Current Issue : January - March Volume : 2013 Issue Number : 1 Articles : 9 Articles
Hydroxypropyl methylcellulose (HPMC) is a semisynthetic, inert, viscoelastic polymer having good filmability and mucoadhesivity. The current aim of our research work is to synthesize a polymeric azo conjugate by using HPMC with phenylalanine and to screen its colon specificity by in vitro release model. HPMC was subjected for synthesizing its azo conjugate by using phenylalanine, sodium nitrite, methanol and conc. hydrochloric acid. The azo polymeric conjugate was evaluated for its color, solubility, Rf value, melting point, IR and 1H NMR spectral analysis. It was further subjected for evaluating its colon targeting property by in-vitro method using rat fecal matter. Our experimental results reveal that the HPMC azo conjugate showed promising colon specificity for a period of 120 minutes in a controlled manner. So it can be used as an excipient for formulating colon targeted drug delivery systems....
Renin Angiotensin System is the most direct, precise, complete, specific and effective approach to antagonize AngII at its receptor site. A relatively new class of compounds known as Ang II receptor antagonists (SARTANs) has been developed for the treatment of hypertension. They exert their action by blocking the binding of Ang II on the AT1 receptor. Based upon the understanding of molecular interaction of Ang II receptor antagonists at the AT1 receptor some of the common structural feature has been identified, such as a heterocyclic (nitrogen atom) ring system, an alkyl side chain and an acidic tetrazole group. Scientist efforts for development of new molecules belong to category non-peptidic Ang II receptor antagonists with different substituted heterocylic such as imidazole (losartan), pyrazole, triazole and benzimidazole. Candesartan and Telmisartan are clinically used AngII antagonist having substituted benzimidazole nucleus with carboxyl function at 7-position and benzimidazole group at 6-position respectively. Present study is for the use of benzimidazole nucleus is potential core for the angiotensin II receptor antagonist developments....
Five membered and two nitrogen hetetro atom containing heterocyclic compounds like Imidazole, Benzimidazole, Pyrazole, Oxadiazole, and Thiadiazole possess varieties of biological activity. These entire compounds collectively known as diazole. Many of literature reveal that among all diazole, imidazole and benzimidazole have wide and distinct antimicrobial activity. Benzimidazoles are remarkably effective compounds, extensive biochemical and pharmacological studies have confirmed that these molecules are effective against various strains of microorganisms. Various newer derivatives of benzmidazol and its Schiff’s base was prepared and screened for antibacterial and antifungal activity....
Quantitative structure–activity relationship (QSAR) analysis for recently synthesized 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea derivatives was studied for CNS depressant activities. The statistically significant 2D-QSAR models (r2 = 0.9533; q2 = 0.9186; F test = 81.6335; r2 se = 0.0089; q2 se = 0.0117; pred_r2 = 0.9177; pred_r2se = 0.0242) were developed using molecular design suite (VLifeMDS 4.1). The study was performed with 24 compounds (data set) using sphere exclusion (SE) algorithm, random selection and manual selection methods used for the division of the data set into training and test set. Multiple linear regression (MLR) methodology with stepwise (SW) forward-backward variable selection method was used for building the QSAR models. The results of the 2D-QSAR models were further compared with 3D-QSAR models generated by kNN-MFA, (k-Nearest Neighbor Molecular Field Analysis) investigating the substitutional requirements for the favorable CNS depressant activity and providing useful information in the characterization and differentiation of their binding sites. The results derived may be useful in further designing novel CNS depressant agents prior to synthesis....
Quinoline derivatives play a vital role in medical field with a wide range of Pharmacological activities such as antimicrobial, antimalarial, antiHIV and anticancer Activity. The potency of these clinically useful drugs in treatment of malarial infections encouraged the development of some more potent and significant Compounds and their screening for antiHIV activity. This review is summarized to know about the chemistry of different derivatives of substituted quinoline derivatives along with their pharmacological activities....
A new class of substituted 8-hydroxyquinoline derivatives containing oxadiazole ring 4a-e were synthesised through multi step reactions. The structures of the newly synthesised compounds were confirmed by LC-MS, 1 H NMR, Elemental Analysis and FTIR-spectral analysis. The second step involved the synthesis of esters (2a-e) by using the base NaOH, which reduced the reaction time drastically as well as improved the yield when compared to the reported methods. The newly synthesised compounds were evaluated for antioxidant, and angiotensin-I-converting enzyme (ACE-I) inhibitory activities. The compound 4d emerged as the most effective antioxidant agent against R-tocopherol, Mannitol, BHT and BHA. Among the compounds tested, 4c, 4d and 4e exhibited ACE-I inhibitory activity with IC50 253.089, 1022.660 and 1101.950 ± 2µM respectively. Docking simulation further supported the probable binding conformation with ACE-I active site for 4c....
Cancer is a class of diseases in which a cell, or a group of cells display uncontrolled growth, invasion, and sometimes metastasis. It caused about 13% of all human deaths in 2007. In 2015, 9 million are expected to die of cancer. Hence there is tremendous research going on to develop new anticancer drugs. Alkylating agents like sulphur mustard and nitrogen mustards could interfere with cellular proliferation. Hence various benzisoxazole derivatives containing nitrogen mustard were synthesized by various synthetic routes. The structure of the compounds were confirmed by IR, 1H NMR and mass spectral data. Newly synthesized compounds were screened for their In-Vitro Cytotoxic activity and In-Vivo anticancer activity. Out of eight compound synthesized four compounds showed potent cytotoxic activity. These four were screened for In-Vivo anticancer activity out of which one compound showed extremely significant activity at the dose of 40 mg/kg body weight....
Sets of trisubstituted thiazoles (4a-4i) were synthesized by reaction of substituted N-(piperidinyl/ piperazinyl/N-methylpiperazinyl-4-thioyl) benzamide (3) with 3-(bromoacetyl) coumarin, respectively. The (3) were synthesized by nucleophilic addition of benzoyl isothiocyanate/ substituted benzoyl isothiocyanate and piperidine/ piperazine/4-methylpiperazine in equimolar quantity at reflux temperature. The synthesized compounds (4a-4i) were screened for their in vitro antibacterial activity against S. aureus, B. subtilis and E. coli using ciprofloxacin as standard drug. The targeted compounds (4a-4i) were evaluated for their in vivo anti-inflammatory activity in carrageenin-induced rat hind paw oedema model at three graded doses employed at 10, 20 and 40 mg/kg body weight using ibuprofen standard drug. Compounds (4a-4i) were also evaluated for ADP-induced platelet aggregation of platelet-rich plasma aspirin was used as positive control. Among all the targeted compounds 4h and 4i showed maximum antibacterial activity against all the three bacteria, while 4b showed maximum 89.6% antiplatelet activity. Compound 4c showed maximum anti-inflammatory activity of 33% protection at 10 mg/kg and 57% protection at 20 mg/kg to inflamed paw....
Benzodiazepine derivative are most widely useful as anti fungal, anti inflammatory, anti depressive, anti anxiety and sedative and hypnotics. Due to wide pharmacological action we have selected benzodiazepines and prepared 2, 4-di substituted benzodiazepines and we evaluated the different substituted derivatives by IR, NMR, and MASS spectroscopic studies. The in-vivo anti inflammatory, and in-vitro anti oxidant activities were performed and the compound (1a-1e) showing good anti inflammatory activity and where as compound (1b-1d) having good activity....
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