Probiotic Formulations: A Patent Landscaping Using the Text Mining Approach.

The outstanding research outcomes and registrations of myriads of probiotic strains have flooded the health market with various innovative probiotic-based products and their patents. The study of patented formulations of probiotics can give an overall insight into its existing application. A landscaping review of patents for probiotic-based preparations is presented in the current work. The patent search was performed over commercially available patent databased and analysis tool-PatSeer Pro®. Search strings containing words "Formulation" and "Composition" resulted in more than 3700 patents. Landscaping review of 400 + patents from the last 20 years (2000-2020) was performed using the Text-Mining approach. Text-Mining helped to identify 19 technological clusters which represent these patents. These clusters include the patents of probiotic preparations on animal feed, human food, cosmetics, antimicrobial, antidiabetic, arthritis, etc. A review of this massive number of patents unveiled many exciting preparations. Probiotic-based innovative products for depression, diabetes, Parkinson's, tumor, acne, and animal husbandry are reviewed comprehensively. The present work also unravels a few new-flanged products like probiotic layered condoms, products for acute alcoholism, and traditional Chinese medicine with probiotics. The patent landscape of probiotic-based preparations has presented a whole scenario of probiotic-based preparations. It has also revealed many unexplored areas where innovation can be excelled.

Design, synthesis, molecular docking, and antibacterial evaluation of some novel flouroquinolone derivatives as potent antibacterial agent.

OBJECTIVE: Quinolone moiety is an important class of nitrogen containing heterocycles widely used as key building blocks for medicinal agents. It exhibits a wide spectrum of pharmacophores and has bactericidal, antiviral, antimalarial, and anticancer activities. In view of the reported antimicrobial activity of various fluoroquinolones, the importance of the C-7 substituents is that they exhibit potent antimicrobial activities. Our objective was to synthesize newer quinolone analogues with increasing bulk at C-7 position of the main 6-fluoroquinolone scaffold to produce the target compounds which have potent antimicrobial activity. METHODS: A novel series of 1-ethyl-6-fluoro-4-oxo-7-{4-[2-(4-substituted phenyl)-2-(substituted)-ethyl]-1-piperazinyl}-1,4-dihydroquinoline-3-carboxylic acid derivatives were synthesized. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed using topoisomerase II DNA gyrase enzymes (PDB ID: 2XCT) by Schrodinger's Maestro program. In vitro antibacterial activity of the synthesized compounds was studied and the MIC value was calculated by the broth dilution method. RESULTS: Among all the synthesized compounds, some compounds showed potent antimicrobial activity. The compound 8g exhibited good antibacterial activity. CONCLUSION: This investigation identified the potent antibacterial agents against certain infections.

Bernthsen synthesis, antimicrobial activities and cytotoxicity of acridine derivatives.

The condensation reaction of diphenylamine with 2-oxo-2H-(substituted chromen)-4-yl acetic acid in presence of anhydrous zinc chloride afford 4-(acridine-9-ylmethyl)-2H-(substituted chromen)-2-one. The synthesized compounds were characterized by spectral studies and elemental analysis and screened for their in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus pyogenes (gram +ve), Escherichia coli, Pseudomonas aeruginosa (gram -ve) and antifungal activity against Aspergillus niger and anticancer activity (HL-60, Hep-2 & HEK293T) by MTT assay. Chloro substituted compounds showed antimicrobial and anticancer activity with IC(50) values in the low micromolar range.

Design, Synthesis and Molecular Docking of 1-Cyclopropyl-6- Fluoro-4-Oxo-7-{4-[2-(4-Substituted-Phenyl)-2-(Substituted)-Ethyl] -1-Piperazinyl}-1,4-Dihydroquinoline-3-Carboxylic Acid as an Antimicrobial Agents.

BACKGROUND: Quinolone scaffolds are widely used for the synthesis of a number of medicinal compounds with variety of biological activity. In view of the reported antimicrobial activity of various fluoroquinolones, the structure activity studies of various substituted quinolones, which proved the importance of the C-7 substituents to exhibit potent antimicrobial activities. OBJECTIVE: Based on the structural activity relationship at C-7 position it was rationalized to design and synthesize new quinolone derivatives with increasing bulk at C-7 position of the main 6-fluoroquinolone scaffold. METHODS: A novel series of 1-cyclopropyl-6-fluoro-4-oxo-7-{4-[2-(4-substituted-phenyl)- 2-(substituted)-ethyl]-1-piperazinyl}-1,4-dihydroquinoline-3-carboxylic acid derivatives were synthesized by reacting 1-cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4- dihydroquinoline-3-carboxylic acid with 2-bromo-4-(substituted) acetophenone in the presence of sodium bicarbonate to obtain 1-cyclopropyl-6-fluoro-7-{4-[2-(4- substitutedphenyl)-2-oxoethyl]-1-piperazinyl}-4-oxo-1,4-dihydroquinoline-3-carboxylic acids 2a-2d. Compound 2a-2d underwent further reaction with different substituted hydrazide, hydroxylamine hydrochloride or methoxylamine in glacial acetic acid to give 3a-7d. In vitro antibacterial activity of the synthesized compounds 3a-7d was studied and the MIC value was determined by the broth dilution method. RESULT: Among all the synthesized compounds 3a-7d some compounds showed antimicrobial activity in comparison to the reference standard ciprofloxacin. CONCLUSION: The compound 6d showed the reasonable good antibacterial activity among all the tested compounds. To understand antibacterial data on structural basis and the interaction of binding sites with bacterial protein receptor, the docking studies were carried out using topoisomerase II DNA gyrase enzymes (PDB ID. 2XCT) by shrodinger's maestro program.