Design synthesis and biological evaluation of 2-methylphenyl semicarbazone derivatives

Abstract

We have used phannacophore hybridization technique of drag design and designed a pharmacophoie model 2-inethylphenyIsemicarbazone which is having hydrogen acceptor site, hydrogen donor site, Iipophilic site etc using Ii^ndscout-2.02 software. A series of 2-iiiiethylphenyl-semicarbazone was synthesized and evaluated for their antipyretic activity using boiled cow milk induced pyrexia in rabbits. Compound 11 was, the most active compound. The possible metabolites of some selected syntheazed chalconesemicarbazones ware predicted by computational method using Pallas veirsion-3.1 ADME-Tax prediction software. The major pathway of metabolism was found to be phydroxylation and amide hydrolysis.' This work is licensed under a Creative Comrr«ns Attribution 3.0 License. You are free to copy, distribute and perform the work. You must attribute the work in the manner specified by the author or licensor.

Aryl-4,5-dihydro-1H-pyrazole-1-carboxamide Derivatives Bearing a Sulfonamide Moiety Show Single-digit Nanomolar-to-Subnanomolar Inhibition Constants against the Tumor-associated Human Carbonic Anhydrases IX and XII

“…The 4-Br substitution as R (23-25) stood out as the most efficient for providing <100 nM K I s (i.e., 38.2-45.5 nM), though a comparison can be made on a limited set of Ar substituents. By contrast, when analog Ar groups are considered, a H atom (5-11) produced better CA I inhibition than a chlorine atom (12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22).…”

“…Yield: 70%; mp: 175 • C; IR (KBr) cm 4.1.3. Synthesis of (E)-1-(4-substituted phenyl)-3-substituted Aromatic prop-2-en-1-one 4 [20,21] Substituted acetophenone (0.01 mol) and various substituted aldehydes (0.01 mol) were mixed in ethanol (40 mL) in a conical flask placed in an ice bath. To this, 60% NaOH solution (10 mL) was added dropwise with continuous stirring for 30 min (in ice bath).…”

Design, Synthesis and Biological Evaluation of 2-Anilinopyridyl-Linked Oxindole Conjugates as Potent Tubulin Polymerisation Inhibitors

“…In modern medicinal chemistry, pharmacophore hybridization approach for the synthesis of new bioactive compounds is widely used. This strategy involves hybridization of two different bioactive molecules with complementary pharmacophore functions or with different mechanisms of action, which often shows enhanced effects …”

Syntheses, silylation, characterization, and antimicrobial and antifertility activities of organoboron derivatives of some bioactive monofunctional bidentate semicarbazones

“…Semicarbazone ligands which constitute an important class of Schiff bases and their metal derivatives including those of organoboron have attracted the particular attention of several research groups possibly due to their remarkable anticancer, [1] antitumour, [2,3] antifungal, [4] antibacterial, [5] antimalarial, [6] antiproliferative, [7] antiviral, [8,9] anticoagulant, [10] antioxidant, [11] antipyretic, [12] anticonvulsant [13] and anti-inflammatory [14] activities.…”

“…All these newly synthesized complexes were characterized using elemental analyses and their probable structure was proposed on the basis of infrared, 1 H NMR, 13 C NMR, 11 B NMR and 29 Si NMR spectral data and mass spectrometry. Semicarbazone ligands and their corresponding mono-and heterodinuclear boron derivatives were screened against pathogenic bacteria (E. coli and P. aeruginosa) and fungi (A. niger and P. peniculosum) to examine their antimicrobial activities.…”