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The proposed project has been designed for structure activity relationship by the Schiff base and Mannich base of substituted 5-methyl-1,2-dihydro-3Hpyrazol- 3-one derivatives for antioxidant screening.

The scheme for synthesis has been designed to synthesise 5-methyl-1,2- dihydro-3H-pyrazol-3-one molecule is done by reacting ethyl acetoacetate with hydrazine and then by benzoylation in basic medium produced 1,2- dibenzoyl derivative of the heterocyclic ring. Further condensation with hydrazine with this heterocyclic ring produced Schiff base at three positions where free ketone group is present. This tri-Schiff base has been condensed with various ketone compounds to produce Schiff base of R1/R2 at three positions as well as the same tri-Schiff bas on condensation with benzaldehyde with urea/thiourea/guanidine produced Mannich bases ath three positions for X=O/S/NH. The synthesised compounds have been characterized by N% and UV, IR, NMR and Mass Spectra. The antioxidant screening is based on the iodine spot activity of synthesised compounds by zone diameter calculation. It has been observed that in Mannich bases derivatives guanidine derivative (Compound-7) showed maximum antioxidant activity. The profile for the antioxidant activity is: Compound- 7(X=NH)>Compound-6(X=S)>Compound-5(X=O). It happens due to the electronegativity: NH=3.1+2.2=5.3; S=2.4; O=3.5. Here "N" has one lone pair of electrons whereas "O" and "S" has two lone pair of electrons but the electronegativity of "NH" is maximum in comparison to "S" and "O" which both have two lone pair of electrons but the electronegativity of "S" is lower that "O" so the antioxidant profile showed a very good satisfactory result. In case of Schiff bases the butanone derivative (Compound-4) showed maximum antioxidant activity. The profile for the antioxidant activity is: Compound-4(R₁=CH₃,R₂=C₂H₅)>Compound-1(R₁=R₂=CH₃)>Compound- 3(R₁=R₂=C₆H₅)>Compound-2(R₁=CH₃,R₂=C₆H₅). It happens due to the presence of CH₃+C₂H₅=3 carbons in alipahtic chain in case of Compound- 4(R₁=CH₃,R₂=C₂H₅) but in case of Compound-1(R₁=R₂=CH₃), here CH₃+CH₃=2 carbons in aliphatic chain, in Compound-3(R₁=R₂=C₆H₅), here C₆H₅+C₆H₅=12 carbons in aromatic ring and in Compound- 2(R₁=CH₃,R₂=C₆H₅), here CH₃+C₆H₅=7 carbons in alipahtic and aromatic ring. Compound-4(R₁=CH₃,R₂=C₂H₅) of Schiff base is more active than Mannich base of Compound-7(X=NH) in antioxidant activity.

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The present study is to enhance the solubility of poorly water soluble drug by using different techniques like solid dispersion and crystal formation and selected drug was allopurinol. Allopurinol is poorly water soluble drug (which has solubility 0.1mg/ml) used in treatment of gout. Rapid onset of action of allopurinol drug in treatment of gout is required. Solubility is rate limiting step for this drug. So, by enhancing the solubility we can improve the bioavailability of poorly water soluble drug. For solubility enhancement we used different polymer like PEG4000, PVPK30, poloxamer 127 grade in solid dispersion. And in crystal formation used the different 11 solvent among them only ethanol, ether, and (dimethyl sulfoxide) DMSO has found good solubility and dissolution rate. For selection of solvent and polymer we had checked the compatibility by using (Differential Scanning Colorimeter) DSC And (Infra Red Spectroscopy) IR, and proved that used solvent which compatible with drug. For preparation of solid dispersion we were used melting method and solvent evaporation method. And then prepared solid dispersion carried out for scanning electron microscope) SEM study for surface property of solid dispersion. Checked the solubility and disintegrating time. Final formulation was prepared tablet dosage form after optimized batch of solid dispersion and take dissolution of tablet. All tablet prepared from solid dispersion, crystal and marketed were compare by dissolution study .and finally concluded the tablet prepared by solid dispersion is best than others.

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9-methyl-1,5-diphenyl-3H,7H-pyrazolo-[1,2-a][1,2,4,6]-tetrazepine-3,7-dione ring system has been synthesised by the reaction between hydrazine and ethyl acetoacetate produced pyrazolone moiety which on benzoylation produced dibenzoyl derivative which on condensation with urea produced 9-methyl-1,5-diphenyl-3H,7H- pyrazolo-[1,2-a][1,2,4,6]-tetrazepine-3,7-dione ring which on alkaline oxidation with KMnO₄/KOH produced carboxylic moiety. Treatment with thionyl chloride of produced acid chloride derivative. This on condensation with Mannich base produced by benzaldehyde with urea/thiourea/guanidine produced the desired moiety.

The synthesised compounds were characterised by N% and spectral datas and antimicrobial and antifungal screening has been performed by zone of inhibition studies and MIC calculation with standard antibiotic/antifungal drug against (gram+ve) and (gram-ve) bacterial and fungal strains on agar media after 24 hours incubation at 37ۧC for antimicrobial activity and 24°C for antifungal activity. Gram positive: Staphylococcus aureus ATCC 9144, Bacillus subtilis ATCC 6633, Gram negative: Escherichia coli ATCC 25922, Fungal strain: Candida albicans ATCC 10231 It has been observed that the Compound-2 (X=S) showed maximum antibacterial activity against Escherichia coli, Compound-1 (X=O) and against Bacillus subtilis and Compound-1 (X=O) and against Staphylococcus aureus. Oxygen and Sulphur has two lone pairs whereas Nitrogen has one lone pair of electrons but the electronegativity of Oxygen (X=O; 3.5), electronegativity of Sulphur (X=S; 2.4) and electronegativity of Nitrogen (X=N+H; 3.1+2.2=5.3). MIC value of all the compounds have been found as 250μg as Minimum Inhibitory Concentration by serial dilution method and MIC of Cloxacillin is 250μg and for Fluconazole is 5.5μg.

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The inner eye of chemistry looks forward to the biology for getting the best output to design a potent drug molecule after crossing the iron gates of pharmacological as well as clinical trials. The basic scientific research in pharmacy is blooming in the impact of the compatibility of designed chemical molecule towards biological molecule. Latest technology in pharmaceutical science reflects the implementation of new methodologies to screen a new chemical entity in a biological system. The inner eye of chemistry looks forward to the biology for getting the best output to design a potent drug molecule after crossing the iron gates of pharmacological as well as clinical trials. The basic scientific research in pharmacy is blooming in the impact of the compatibility of designed chemical molecule towards biological molecule. Latest technology in pharmaceutical science reflects the implementation of new methodologies to screen a new chemical entity in a biological system. A representative problem in bioinformatics is the assembly of high-quality genome sequences from fragmentary "shotgun" DNA sequencing. Other common problems include the study of gene to perform expression profiling using data from microarrays or mass spectrometry. Framing the structural framework of a chemical molecule is first done by in-silico by computational chemistry and that is synthesized by in-situ method. This after synthesis the biological screening is done by both in-vitro and in-vivo studies to enlist as a potent moiety by QSAR. All these newer techniques possess a prefix “In” for in-vitro, in-vivo, in-situ and in-silico which are the In-ner eye of the members of pharmaceutical research.

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Imidazole on reaction with chloroacetyl chloride afford 2-chloro-1-(1H-imidazole-1-yl)-ethanone, 1 which on treatment with hydrazine hydrate has yielded 2-hydrazinyl-1-(1H-imidazol-1-yl)-ethanone, 2. Condensation of 2 with various aromatic aldehydes afforded sustituted Schiff’s base of 2-hydrazinyl-1-(1H-imidazol-1-yl)-ethanone. The structures of all the products were characterized on the basis of their IR, Mass and ¹H-NMR spectroscopic data analysis. All the synthesised products were screened for their antibacterial activity against gram-positive and gram negative bacteria by cup-plate method.

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Biological macromolecules are composed of one or more linear oligomers that fold into a functional form. The information that governs the final structure is encoded in the sequence of monomers and the precise functionality that they display, but accurate prediction of such structures remains a major challenge in structural biology. Recently, chemists have begun to develop small molecule systems that fold in a similar way and these may help to answer more complex questions or find applications in artificial molecular assemblies. Study of the properties of a family of oligoamides composed of alternating repeats of isophthalic acid and bisaniline building blocks have a rich supramolecular chemistry in non-polar solvents, forming macrocyclic receptors, catenanes, knots and double-stranded zipper complexes via a combination of amide–amide hydrogen bonds and aromatic interactions. Here the serendipitous discovery of a new member of the family that folds into a well-defined, compact, three-dimensional structure, governed by a combination of hydrogen bonding and aromatic interactions.

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Dipeptidyl Peptidase-IV (DPP IV) is a serine protease enzyme. It selectively cleaves first two amino acids (His- Ala/Gly) of 29 amino acids GLP-1 peptide and thereby makes it inactive. Thus, inhibition of DPP IV enzyme activity, using suitable DPP-IV inhibitor likely to increase the levels of endogenous intact and bioactive GLP-1 peptides, thereby, it acts as antidiabetic agents.

In this project, based upon SAR study of NVP-DPP728, we have designed new series of dipeptide based DPP-IV inhibitors, which mainly consist of five membere proline ring system, attached to sterically hindered aromatic acid, with suitable linker. Total 24 new compounds were prepared, using solid phase peptide synthesis (SPPS) approach and purified by prep-HPLC. All the test compounds were subjected for DPP IV inhibitory activity and also selectivity of test compounds was assessed against DPP8, DPP9 and QPP enzymes (in vitro). Most potent compounds from each series were subjected for in vivo antidiabetic activity. In vitro, compound IIIb and IIId was found to be most active (IC50 similar to sitagliptin) and selective. In vivo, compound IIIb showed significant blood glucose reduction @ 20 mg/kg dose (ip and oral route administration).

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