Dual ACC1 / ACC2 Inhibition

9,10-anthraquinone to anthrone [76] was used in order to obtain similar substituted molecule from 4a. It was found that this reaction leads not only to the reduction but also to a simultaneous protection of the alcoholic function with an acetyl group. Resulting compound 4b was expected to appear in the form of two isomers: 3-(9-oxo-9,10-dihydroanthracen-2-yl)propyl acetate

9-anthraldehyde and (carbethoxymethylene)triphenylphosphorane were reacted together using the Wittig reaction to produce E-3-(9-Anthryl)-2-propenoic acid ethyl ester. .100 g of 9-anthraldehyde and .180 g of (carbethoxymethylene)triphenylphosphorane were used. 9-anthraldehyde was a green powder while (carbethoxymethylene)triphenylphosphorane was a white powder. Both were added together into a 3.00 mL conical vial with a magnetic spin valve. The vial was inserted into a 120 C sand bath to melt the reagents. Once the reagents melted, they were stirred for 15 minutes (2:30 pm-2:45 pm). After stirring, the vial was removed to cool to room temperature. 3.00 mL of hexanes were added to the vial and the suspension was stirred. The solvent was removed

NMR: NMR analysis was done on the product. The reactant NMR is also shown for comparison purposes. Coloring is used to assign peaks to specific hydrogens. Highlighted carbons are indicative of the hydrogen(s) attached to the respective carbon. The NMR results are shown in Table 2. A spectrum was also run on the adduct.

Based on the Rf value for unknown, aspirin, acetaminophen, ibuprofen, salicylamide, and caffeine were 0.2612, 0.2581, 0.0476, 0.5714, 0.3, 0.0714. The second hypothesis was like initial hypothesis that the possible components contain in the unknown drug were aspirin, and salicyamide, the possible drug was aspirin, but cannot for sure what the unknown was. Because the drug that contain salicylamide, but didn’t contain the caffeine component which didn’t show up in this case. The drugs list in the chart, none of the drug contains the component aspirin, and salicyamide at the same time. Based on the Rf value and the observation, the lab experiment wasn’t accurate and some error was occurred during the lab period.

This information is useful so that pharmaceutical researchers can understand the enzyme interactions between these drugs and the enzymes in the brain and know what to include in the new drugs they design and synthesize. Therefore, the ultimate goal of this study is to evaluate the 3D chemical structures of each of these drugs in comparison with the active sites of the enzymes they work on in order to determine what factors of the current drugs have that leads to the best enzyme interaction in order to prevent seizures in epilepsy patients in the

As seen in the results, ACh has specificity to methacholine, which is due to the similarity of their shape and size, with the only variance being an extra methyl group on the central carbon in the methacholine. In spite of this, methacholine is not as efficiently hydrolysed as ACh, as ACh has a flexible carbon backbone that allows it to bind and be hydrolysed by both AChE and BChE (Rang and Dale, 2013). The stability of carbachol to hydrolysis can be accounted for by the amino group attached to the acetyl end of the molecule, rather than a methyl group that is at the end of ACh. BChE can hydrolyse ACh, however AChE cannot hydrolyse BuCh, as BChE possesses a butyryl group at the acetyl end of the molecule which produces a longer chain than that of ACh making AChE specific for smaller molecules. AChE has a smaller active site than BChE due to the fact that ACh is lacking in two amide residues, preventing the binding of some substrates to Ach (Cokugras, 2003). The structure of a suxamethonium molecule resembles a BuCh and ACh molecule attached together, and ultimately this should have had an effect as it is specific to BuChE, however this did not occur. There is a possibility that the lack of reaction between BuChE and suxamethonium could be a consequence of contamination of the wells with another substance, using the wrong substance or no substance added at

To a solution of o-aminoester 1 (0.9 g, 3 mmol) in DMSO (5 mL), carbondisulfide (0.3 mL), saturated sodium hydroxide (0.2 mL) and dimethyl sulfate (0.5 mL) were added. The mixture was stirred overnight (TLC showed complete conversion). The precipitate that formed was filtered off, washed with ethanol and crystallized from methanol to give compound 3 as yellow crystals (0.72 g, 62%); mp: 168-169oC; 1H-NMR (400 MHz, DMSO-d6): δ 1.21 (t, 3H, J ¬= 7.1 Hz, COOCH¬2¬CH-3), 1.32 (t, 3H, COOCH¬2¬CH¬3), 2.80 (s, 3H, CH¬3), 2.82 (t, 2H, J ¬= 6.5 Hz, H-4), 3.62 (t, 2H, J¬ = 6.5 Hz, H-5), 4.03 (q, 2H, J = 7.2 Hz, COOCH¬2¬CH¬3), 4.08 (bs, 1H, NH), 4.30 (s, 2H, H-7), 4.53 (q, 2H, J = 7.2 Hz, COOCH¬2¬CH¬3); 13C-NMR (100 MHz, DMSO-d6): δ 14.2 (CH3), 22.8 (C-4),

The ring activating reactants were electron donating because they had electron lone pairs and therefore reacted faster. The reactants that were ring deactivating reacted slower because of they were attached to electron withdrawing groups. The reaction order from fastest to slowest was as predicted with phenol being the fastest, then anisole, 4-bromophenol, acetanilide, and diphenyl ether being the slowest due to the electron withdrawing group joined to it. These outcomes are constant with the concepts of ring activating and deactivating functional

In order to determine the major product of the alkylation, an NMR test was run to figure

Comparing with the literature value5 range between 45-65 ppm, signal 3 corresponds with O-CH2 group. Signal 3 was downfield and deshielded comparing with signals 4,5,6, and 7 because it was directly bonded to the oxygen electronegative atom. It can be concluded that signal 3 is a CH2 group connected to the ester group. According to the13C NMR spectrum, signals 4, 5, and 6 were very similar and the three of them were upfield and shielded because of the weak magnetic field applied around them. Signal 4, 5, and 6 had an observed ppm values of 28.253 ppm, 28.248 ppm, and 22.533 ppm respectively and a calculated ppm values10 of 28.5 ppm, 28.3 ppm and 22.4 ppm respectively. Comparing with the literature ppm value5 range 13-35 ppm, signal 4, 5 and 6 corresponds with R-CH2-R group. It can be concluded that signals 4, 5 and 6 are part of CH2 groups. Lastly, signal 7 had an observed ppm value of 14.163 ppm and a calculated ppm value10 of 14.0

The dose-response curve in the presence of antagonist shows it effect on the ileum smooth muscle contraction which increases rapidly after 5 minutes exposure to atropine at a constant concentration of 3 x 10-7 M. The dose-response curve in the absence of antagonist shows it effect on the ileum smooth muscle contraction which increases rapidly on 3 minutes exposure to acetylcholine with the interval of 20 seconds between all doses at the concentration of 1 x 10-8 M to 1 x 10-4 M for every 3-2 doses. Also, as shown in figure 1, dose-response curve in the absence of antagonist has a higher contraction than the dose response curve in the presence of antagonist.

The S1-C8 distance of 1.7600(2) Å is normal single bond values and conforms to those observed in other sulfonamides [29]. The torsion angle C-S-N-C defining the conformation of the sulfonamide group is reported to lie in the range 60-90o

Adriamycin may cause severe and possibly life-threatening heart problems such as myocardial oxidative injury as well as the apoptosis of myocardial cells it found that Astragaloside IV can suppress these effects induced by Adriamycin(2003;Li et al.,2006). These findings showed that the mechanisms of action of Astragaloside IV against myocardial damage may be

Firstly, dipyridamole inhibits platelet, epithelial cells and erythrocyte uptake of adenosine. When the therapeutic concentration of dipyridamole reaches 0.5-1.9μg / dl, the inhibitory effect of dipyridamole will have a dose-dependent manner. Because of this, the local adenosine concentration increases to act on the A2 receptor of platelet for stimulating adenylate cyclase. Which result in increased

Costin T. A. et al., (2017) designed a series to show the reactivity of a diazobketo esters with primary amines of linear structure, it was reported that n-butylamine and allylamine are potent nucleophiles for the acyl cleavage of a-diazo-b-keto esters having electron withdrawing groups at respective position, such as azido and chloro , giving to the corresponding amides (71) in high