in Wiley Online Library (wileyonlinelibrary.com).Some novel [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazole derivatives were synthesized from aryl acetic acids. All the synthesized derivatives were selected for the screening of antibacterial potential against Grampositive bacteria [Staphylococcus aureus (MTCC 3160) and Micrococcus luteus (MTCC 1538)] and Gram-negative bacteria [Escherichia coli (MTCC 1652) and Pseudomonas aeruginosa (MTCC 424)] and antifungal potential against Aspergillus niger (MTCC 8652) and Candida albicans (MTCC 227), and free radical scavenging activity through 2,2-diphenyl-2-picrylhydrazyl hydrate method. The compounds TH-4, TH-13, and TH-19 were found to be more potent antimicrobial agents compared to standard drugs. The compounds TH-3, TH-9, and TH-18 also showed significant antimicrobial activity. The compound TH-13 showed antioxidant activity with IC 50 value better than the standard compound. The structures of all the synthesized compounds were confirmed by Fourier transform infrared, 1 H-NMR, liquid chromatography-mass spectrometry, and CHN analyzer.
Pyridazinones are important nitrogen-rich heterocyclic core that has been driving the substantial medicinal interest due to their wide range of biological activities. This privileged scaffold forms a central core in numerous potent compounds, which results in the development of novel anticancer drugs with fruitful biological activities. The current review article summarizes the progressive development of novel pyridazinone derivatives that are targets for numerous receptors such as C-met kinase inhibitors, PARP inhibitors, Tubulin polymerization inhibitors, Dihydro folate reductase inhibitors, B-Raf inhibitors, Bruton tyrosine kinase inhibitors, FER tyrosine kinase inhibitors, and fibroblast growth factors receptors. It features the various simple techniques for the synthesis of pyridazinones and also highlights the mechanistic insights into the anticancer properties of pyridazinone derivatives.
Due to the unusual structure and chemical composition of the mycobacterial cell wall, it is difficult to develop effective antitubercular treatment as it leads to many antibiotics not working and preventing drug entry. It also leads to the problem of more drug resistance. Tuberculosis (TB) is still the second most contagious disease with about 33% of the world's population being affected mainly by drug-resistant TB (MDR, XDR), chronic infections, and the combination of TB and human immunodeficiency virus (HIV). Therefore, there is an urgent need for the development of novel antitubercular drugs that will shorten the total duration of effective treatment taken under directly observed treatment, short-course (DOTS) guidance, solve the problem of multiple drug resistance, and provide effective treatment for TB diseases. In this review, we considered various synthetic schemes of pyrazinamide, benzimidazole, and carboxamide derivatives that have antitubercular properties that can overcome the resistance to parental drugs and thus act as an effective alternative.
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