Synthesis Essay : 25 Di ( 2h 1

Azacitidine was first synthesized by Piskala and Sorm in 1964 [Piskala A, Sorm F. (1964). Collect Czech Chem. Commun., 29: 2060-2076]. It was developed as a nucleoside antimetabolite specifically used for the treatment of acute myelogenous leukemia (Cihak, 1974;Sorm et al., 1964).

The second cause of death worldwide is Cancer [1]. It is expected that the number of people that will die because of cancer in 2030 is about 13.1 million [2]. It is better to develop novel, safe and effective chemotherapeutic drugs to treat cancer with minimal side effects. The pyridine ring is one of the most well known nitrogen containing heterocyclic compounds. Pyridine derivatives possess a wide spectrum of biological properties such as antifungal [3], antimicrobial [4-10], antioxidant [11], and anticancer [12-14]. α-Aminophosphates is one of the biologically active compounds may be because they are analogues to α-amino acids [15, 16]. α-Aminophosphonates and their derivatives are considered to be bioactive molecules due to their biological

as our synthesized compounds are thiadiazole and schiff base derivatives i will start with thiadiazole ,A five-membered heterocyclic ring containing one sulfur and two nitrogen atoms.

A plausible mechanism for this reaction is suggested in Scheme 2. It is reasonable to assume that the functionalized spiroquinazoline 3a-g could obtained from the initial condensation of amino group in 2-aminobenzamide and carbonyl group of the ketone, followed by attack of the lone pair of N-atom of amide on the positively charged carbon of imine. Finally, N-anion of ketenimine could protonated to form the targeted compounds

2.11.1 Structure: riluzole is a derivative of benzothiazole (Hofmann, 1879), a bicyclic ring compound which comprises a benzene ring fused with five membered ring containing one sulfur and one nitrogen atom. It has the molecular formula C8H¬F3N2OS with a molecular weight of 234.20.

The polyhydroquinoline motifs range prominent among nitrogen containing heterocycles due to their occurrence in a broad range of biologically active natural products & pharmaceuticals. 1, 4-Dihydropyridine (DHP) scaffold is an important pharmacophore found in a large number of biologically active and potential therapeutic compounds. DHP is a diverse pharmacologically active motif which is useful for clinically validated therapeutic agents such as amlodipine, lacidipine, nicradipine and also many

1. Identify your thesis statement. How can it be more clear and/or specific? If you don’t have a thesis, identify a common thread or idea between the two assigned readings and create one. Remember, a synthesis is not a compare & contrast essay.

Viktor E. Frankl didn’t grow up living a easy life. During World War II he spent 3 years in various concentration camps, including Theresienstadt, Auschwitz, and Dachau. Viktor has a life story to tell. Concentration Camps were a place where large numbers of people, especially political prisoners or members of persecuted minorities, are deliberately imprisoned in a relatively small area with inadequate facilities, sometimes to provide forced labor or to await mass execution. Frankl may have survived the holocaust but coming out of it he was not the same person. Viktor Frankl is an inspiration to many Generations. Viktor Frankl always looked at life differently than everyone else did. “Each man is questioned by life; and he can only answer to life by answering for his own life; to life he can only respond by being responsible.” Frankl tells that know matter what obstacles you have to face there will always be a way out, you just have to be patient and responsible. The story Man 's Search for Meaning based on a true story, published by one of the main Characters Viktor Frankl. Viktor Frankl survived the holocaust and has lived on to pursue a dream of his which was becoming therapist.

Objective: Present research work is carried out for rapid development of some biological active new heterocyclic moieties.

These turning points led to the formation of several bis-triazoles. The first was a chloroacetyl derivative, which was reacted with 1,2,4-triazol to yield a ketone, which was then converted to an epoxide and then opened, resulting in the first bis-triazole derivative. The second approach required converting dichloroacetone to dichloropropanol derivative and reacting it with 1,2,4-triazole, which produced the second bis-triazole. These bis-triazoles were then synthesized in a large number of 2-substituted 1,3-bis-triazolylpropan-2-ol derivatives. Out of the tested derivatives, it was found that the 2,4-difluorophenyl analogue was water soluble, meaning it was could be used intravenously; hence the successful development of fluconazole.2

Imidazolinone (C3H4N2O), a keto dihydro imidazole, is a 5-membered heterocyclic with two nitrogen atoms at the first position and third position. It also contains a C=O group which can be located either in second position, fourth position or fifth position, namely 2-oxo-imidazoline, 4-oxo-imidazoline and 5-oxo-imidazoline respectively.

Tetraoxanes (also stabilizes O–O bond), as was employed in the drug development candidate RKA 182, has displayed IC50 values of 4.9 nM against the P. falciparum 3D 7 strain and of 1.9 nM against the K1 strain (chloroquine sensitive and -resistant, respectively). It reduced P. berghei parasitemia in mice to undetectable levels 24 hours after treatment. This compound is currently in preclinical trials and although it has greater stability than OZ277, its antimalarial activity is inferior to OZ439. [8, 9]

In particular, chiral compounds with β-amino-α-thiocyanate moieties are rarely explored in the medicinal chemistry area because of their synthetic difficulty,[5] although they are versatile precursors for the synthesis of β-aminothiols,[6] β-aminosulphonic acids,[7] and 2-iminothiazolidines,[8] present in some stereoselective catalysts, and many biologically and pharmacologically active compounds.

It is essential to discover new drugs with less resistance (Navan et al, 2011). A number of heterocyclic compounds are known and have been shown to possess pharmacological activities. The significant one among them is that containing ring junction nitrogen. The presence of these systems are rare in natural products, but important in many studies for preparation of potentially, biologically active analogues. Indolizines are such type of systems, which contain ring junction nitrogen and are very rare in nature (Srikanth et al, 2011).

In spite of impressive recent advances of synthetic drugs, the approach to develop newer drugs from chemical libraries, however, was proven to be less useful in terms of overall success rate. In recent years, there is a renewed interest on natural product research due to the failure of alternative drug discovery methods to convey many lead compounds in the major therapeutic areas such as immunosuppression, metabolic diseases and anti-infectives. Natural products acquire massive structural and chemical diversity which is incomparable by any synthetic libraries. About 40% of the chemical scaffolds observed in natural products are deficient in today’s medicinal chemistry and thus become complementary to synthetically developed molecules.