ABSTRACT Pyrazolone is a five-membered lactam ring containing two Nitrogens and one ketonic group in its structure. Numerous pyrazolone derivatives were exhibited with diverse biological, pharmacological, and chemical applications. When pyrazolones were discovered, they were only known as NSAIDs but in recent times they play a versatile role in several complications like cerebral ischemia, cardiovascular diseases, antibacterial, antioxidant, anticancer and several other pharmacological activities. Over the last few decades, pyrazolone derivatives have been used for various biochemical applications. Some of these derivatives such as metamizole, phenazone, aminopyrine, and propyphenazone, are widely used as anti-inflammatory and analgesics. The chemistry of pyrazolone has gained increasing attention due to its diverse pharmacological properties such as anticancer, analgesic, anti-inflammatory, antimicrobial, antioxidant, antifungal, antiviral, antidiabetic, and several other biological activities. Thus, keeping because of their importance, synthetic strategies for existing as well as novel pyrazolone derivatives have been developed and explored their biochemical utility. This review deals with the various pharmacological properties of different pyrazolone derivatives and puts chemical synthetic schemes.

ABSTRACT In current review, authors aim to inspire the researcher through structure activity relationship strategy for the finding of safe and effective anticancer molecules. Nowadays cancer is measured as one of the major health problems in human beings in the world from decades. A classes of heterocyclic compounds have been recognized through molecular biology, empirical screening and rational drug development for the evaluation of anticancer molecules however regrettably, till now we could not find a medicine to be entirely active and nontoxic for the treatment of cancer patients. In pointed view, it might be measured that Thiazolidinedione (TZD) heterocyclic compounds are prodigious standing in the synthetic and pharmacological approach of medicinal chemistry. Thiazolidinedione (TZD) nucleus upon the substitution of various functional groups is provides a wide spectrum of biological activity by the use of different mechanism on different target sites. Recently, some of the substituted thiazolidinedione molecules are designed for the treatment of human cancers cell line through different molecular mechanism such as EGFR & Mushroom Tyrosine kinase inhibitor, COX enzyme inhibitors, Histone deacetylase inhibitors, Alpha glucosidase inhibitor, DNA intercalation and Protein tyrosine phosphatase 1B (PTP1B) inhibitor, basically in which PPAR gamma express are in high levels. Peroxisome proliferator-activated receptor (PPAR) gamma ligands effect on apoptosis, cell proliferation and cell differentiation on different types of cell. The most commonly cascades in human cancers cell are Raf/MEK/ERK, Wnt and PI3/Akt. This article highlights and embraces a concise overview of recent approaches for the synthesis of new thiazolidinedione molecules with its structure activity relationship strategy and effects on various signaling pathways, which is responsible for the expresses of cancer cell line activity.

We report herein the synthesis and pharmacological evaluation of a new series of 6-aryl-2-(imidazol-1-yl/1,2,4-triazol-1-yl)-2-methyl-4,5-dihydro-(2H)-pyridazin-3-one (3a-j) as potential anticonvulsant and antitubercular agents. The title compounds were prepared by reacting 6-aryl-4,5-dihydro-(2H)-pyridazin-3-one (2a-e) with formaldehyde and secondary cyclic amine imidazole or 1,2,4-triazole as per Mannich reaction. Anticonvulsant activity of pyridazinone derivatives was tested at 50 mg.kg-1 dose level against maximal electroshock (MES), isoniazid (INH, 250 mg.kg-1) and pentylenetetrazole (PTZ at 80 mg.kg-1) induced seizure methods. Phenytoin sodium (25 mg.kg-1) and sodium valproate (100 mg.kg-1) were used as reference drugs for comparison purpose. In-vitro antitubercular activity was tested by Microplate Alamar Blue assay (MABA) method and the results were compared with clinically used antitubercular agents such as INH, Pyrazinamide (PZA) and Streptomycin (STM). None of the screened compounds were found to be neurotoxic at a dose level of 100 mg.kg-1. All the screened compounds (3a-j) significantly reduced the MES, INH and PTZ induced convulsions and thus showed good anticonvulsant activity. The minimum inhibitory concentration (MIC) of the title compounds against M. tuberculosis ranged from 1.6 µg/mL to 6.25 µg/mL in comparison to INH, PZA (3.125 µg/mL) and STM (6.25 µg/mL) which indicated good antitubercular activity.

Some new 6-(substituted phenyl)-2-(4-substituted phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydropyridazin-3(2H)-one derivatives were synthesized by a sequence of reactions starting from respective aryl hydrocarbons. The final compounds (4a-i) were screened for antihypertensive activities by non-invasive method using Tail Cuff method. The compounds 4e and 4i showed appreciable antihypertensive activity.

Two series of pyridazinone derivatives (19-34) were synthesized and evaluated for antitubercular activities against Mycobacterium tuberculosis H37Rv strain. The results illustrated that among the synthesized compounds, compound 25, 5-(4-hydroxy-3-methoxybenzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone emerged as a lead compound with good antitubercular activity. Four more compounds, (21, 22, 29 & 33) were significant in their antitubercular action.

In the present investigations 4,6-diacetyl resorcinol 1 on condensation with formaldehyde and some selected amines following the Mannich reaction conditions yielded eight new Mannich bases 2a-h. It was observed that the reaction did not take place at the acetyl function but occurred at the 2-position into the aromatic ring. The compounds were characterized on the basis of elemental analysis as well as ¹H NMR and Mass spectral data. The antibacterial and antifungal activities of the title compounds were tested by the disc diffusion method using nutrient agar medium against various microorganisms such as gram positive Staphylococcus aureus and Bacillus subtilis, gram negative Escherichia coli and the fungi Aspergillus flavus and Candida albicans. Ofloxacin and voriconazole at 20 ug/mL were used as standard drugs for antibacterial and antifungal activities, respectively.

A series of amide-derivatives has been synthesized by establishing an amide linkage (-CONH-) between appropriate sulphonamide moiety and different 3-(4-substituted-benzoyl) propionic acids through one-pot reaction. The structures of the newly synthesized compounds were established on the basis of modern analytical techniques. These amides were evaluated for their antiinflammatory, ulcerogenic and antibacterial activities. Some of the compounds showed good antiinflammatory activity. Additionally, these derivatives were very low in their ulcerogenic action.