Synthesis, Spectral And Biological Activities Of Pyridine 26 Dicarboxalic Acid Hydrazone Derivatives And Its Metal Complexes Essay

In the next step, 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)-N-(4-fluorophenyl)acetamide (3a) was subjected to condensation reaction to afford N-(substituted)-2-((6-oxo-5,6-dihydroimidazo[2,1-b][1,3,4]thiadiazol-2-yl)thio)acetamide (4a-m) and their structures were confirmed by spectral analysis. The FT-IR spectrum of compound (4a) showed characteristic absorption bands at 3255cm-1 (NH), 3024cm-1 (ArC-H), 1614 (C=O), 1263cm-1 (C-S) and 1588cm-1, which could be attributed to (C=N). The 400MHz 1H-NMR spectrum of compound (4c), showed a singlet for the amide NH proton at δ 10.37ppm. The signal corresponding to the two protons of NH2 group in the 2-aminothiadiazole ring disappeared and a new sharp singlet for imidazole protons was appeared

Bromide molecule from pyridinium tribromide was attacked by pi bond creating a positive charge on the bromide. To stabilize the structure, the negative bromide was introduced via frontside attack and made an syn product.

The 1H-NMR titration experiment revealed that the benzyl group of TUs strengthened the intermolecular interactions toward an organophosphonate (Figure 3). It has been known that the chemical shift of thiourea N–H changes according to the degree of hydrogen bond with an acceptor (i.e., DMMP), and its association constant (Ka) can be obtained by non-linear regression analysis (Figure 3a).18 The 1H-NMR spectra of TU 1, 2, 4, or 8 in chloroform-d (~100 mM) indicate that the chemical shift of the N–H protons shifted downfield with increasing amount of DMMP up to 80 equivalents, confirming the formation of the TU-DMMP complex through hydrogen bonding (Figure 3b). In the 1H-NMR titration experiment, proton peak shifting shows deferent shapes

These tools give useful insight of information regarding the nature of target-ligand interactions, which consequently predict molecular models which are further used for the lead discovery and optimization. Ligand-based designing approaches are based on the information about structure of the active ligand which can interact with biological targets. The efforts for the designing of the novel drug molecule is based on the concept known as molecular similarity; compounds with high molecular structural resemblance with pre-existing ligands, are more likely to have similar pharmacological activity profiles. This approach is considered an indirect methodology as it is usually followed in absence of the 3-D structure of the target or if the target is unknown or cannot be predicted.

Imidazoline and its derivatives are important sort of inhibitors which could effectively inhibit corrosion of carbon steel against CO2 and H2S [6, 7]. Recently C.D Contreras [8] was reported the structural and vibrational analyses of 2-(2-benzofuranyl)-2-imidazoline.

Abstract: A series of new N-substituted pyrazoline derivatives were synthesized by reacting hydrazine hydrate and its derivatives with chalcone, which in turn prepared from base catalysed Claisen Schmidt condensation of cuminaldehyde and 4-chloro acetophenone. The newly synthesized structures were characterized by analytical and spectral studies. All the synthesized compounds were screened for their in vitro antioxidant and antimicrobial properties.

A 1,3,4-thiadiazole library was constructed by solid-phase organic synthesis. The key step of this solid-phase synthesis involves the preparation of polymer-bound 2-amido-5-amino-1,3,4-thiadiazole resin by the cyclization of thiosemicarbazide resin using p-TsCl as the desulfurative agent, followed by the functionalization of resin by alkylation, acylation, alkylation/acylation, and Suzuki coupling reaction. Both the alkylation and acylation reactions chemoselectively occurred at the 2-amide position of 2-amido-5-amino-1,3,4-thiadiazole resin and the 5-amine position of 2-amido-5-amino-1,3,4-thiadiazole resin, respectively. Finally, these functionalized 1,3,4-thiadiazole resins were treated with trifluoroacetic acid in dichloromethane,

Abstract: The reactions of 2-amino-3-cyano-4.6-diarylpyridines with formic acid, glacial acetic acid, benzoyl chloride, formamide and acetamide afforded 5-(5-substitutedfuran-2-yl)-7-(4-substitutedphenyl)-3H-pyrido[2,3-d] Pyrimidin-4-one , 2-methyl-5-(5-substitutedfuran-2-yl)-7-(4- substituted phenyl)-3H-pyrido[2,3-d] pyrimidin-4-one, 5-(5-substitutedfuran-2-yl)-7-(4-substitutedphenyl)-2-phenyl-3H-pyrido[2,3-d] pyrimidin-4-one, 5-(5-substitutedfuran-2-yl)-7-(4-substituted phenyl)-pyrido[2,3-d] pyrimidin-4-ylamine, 5-(5-substitutedfuran-2-yl)-7-(4-substitutedphenyl)-2-methyl-pyrido[2,3-d] pyrimidin-4-ylamine, respectively. The newly synthesized heterocycles were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectral data. Compounds have been screened for their antibacterial, antifungal and anticancer activities.

The structures of LPSF-33, LPSF-34 and LPSF-35, including both E and Z isomers, were drew using the SPARTAN 08' program [20] and the optimization of each structure was carried out using the RM1 [21] method, available as part of the SPARTAN 08’ program, using internal default settings for convergence criteria. Docking analysis was carried out on Peroxisome Proliferator Activated Receptor (PPAR) Gamma (PDB code: 2PRG). The chosen PPAR structure has been used in another work involving an antidiabetic drug [22]. The binding site was defined as all atoms within a radius of 6.0 Å from it co-crystallized ligand. The GOLD 5.2 program [23] was applied for docking calculations, using the ChemPLP score function. In order to take into account, the

Organometallic are the most commonly compounds used in homogeneous catalysis. They usually contain various kinds of metals. Their reactivity, bonding (ionic and covalent or in-between) and stabilities are premised on 18 electrons rule. Organometallic compounds contain at least 1 carbon to metal bond. There are also organometallic complexes which have covalent bonds between organic ligands and a metal. The metal binds to ligands through an atom e.g. O2 or N; such compounds are referred to as coordination compounds. The complexes are basic in nature, also as reducing agents act as superoxide anion scavengers which help in catalyzing polymerization reactions and thus used clinically to treat tissues and cell injuries be it lymphomas or carcinomas. Rhodium compounds is analogues to the corresponding Platinum and Ruthenium compounds serve as effective anticancer agents due to significant antitumor properties. Effective advanced technologies such as nuclear magnetic resonance (NMR) and infrared spectroscopy (IR) are used to determine the dynamic properties, structures and industrial uses of organometallic compounds and complexes due to the ability to absorb the available proton occupied each site of a metal atom in the solution.

In this assessment I have chosen to research pharmaceuticals as a material that has been developed in the last twenty years. This is a report that will demonstrate my understanding of the chemistry of the material. In this report I shall include the historical development, the properties of the material that makes it useful to society, whether there was experimentation or discoveries that led to its development, any other notes and a personal opinion, and references to my findings.

Medicinal chemistry and pharmaceutical chemistry is a branch of chemistry, especially synthetic organic chemistry, various other biological specialties, or bio-active molecules. Compounds used as medicines are most often organic compounds, which are often divided into the broad classes of small organic molecules like atorvastatin and fluticasone. Inorganic and organ metallic compounds are also useful as drugs. These compounds include lithium carbonate and gallium. In particular, medicinal

Organoselenium compounds are of considerable interest due to their wide efficiency and applicability with numerous therapeutic applications [23]. In addition, the presence of a heterocyclic ring in these compounds upgrades their properties to a great

Time: 50 minutes Total number of pages: 6 Answer all questions in the space provided.

Most indolizine compounds present interesting pharmacological effects (Singh and Mmatli, 2011) and several biologically active indolizines were reported to possess biological activities like; anti-inflammatory activities (Malone et al, 1998). Other activities reported are antiviral, antitumor and analgesic activity (Gubin et al, 1992, Bolle et al, 2004, Campagna et al, 1990, Pearson and Guo, 2001, Artico et al, 1989). Due to their strong fluorescence in the UVvisible region, the photophysical properties of some indolizines have already been reported (Delattre et al, 2005, Rotaru et al, 2009).