Ten novel (E)-1-((2-phenoxyquinolin-3-yl) methylene) thiosemicarbazides were prepared by reacting 2-chloroquinoline-3-carbaldehydes with phenols followed by coupling the products with thiosemicarbazide. The ten thiosemicarbazides 1-10 were subjected to both in vitro and in silico studies for their pharmacological properties. They were found to exhibit very good antioxidant, antibacterial, antifungal and anti-proliferative activities. A few of them show even better free radical scavenging activity as compared to ascorbic acid used as standard compound. The in silico studies include drug likeness and bioactivity on the basis of their compliance of Lipinski’s Rule of Five, physical properties using Molinspiration programme and molecular docking with the enzyme EGFR (Epidermal growth factor receptor)tyrosine kinase. The results of molecular docking studies corroborate the results obtained from the in vitro anti-proliferative experiments. All these results indicate that aryloxyquinolinethiosemicarbazides have highly promising pharmacological properties and have the potential to be developed into therapeutically beneficial products. In particular, (E)-1-((2-(2-nitrophenoxy)-6-methylquinolin-3-yl) methylene) thiosemicarbazide (7) seems to have the potential for further investigation of its anticancer properties.
N. Preveena*, Gopalpur Nagendrappa, Amit Kumar Tiwari, M. S. Chaithanya, G. S. Nagananda, S. D. Shruthi, T. H. Suresha Kumara.
Nowadays garlic plays an important role in many diseases so that it is used as a source of medicine in human beings. So that researches are directing their efforts to determine the medical values of garlic. One of the main active principles of crushed garlic is allicin (diallylthiosulfinate), which is a defence molecule from garlic (Allium sativum L.) with a broad range of biological activities. Garlic extract has antimicrobial activity against many genera of bacteria, fungi and viruses. The chemical constituents of garlic have also been investigated for treatment of cardiovascular disease, cancer, diabetes, blood pressure and hyperlipidaemia.
Salbutamol Sulphate and bromhexine hydrochloride ascomponents of a multi-ingredient formulation is useful in asthma therapy. This article reviews the Chromatographic methods for simultaneous determination of bromhexine and salbutamol in pharmaceutical samples. The most commonly adopted methods for the determination of bromhexine and salbutamol are RP- HPLC. Recent preferences in the simultaneous estimation of bromhexine and salbutamol proves primacy of RP- HPLC and confirms a general trend of moving towards more sensitive methods having higher resolution potential, consuming small quantities of samples and reagents and requiring less time for analysis.
Sandhya N Kumar* , M. P. Kavitha , K. Krishna Kumar.
Telmisartan (TLM) is an angiotensin II receptor antagonist used in the treatment of hypertension. The aim of present investigation was to prepare Mouth dissolving tablets of an Anti-hypertensive drug Telmisartan. The solubility of poorly soluble drug was enhanced by preparing solid Dispersions of the drug with Poloxamer 407 and PEG 3350 in various concentrations by Kneading method. The optimized solid Dispersions (Drug: Poloxamer 407, 1:3 ratio) were further kneaded with suitable proportions of superdisintegrants such as; Crosscarmellose, Sodium starch glycolate and Crosspovidone. Mouth dissolving tablets of Telmisartan was prepared by direct compression method. The pre-compressive parameters for the blends and postcompressive parameters for the prepared tablets were evaluated. All formulations showed desired pre and postcompressive characteristics. FTIR study showed no evidence of drug excipient interaction. The optimized formulation was found to be F6. It was concluded that Mouth dissolving tablets of Telmisartan can be prepared by solid Dispersions of drug with Poloxamer 407 andcombination of superdisintegrants provide completeand better dissolution within in shorter period of time. Hence effective Hypertensive treatment anywhere, and anytime particularly for geriatric, pediatric, mentally ill, bedridden and patients who do not have easy access to water.
A simple and rapid stability indicating HPLC method was developed and validated for the determination of dinoprostone, naturally occurring prostaglandin E2,(PGE2) in the presence of its induced degradation products. The drug was subjected to stress acidic, alkaline, oxidative and thermal stress conditions, and the stressed samples were analyzed by the proposed method. The developed method utilized Symmetry ® C18(75 × 4.6 mm i.d., 5μm) column in an isocratic separation mode. The mobile phase consisted of phosphate buffer (pH 4.4) -acetonitrile (67: 33, v/v) at a flow rate 1mL/min with UV-detection at 200 nm. The proposed method was validated according to the International Conference on Harmonization (ICH) guidelines. The method was applied for determination of PGE2 in pure powder and in its pharmaceutical formulation. The proposed method was applied to an accelerated stability study of the compound.