Ultrasound Accelerated Syntheis of Novel Benzimidazole Derived Chalcones as α-Glucosidases Inhibitor Agents

4d and 4e having electron withdrawing groups exhibited better activity against the bacterial strains Escherichia coli and Pseudomonas aeruginosa by showing the zone inhibition of 11-15mm at 12.5µg/mL and 36-40mm at 6.25µg/mL compared to standard, whereas, compound 4f bearing two phenyl groups attached to the nitrogen atom showed almost equal to the standard against the bacterial strain Staphylococcus aureus with the zone of inhibition of 30-35mm at 3.125 µg/mL (Fig 1, Table

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5 points Name 5 and only 5 ways to make the synthesis of a pharmaceutical compound more green that are presented on the poster.

Chemical antimicrobial agents are chemical compounds capable of either inhibiting the growth of microorganisms or killing them outright. Those which are taken internally to alleviate the symptoms of or promote healing from disease are called chemotherapeutic drugs, and among these is a class of compounds called antibiotics. In order for a chemotherapeutic drug to be classed as an antibiotic, it must be produced by a microorganism such as bacterium or fungus or at least derived from a chemical produced by one. It must also be capable of killing or inhibiting the growth of other microorganisms and of doing so when taken in very small quantities.

Natural products have been a source of medicinal agents for thousands of years. Impressive number of modern drugs derived from natural products. Today, natural products are one of the main interests for research directed towards drug design and discovery. It also has provided considerable value to the pharmaceutical industry over the past half century. In particular, the therapeutic areas of infectious diseases and oncology have benefited much from numerous drug classes derived from natural form and it is used as template for synthetic modification.

M.p. 294-295 oC. 1H NMR (300 MHz, DMSO, ppm): δ 1.22 (t, 3H, J¬ = 7.1 Hz, COOCH¬2¬CH¬3), 2.85 (t, 2H, J¬ = 5.6 Hz, H-5), 3.56 (s, 3H, ¬CH¬3), 3.62 ( t, 2H, J = 5.1 Hz, H-6), 4.09 (q, 2H, J¬ = 7.0 Hz, COOCH¬2¬CH¬3), 4.53 (s, 2H, H-8). 7.13 (s, 1H, NH2), 13.55 (s, 1H, NH). 13C NMR (75 MHz, DMSO, ppm): δ 14.3 (CH3), 25.0 (C-5), 36.2 (CH3), ¬40.1 (C-6), 42.6 (C-8), 60.9 (CH2, carbamate), 119.2 (C-4a), 126.3 (C-4b), 129.0 (C-8a), 154.6 (C-9a), 156.3 (C-2), 157.8 (C=O), 163.3 (C=O, carbamate). Anal. Calcd for C13H17N5O3S (323.37): C, 48.28; H, 5.30; N, 21.66; Found: C, 48.10; H, 5.13; N,

A 1:5 mixture of ethyl acetate (10mL) and hexane (50mL) was used as the eluent. After the products were purified, they were submitted to analytical group who ran GCMS and FTIR on them to confirm the presence of sarmentine derivative, which is pyrrolidin-1-yl.

The condensation product of primary amines with active carbonyl compounds have resulted in the formation of Schiff base compound. This has been reported by Hugo Schiff in 1864. Schiff base compound contain azomethine -C≡N with a general formula RHC=N-R’ where R and R’ are alkyl, aryl, cyclo alkyl or heterocyclic groups which may be variously substituted. These compounds are also known as anils, imines or azomethines (Mishra N. et al, 2013). Structurally, a Schiff base is a nitrogen analogue of an aldehyde or ketone in which the carbonyl group (C=O) has been replaced by an imine or azomethine group (Figure 1.1) (Abu-Dief M.A et al, 2015).

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),

Alantolactone (1): mp 78-79 °C.1H NMR (CDCl3, 500 MHz) δ ppm: 6.06(1H, d, J= 1.8 Hz, H-13a), 5.73(1H, d, J =1.8 Hz, H-13b), 5.26(1H, d, J= 3.9 Hz, H-6), 4.86(1H, m, H-8), 3.64(1H, m, H-7), 2.85(1H, m, H-4), 2.47(1H, d, J=15.5 Hz, H-9a), 2.06(2H, m, H-1a), 1.58(3H, o. m, H-2), 1.54(1H. o. m, H-9b), 1.46(1H, m, H-1b), 1.08(3H, s, 14-CH3), 1.06(1H, d, J= 8.0 Hz, 15-CH3); 13C NMR δppm: 17.01(C-1), 32.99(C-2), 41.98(C-3), 37.87(C-4), 149.45(C-5),119.00(C-6),39.76(C-7), 76.73(C-8), 42.92(C-9), 32.95(C-10), 140.06(C-11), 170.81(C-12), 121.97(C-13), 28.83(C-14), 22.85(C-15). All datas are in correspondence with that reported in the literature [9].

The Effect of different Temperatures on the reaction rate of Amylase Introduction: Amylases are enzymes that breaks down starch which accelerates the hydrolysis of glycosidic bonds in polysaccharides (S. Sivaramakrishnan et al., 2006). They bond with certain substrates to effectively increase the reaction rate of a chemical experiment. Most enzymes are very specific, as in they would only bond with a distinct substrate for it to cause a certain reaction. This can be described with the key and lock analogy. Only one type of key, certain amylase, will be able to open a particular lock, substrate.

Camptothecin. Whether these are used or not depends on the gains that can be received versus

These compounds are all characterized by the ability to induce tubulin polymerization in vitro and their gross cellular profiles are similar.

They have been reported to possess antioxidant,1-4 antimalarial,5 antileishmanial,6 antiinflammatory,7 antitumor8 and antibacterial activity9. The presence of a reactive

Phenolic compounds. Of the antiseptic agents , phenols have been in clinical use the longest and have been available worldwide for over a century with minimal adverse effects reported. Listerine is a com-