Pyridazine: A Magical Moiety

Introduction: A heterocyclic organic molecule having the chemical formula, C4H4N2. It is aromatic and has a 6-membered ring with two nearby nitrogen atoms. It has a specific heat of 208 °C and is an inert liquid. This paper presents a complete summary of the phytochemical and pharmacological activity of pyridazine as well as its derivatives published to date using new research findings and a wide variety of data. For the study, authors' scientific journal articles on pyridazine as well as its derivatives were investigated. The pharmacological properties of pyridazine as well as its derivatives include anti-cancer, anti-hypertensive, anti-allergic, anti-histaminic, eosinophil chemotaxis-inhibiting, anti-inflammatory, anti-PAF (thrombin factor), anti-HIV, and anti-histaminic effects. Conclusion: Pyridazine and its derivatives are involved in many pharmaceutical procedures. Although researchers have highlighted the crucial roles pyridazines and its derivaives that fulfills, we emphasize that further laboratory studies should be conducted in order to broaden the breadth of this compound's possible applications

5-(Biphenyl-4-yl)-3-(3-meth­oxy­benzyl­idene)furan-2(3H)-one

In the title compound, C24H18O3, the dihedral angles between the mean planes of the five-membered furan ring and the meth­oxy-substituted benzene and the adjacent and outer biphenyl benzene rings are 2.43 (7), 4.48 (7) and 30.47 (8)°, respectively. The crystal packing is stabilized by weak C—H⋯O and C—H⋯π inter­molecular hydrogen bonds and π–π stacking inter­actions [centroid–centroid distances = 3.8752 (8) and 3.8331 (8) Å]

Nano-formulations: Recent Trends for Ocular Bioavailability Enhancement

Eye is a critical part of the body that is readily available and with damage having direct effects on the life of an individual. Delivery of ocular drugs always remain challenging for healthcare professionals and scientists all over the world due to the challenges that dynamic opthalamic environment provides. These challenges involves different barriers like corneal epithelium, corneal stroma, sclera and other bio-membranes (static barriers), choroidal or conjunctival blood flow, lymphatic clearance, tear turnover (dynamic barriers) and efflux pumps/enzymes(metabolic barriers).Ocular diseases include various diseases affecting different parts of the eye. The eye presents comprehensive perspectives and difficulties in the distribution of medicaments, primarily due to the exceptional ability inherent in this mechanism for drugs to enter the main circulatory system and also for eye barrier limitations. Even if conventional non-invasive and invasive treatments like eye drops, injectable preparations and implantable devices are available but these treatments either have bioavailability issues or serious adverse eye effects. Additionally, the new concept of nanoscience and nano-technology gives new a pathway for treating ocular disease. Different active molecules were engineered to communicate with nano-carriers to pass these eye barriers and interact closely with unique specific eye tissues. This study highlights the latest advances in nano-formulations for ophthalmic diagnosis and provides discussions in the mainstream of opthalamic diseases about the role of nano-formulations in nearby future. Keywords: ocular diseases, nano-technology, static barrier, dynamic barrier, nano-carriers, bioavailability

Synthesis, characterization and potential anticonvulsants activity of various 3-(substituted)-benzylidene-7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one

639-645A number of new 3-(substituted)-benzylidene derivatives of 7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one have been synthesized and their anticonvulsant activity tested through Maximal Electroshock (M.E.S.) model and PTZ animal model by using Phenytoin and Diazepam as reference drugs respectivily. The five compounds, namely 3-(4-chlorobenzylidene)-7-chloro-5-phen­yl-1,­3-dihydro-benzo[e][1,4]diazepin-2-one 4a, 3-(2-chloro­benzyl­i­­dene)-7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diaze­pin-2-one 4b, 3(3-hydroxybenzylidene)-7-Chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 4d, 3-(4-N, N-dimethyl­benzylidene)-7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4] diaze­pin-2-one 4h and 3(4-florobenzylidene)-7-chloro5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 4j have shown significant anticonvulsant activity as compared to reference drugs

(8-Chloro-3-methyl-1H-pyrazolo[4,3-c]cinnolin-1-yl) (pyridin-4-yl)methanone

(8-Chloro-3-methyl-1H-pyrazolo[4,3-c]cinnolin-1-yl) (pyridin-4-yl)methanone 2 has been synthesized through condensation of 3-acetyl-6-chloro-1H-cinnolin-4-one 1 with isonicotinic acid hydrazide (INH) in absolute ethanol. The structure of the title compound 2 was established on the basis of IR, 1H-NMR, 13C-NMR and mass spectral data

6-Phenyl-2-(4-phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydropyridazin-3(2H)-one

6-Phenyl-2-(4-phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydro­pyridazin-3(2H)-one 3 has been synthesized by a sequence of reactions starting from 6-oxo-3-phenyl-5,6-dihydropyridazine-1(4H)-carbohydrazide 1. The structure of the title compound 3 was established on the basis of IR, 1H-NMR, 13C-NMR and mass spectral data

Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives

Background : Pain is an unpleasant and subjective sensation that results from a harmful sensorial stimulation, which alerts the body about current or potential damage to its tissues and organs. Fever is a complex physiological response triggered by infections or aseptic stimuli. Elevation in body temperature occurs when the concentration of prostaglandin E 2 (PGE 2 ) increases within parts of the brain. Triazole derivatives have been found to possess various pharmacological and biological activities, such as, anti-inflammatory, analgesics, antipyretic, and antifungal. Materials and Methods : Various 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide. The synthesized compounds were screened for in-vivo analgesic by the tail-flick method and anti-pyretic activities at a dose of 25 and 100 mg/kg body weight respectively. The antipyretic activity was evaluated using Brewer′s yeast induced pyrexia in rats. Fever was induced by subcutaneously injecting 20 ml/kg of 20% aqueous suspension of Brewer′s yeast in normal saline. Results and Discussion : The analgesic screening results revealed that the compounds 3b, 3c, and 3d exhibited excellent analgesic activity at 60 and 90 minutes compared to the standard drug (Analgin). Results revealed that the compounds 3a, 3e, and 3f significantly decreased the temperature of pyretic (P<0.001) rats at one, three and six hours after compound administration as compared to Aspirin (standard drug). Conclusion : Compounds 3b, 3c, and 3d exhibited significant analgesic activity comparable with the standard drug analgin, using the tail flick model. Compounds 3a, 3e, and 3f showed significant anti-pyretic activities comparable with the standard drug aspirin using the yeast-induced pyrexia model

6-Oxo-3-phenyl-5,6-dihydropyridazine-1(4H)-carbohydrazide

We report herein the synthesis of 6-oxo-3-phenyl-5,6-dihydropyridazine-1(4H)-carbohydrazide from β-benzoylpropionic acid and carbohydrazide by refluxing in absolute ethanol in presence of sodium acetate. The structure of the newly synthesized compound was established on the basis of IR, 1H-NMR, 13C-NMR and mass spectral data