 and 16 μg/mL and 20, 25, 17 and 17 μg/mL MIC values, respectively. Thus, the main purpose of docking studies was to investigate the possible interaction of these compounds with enzyme. All inhibitors were docked [33] into the enzyme’s active site, and three-dimensional poses of the compounds are presented in Figure 3(A-B). The forecasted binding energies of the synthesized benzimidazole compounds are recorded in Table 4. The docking poses in Figure 4(A-C) the compound 3 n makes two hydrogen-bonding interactions at the enzymes active site (PDB ID: 1EA1), interactions came from the fluorine atom of the trifluoromethyl group with hydrogen atoms of ARG96 and GLN72 (F – – H-ARG96, 2.66 Å; F – – H-GLN72, 2.67 Å). This evidence confirmed that suitable functional groups on imidazole ring second position were necessary for better antifungal activities in designing the molecule. Similarly, as shown in Figure 5(A-C), compound 3 m, makes two hydrogen bonding interactions at the active site of the enzyme (PDB ID: 1EA1), interactions came from the two fluorine atoms of the trifluoro methyl group with hydrogen atoms of ARG96 and GLN72 (F – – H-ARG96, 2.41 Å; F – – H-GLN72, 2.54 Å). Thus, these results suggest that electron withdrawing groups play important roles in the antifungal activities of these tested compounds.
Structure elucidation capabilities on typical pharmaceutical drugs by new nuclear magnetic resonance technology: a 400 MHz high-temperature superconducting power-driven magnet NMR system
Published in Instrumentation Science & Technology, 2019
Maria Victoria Silva Elipe, Neil Donovan, Robert Krull, Donald Pooke, Kimberly L. Colson
The three compounds selected for this study contain fluorine as a trifluoromethyl group, which allowed us to obtain 19F NMR together with 1H and 13C NMR data to fully characterize their structures. Cinacalcet HCl, N-[(1R)-1-(naphthalen-1-yl)ethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine – hydrogen chloride (1/1), (Figure 1) is the API of commercial oral formulated tablets that were approved in 2004 by the US Food and Drug Administration (FDA) as Sensipar and by the European Medicine Agency (EMEA) as Mimpara to treat patients with secondary hyperparathyroidism (sHPT) with chronic kidney disease (CKD) on dialysis.[4–8] In addition, cinacalcet HCl was approved for the treatment of primary hyperparathyroidism and parathyroid carcinoma in 2008 by EMEA and in 2011 by FDA.
2-(4-Biphenylyl)-1,3,4-oxadiazoles: synthesis and mesogenic studies
Published in Liquid Crystals, 2018
Farid Fouad, David R. Davis, Robert Twieg
One way to reduce the number of hydrogen atoms in a molecule is to replace alkyl substituents with a partially or fully fluorinated alkyl group. Replacing the methyl group in A34 by a difluoromethyl or a trifluoromethyl group (compounds 41 and 42, respectively) resulted in the loss of mesogenity. Replacing the alkyl groups R’ = Me and R’ = Bu, in compounds A38 and A39 by the perfluoroethyl group (compound A50) reduced both the breadth and transition temperature of the smectic A phase (Table 5). The smectic A phase is still preserved for a number of branched and cyclo-alkyl derivatives as shown in Table 5. The importance of this finding is the potential structure modification incorporating asymmetric groups in making chiral liquid crystals, and the possibility of obtaining liquid crystals containing a reduced number of hydrogen atoms as IR transparent liquid crystals opening the door towards optical applications such as optical information processing, wavefront phase control of a semiconductor laser, microscopic optical imaging, and three-dimensional femtosecond processing [42–44].