Posted by admin on Sep 2, 2017 in |
A series of new Mannich base derivatives were designed, synthesized by conventional and non-conventional microwave method, compared and evaluated for their antimicrobial and anti-mycobacterial activity. Structures of the newly synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR, 13C NMR and mass spectral studies. The bioactive assay showed that Mannich base derivative 1c displayed encouraging anti-tubercular activity in vitro against Mycobacterium tuberculosis H37Ra using MABA method in primary screening. The antibacterial and antifungal efficacy of these derivatives using broth micro dilution method, showed potency for 1c against Escherichia coli, 1g against Staphylococcus aureus, Candida albicans and 1j against Candida albicans in comparison with reference drugs. Furthermore, docking study has been performed for three different PDBs (3JZF, 4NZ9 and 2WHF) of different strains that showed good binding interactions. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug...
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Posted by admin on Aug 31, 2017 in |
Tuberculosis is caused by Mycobacterium tuberculosis and affects primarily the lungs. Breast tissue is remarkably resistant to tuberculosis. This is due to fact that it gives infertile environment for survival and multiplication of tubercle bacilli like skeletal muscle and spleen. The breast may become infected by variety of ways e.g. haematogenous, lymphatic, spread from contiguous structures, direct inoculation and ductal infection. The path of spread of disease from lungs to breast tissue was traced via trachea-bronchial, Para tracheal, mediastinal lymph trunk and internal mammary nodes. Scrofulous swelling of the bosom is the description given by Sir Astley Cooper who recorded first ever Breast Tuberculosis. It is usually seen in lactating young multiparous women and presents as lump in the central or upper outer quadrant of breast. It is occasionally mistaken as Carcinoma Breast or Breast Abscess. The overall incidence of tuberculosis Mastitis is reported to be 0.1 % of all breast lesions while in developing countries it constituted approximately 3.0 % of surgically treated breast...
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Posted by admin on Aug 31, 2017 in |
Baboon’s Cucumber (Kedrostis africana (Linnaeus) Cogn is a monoecious caudiciform plant that belongs to Cucurbitaceae family. Baboon’s Cucumber is used traditionally for the management of syphilis and obesity in South Africa. In the present study, we examined the hatchability and lethality of Baboon’s Cucumber bulb extracts against brine shrimps. The tested samples were aqueous extract, acetone extract, and ethanol extract. Cytotoxicity was screened using Brine Shrimp Lethality Test (BSLT). The hatching success was in the order: ethanol extracts (49.2%) >aqueous extract (45.4%) >acetone extract (45.2%). All the extracts hatching success were significantly higher than the positive control (potassium dichromate) (p <0.05). Based on Clarkson’s toxicity index, LC50> 1 mg/mL were considered non-toxic for acetone extract while the aqueous and ethanolic extracts were considered to be moderately toxic (LC50 100-500 μg/mL) with LC50 of 0.298 and 0.489 mg/mL respectively. In conclusion, since the aqueous and ethanolic bulb extracts of K. africana exhibits potent cytotoxic property comparable to that of standard drug. Therefore, this might be utilized for the development of...
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Posted by admin on Aug 31, 2017 in |
Crystal engineering of cocrystals promises a new approach for the development of suitable solid phase when the solubility of API is compromised. Cocrystals are an emerging solid-state form to change physicochemical and biopharmaceutical drug properties. A cocrystal is defined as a stoichiometric hydrogen-bonded complex in the solid state between the active drug species and a suitable coformer molecule that is safe for human consumption. In the present work, cocrystal of telmisartan has been prepared with citric acid. The TEL-CA cocrystal prepared by fast evaporation technique was initially characterized using DSC and FTIR studies. The PXRD pattern of the cocrystal was completely different from that of drug and coformer. The crystal structure determined using Material Studio software (Accelrys) showed triclinic symmetry with P1 space group. TEL-CA cocrystal forms a hetersynthon involving the amine group of telmisartan and carboxylic acid group of citric acid. The equilibrium solubility and intrinsic dissolution rate of cocrystal showed improvement in solubility as compared to pure drug. The pharmacokinetic parameters also showed a two fold increase...
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Posted by admin on Aug 31, 2017 in |
Introduction: Irbesartan is chemically 2-butyl-3-({4-[2-(2H-1,2,3,4-tetrazol-5-yl) phenyl] phenyl} methyl) -1,3-diazaspiro [4.4] non-1-en-4-one. Irbesartan is an Angiotensin II receptor antagonist effective in the treatment of Hypertension. It is also effective in the treatment of High blood pressure. It is also effective when used alone or in combination with other drugs. Aims and Objectives: Objective of the present study is to develop a simple, sensitive, accurate, precise and rapid first order derivative spectrophotometric method for the estimation of irbesartan in pure form. Results: For the estimation of irbesartan, solvent system employed was 50% v/v aqueous ethanol and wavelength of detection (λdet) was 237 nm. The linearity was obtained in the range 8 -18 µg/ml, with a regression coefficient, R2 = 1. Discussion: Obtained results showed that there is minimum intraday and inter day variation. The developed method was validated and recovery studies were also carried out. Sample recovery using the above method was in good agreement with their respective labeled claims, thus suggesting the validity of the method and non-interference of formulation...
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