1

A series of 3-amino-5-sugarimino-1, 2, 4-thiadiazolines have been synthesized by oxidative cyclization of sugar-3-amidinothiocarbamides by using bromine. These amidino thiocarbamides were prepared by interaction of guanidine and sugar isothiocynates. Guanidine itself plays an important role as antifungal, anticancer activities when it links with glycosides its acivity increased. These newly synthesized compounds have pharmaceutical uses. The identities of these newly synthesized compounds have been established on the basis of usual chemical transformation and IR, 1H NMR, and Mass spectral studies. The synthesized compounds were screened for their in vitro antimicrobial activities using human pathogens.

2 (H/substituted)-4-aryl-5H,6H, 7-arylimino-1,2,3,5,6-thiatetraazepines (6) have been obtained by basification of 2-(H/substituted)-4-aryl-5H,6H-7-arylmino-1,2,3,5,6-thiatetraazepine monohydrochloride (5).  The latter were synthesized by the interaction of N-aryl-S-chloro isothiocarbamoyl chloride (4) and 1-(H / substituted)-3-aryl-dihydroformazan (3), which were prepared initially by the condensation of aryl acid hydrazide (1) and hydrazine hydrate or substituted hydrazine (2). Compound (6) on benzoylation with benzoyl chloride and excess 10 % sodium hydroxide solution afforded benzoyl derivatives (7) and on boiling with aqueous ethanolic sodium hydroxide solution isomerizes into corresponding 1, 2, 3, 5, 6-pentaazepines (8).  The structures of all the synthesized compounds were established on the basis of elemental analysis, equivalent weight determination, spectral analysis like IR, 1H-NMR and Mass.  These newly synthesized compounds (6) were screened for their antifungal and antibacterial activity.

Several pharmacological activities like antitubercular, analgesic, anti-cancer, anti-inflammatory, antiasthmatic, antioxidant and antibacterial activities have been attributed to pyrazoles. The above observations prompted us to synthesize some novel pyrazole derivatives as possible antimicrobial agents. A series of novel 1,3,5-trisubstituted pyrazole derivatives (P1-P15) have been synthesized by the reaction of substituted chalcones (C1-C15) with succinichydrazide. The starting material, chalcones were prepared by claisen Schmidt condensation of acetophenone with aldehydes in the presence of sodium hydroxide in ethanol. Succinichydrazide was synthesized by condensing succinic acid with hydrazine hydrate. The cycloaddition of chalcones with succinichydrazide gives 1,3,5-trisubstituted pyrazole derivatives. The structures of synthesized derivatives were confirmed by IR, 1HNMR and Mass spectrum. The synthesized compounds were screened for their antibacterial and antifungal activity. The antibacterial activity data of the synthesized derivatives revealed that the compound P4, P13 and P7, P14 were effective against gram positive and gram negative organisms respectively. The antifungal activity data revealed that the compound P7 and P8 showed good activity against tested fungi.

Azacitidine and its deoxy derivative are used in the treatment of myelodysplastic syndrome. These types of drugs were first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer. Conventional compositions of Azacitidine are available as powder product or as a solution of Azacitidine in water. Both these products have been associated with a number of toxicities when administered intravenously. To overcome these problems, in the present study, inclusion of Azacitidine in liposomal formulation has proved to be good approach to eliminate the toxicities and improve drug antitumor activity. We formulated Azacitidine liposomes containing Hydrogenated soy phosphatidylcholine, 1,2-Distearoyl-sn-glycero-3[Phospho-rac-(1-glycerol ) (Sodium Salt) [DSPG-Na] and Cholesterol by dried thin film hydration technique. Particle size analysis, zeta potential, %free drug are strongly affected by the different lipid concentration and result shown F5 formulation have the optimum % free drug, Particle size and F2 formulation shown highest Percent drug release when compared to the F4 & F5 formulations. The release kinetics of F2, F4 and F5 formulations were studied. All the formulations follow zero-order release kinetics and follow case-II transport when it applied to the Korsmeyer-Peppas model for the mechanism of drug release. The stability of the F2, F4 & F5 formulations were studied at 5±3oc and at room temperature for duration of 3 months. Hence it can be concluded that the liposomes along with Hydrogenated soy phosphatidylcholine, DSPG-Na and Cholesterol are suitable carriers for the preparation of Azacitidine liposomes. Key words: Azacitidine, Liposomes, Hydrogenated soy phosphatidylcholine, 1,2-Distearoyl-sn-glycero-3[Phospho-rac-(1-glycerol.) [DSPG-Na], cholesterol.

  Triazine is the chemical species of six-membered heterocyclic ring compound with three nitrogens replacing carbon-hydrogen units in the benzene ring structure. The names of the three isomers indicate which of the carbon-hydrogen units on the benzene ring position of the molecule have been replaced by nitrogens, called 1,2,3-triazine, 1,2,4-triazine, and 1,3,5-triazine respectively. Symmetrical 1, 3, 5-triazine is the common.  Triazines are prepared from cyanic acid amide by trimerization (1, 3, 5-triazine). Pyridine is the aromatic nitrogen heterocyclic compound having only one nitrogen, and diazines are with 2 nitrogen atoms, triazine having three nitrogen and tetrazines are with 4 nitrogen atoms on the benzene ring system. Triazines are weak base. Triazines have much weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Heterocyclic bearing a symmetrical s-triazines or 1, 3, 5-triazines moieties, represent an interesting class of compounds possessing a wide spectrum of biological activities such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal and antimicrobial, antimalarial agents. They also find applications as dyes, lubricants and analytical reagents.   Key words: Triazine, Nucleophilic substitution, Cyanuric chloride, 1, 3, 5-triazine, s- Triazine