5 research outputs found
In Silico study of 3-D structural interactions and quantitative structural drug likeness of marketed Cox-2 inhibitors
No full textIn the field of molecular modeling, docking may be a method which predicts the well-liked orientation of any molecule to a receptor to make a stable complex. Knowledge of the well-liked orientation successively could also be able to predict the strength of association or binding affinity between two molecules using, for instance, scoring functions.
Cyclooxygenase-2 (COX-2) inhibitors block cyclooxygenase-2 (COX-2), an enzyme that promotes inflammation. COX-2 enzyme converts to prostaglandin via arachidonic acid, causing pain and inflammatory responses. They are mainly present in places of inflammation and are responsible for formation of prostanoids (prostacyclins, prostaglandins and thromboxane) as part of the inflammatory response. COX-2 inhibitors are used to relieve pain raised from the inflammation.
In the present study, the marketed COX-II inhibitors are subjected for the docking study and the drug likeness study which validate that the drugs show the optimum binding energy and drug likeness score with optimum bioactive score
A study on Formulation and Evaluation of Gastroretentive tablet incorporating Ciprofloxacin Hydrochloride
No full textCiprofloxacin is a broad spectrum fluoroquinolone antibiotic effective in a broad range of infections including some difficult to treat ones. Because of wide-spectrum bactericidal activity, oral efficacy and good tolerability, it is used in Urinary tract infection, Gonorrhea, Bacterial gastroenteritis, Typhoid, Bone, soft tissue and gynecological infection, Respiratory infection and tuberculosis. The main objective of formulating the floating system was to reduce the frequency of administration, to improve patient compliance and improve bioavailability of drug by preparing a gastroretentive drug delivery system. Floating tablets of Ciprofloxacin hydrochloride were prepared by employing two different grades of control releasing polymers HPMC K4M and HPMC K100M in different concentration. Sodium bicarbonate was incorporated as a gas-generating agent. The tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating behavior, swelling studies and dissolution studies. Among tablet formulations, formulation F3 showed maximum drug release i.e. 92.25% at the end of 12 h compared with other formulations and was concluded as optimized one.
Keywords: Ciprofloxacin HCl, floating tablets, HPMC K4M, HPMC K 100M, FTIR
PRECLINICAL ASSESSMENT OF NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES FOR BREAST CANCER INTERVENTION IN ANIMAL MODELS
No full textDue to their inherent adaptability and distinctive physicochemical characteristics, the majority of heterocycle compounds and generally frequent heterocycle units found in the majority of medications now on the market have established them as genuine bases of medicinal chemistry. In addition to the medications that are now on the market, several more are being researched for their possible effectiveness in treating a variety of cancer. Specifically, these molecules inherent adaptability and dynamic core scaffold have been used in anticancer research. However, much like every other potential anticancer medication, heterocyclic compounds have drawbacks. We give a succinct summary of heterocyclic active compounds and families in this study, along with an emphasis on their primary medical uses.While examining the primary biochemical mechanisms of action, biological targets, structure-activity connections, and fundamental limitations in the utilisation of these substances, we have concentrate on those that are appropriate for cancer therapy
