1. | 2-D QSAR STUDY OF 5-ARYL BENZIMIDAZOLONE AND OXINDOLE BASED AMPA RECEPTOR MODULATORS SELECTIVE FOR TARP ï§-8 FOR ANTI-EPILEPTIC ACTIVITY |
| Sweta N.Desai, Ghanshyam Sanghani, Nishadh Solanki, Vineet Jain. |
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Quantitative Structure Activity Relationship (QSAR) represents an attempt to correlate 2D and 3D properties(descriptors) of compounds with activity. In order to understand the structural requirements for AMPA receptor antagonism.QSAR study for the anti-epileptic activity of 18new15-Aryl Benzimidazolone and Oxindole- Based AMPA ReceptorModulators Selective for TARP γ-8 was established. With the PaDEL-Descriptorprogram, more than 1000 differentMolecular descriptors were calculated. Bias-Variance Estimator using Bootstrapping method did re-sampling ofdescriptors.For Regression, analysis dataset division was performed by Kennard stone method. Partial least squaresregression (PLS regression) generated model from 12 molecule training set and 6 molecule test set revealed that polarity ofthe molecules is governing factor for anti-epileptic activity. The best model with 4 descriptor was selected which has r2 =0.96251, q2 = 0.91389
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2. | DEVELOPMENT OF VALIDATED BIO ANALYTICAL METHOD FOR THE INVITRO DETERMINATION OF DOXOFYLLINE FROM HUMAN PLASMA BY HPTLC |
| Nihila K, Akhil MB, Y Haribabu, Kumar Palanisamy |
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Bio-analytical methods employed for the quantitative determination of drugs and their metabolites in biologicalsamples plays a significant role in the evaluation and interpretation of bioavailability, bioequivalence and pharmacokineticstudy data. These studies generally support regulatory findings. HPTLC is one of the most widely used methods for bothqualitative and quantitative analysis. After extraction, various concentrations of drug solutions were applied on the plate anddevelopment of the plate was done by using mobile phase system consisting of Toluene: n-butanol: Triethylamine: Ammonia(3:5:2:0.1%v/v/v/v) Rf values of Doxofyllinewasfound to be 0.47±0.01. The developed method was validated according tothe US-FDA guidelines. Linear regression data revealed an excellent linear relationship between concentration and peak arearatio over a concentration range of 20-200 ng/spot. The stability of Doxofylline in prepared sample was found to be 7hoursunder room temperature.
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3. | SYNTHESIS AND CHARACTERIZATION OF BENZIMIDAZOLE DERIVATIVES FOR ANTI- B ACTERIAL ACTIVITY |
| Manisha Negi*, Dr.Sanjay Singh |
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The present study was conducted to evaluate 3 synthesised benzimidazole derivatives and the derivatives were prepared by treating with primary amine (methyl amine) and secondary amine (pyridine) and hence they are confirmed by IR, NMR and GC-MS. The synthesized compound shows anti bacterial activity activity against E.Coli, S.Aureus and they shows more, most and significant activity towards the microorganism hence the compound is beneficial to treat bacterial infection
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4. | SYNTHESIS AND CHARACTERIZATION OF TRIAZOLE COMPOUNDS DERIVED FROM OXADIAZOLE MOIETY FOR ITS ANTIMICROBIAL AND ANTI-OXIDANT EVALUATION |
| Hricha Joshi*, Ajay Singh Bisht, Divya Juyal |
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The broad spectrum and excellent property of triazole compounds have led to the various synthetic researches in the derivation of these compounds. Also because they have an immense biological activity, therefore they promise to possess significant pharmacological activity. A new technique for the synthesis of new triazole derivatives from a heterocyclic nucleus oxadiazole has been developed by binding two types of amino acids in the oxadiazole molecule. The name of the final compounds as triazole compounds are 4-(1`indoline propionic acid)-3(3-pyridyl)-5-thione-1, 2, 4-triazole and4-(2`- methyl pentanoic acid)-3(3-pyridyl)-5-thione-1, 2, 4-triazole. The reaction and purity of the compounds is checked by TLC and melting point. The characterization of the compounds is performed by 1D-NMR and IR. The antibacterial activity is done on two strains of bacteria gram negative and gram positive and the antifungal activity has been performed by the strains of A.niger. The antioxidant activity has been done by in-vitro DPPH method
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5. | AN INSIGHT TO THERAPEUTIC POTENTIAL OF COUMARINS AS ANTIVIRAL AGENTS |
| Rushda A V, Nehlayahcoob, Shiji Kumar, Sirajudheen M K, Sherin A |
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Coumarin compounds also known as benzopyran-2-one.Coumarins are made up of a bicycle system, which contains an alpha-pyrone ring and a cooled benzene. Many center patterns appear on the central bicycle system, it alters a variety of biological effects and a number of medicinal and therapeutic properties have been attributed to natural product coumarin. Antivirals are the type of drugs used to treat viral infections as well as bacterial infections. Most antiviral drugs are used for specific virus infections in a broad spectrum of antivirals effective against a wide range of virus. Coumarins has increased significantly recently as it is found in the prevention of HIV (human immunodeficiency virus). It affects the integration and reverse transcriptase and plays a crucial role in the cycle of HIV replication. Gone were the days of focusing on the study of antiviral activity of assay for coumarin derivatives. Natural products have been used to treat viral infections for 1000 years and play a greater role in drug discovery and development. Plant semisynthetic calanolide compounds and semisynthetic in invitro activity against human HIV 1and cytomegalovirus and have been shown to be a naturally occurring non-nucleoside transmerase inhibitor. The reverse transcriptase is an established target for chemotherapeutic agents used for the treatment of HIV infections. These coumarins represent a distinct class of non-nucleoside reverse transcriptase inhibitors. The herbal medicines are commonly used as an alternative medicine by individuals living with HIV. In this review we aim to review the antiviral potential of coumarin as HIV defenders
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