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Article
Design and synthesis of butenolide-based amide derivatives as anti-inflammatory agents
Butenolide-based eighteen new amide derivatives (1–18) have been synthesized and evaluated for anti-inflammatory activity. The compounds 9, 17 and 4 exhibited significant in vivo inhibition of 84.69, 76.52 and 76...
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Article
Synthesis, characterization, in vitro antimicrobial, and anthelmintic evaluations of 2-(4-chloro-3-methylphenoxy)-N′-[{5′-(substituted aryl)-furan-2′-yl}-methylidene]-acetohydrazides
In the present study, a novel series of 2-(4-chloro-3-methylphenoxy)-N′-[{5′-(substituted aryl)-furan-2′-yl}-methylidene]-acetohydrazides (4a–k) have been designed and synthesized with a new class of p-chloro-m-...
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Article
Essential aminoacid incorporated GABA–phthalimide derivatives: synthesis and anticonvulsant evaluation
A series of novel N-(2-(benzylamino)-1-substituted-2-oxoethyl)-4-(1,3-dioxoisoindolin-2-yl)butanamide derivatives were synthesized unifying the functionalized amino acid unit and GABA–phthalimide moiety with esse...
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Article
Synthesis, biological activities, and pharmacokinetics studies of a mutual prodrug of aceclofenac and paracetamol
An ester-based mutual prodrug (aceclofenac–paracetamol; AC-PR) was synthesized (one-pot method) with an aim of improving the therapeutic index through prevention of gastrointestinal irritation and bleeding tha...
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Article
Docking studies on butenolide derivatives as Cox-II inhibitors
To supplement hits from a high through put screening, a docking study on butenolides derivatives was performed as COX-II inhibitors. The fourteen ligands were docked inside the ligand-binding domain (LBD) of p...
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Article
Pharmacophore modeling studies on N-hydroxyphenyl acrylamides and N-hydroxypyridin-2-yl-acrylamides as inhibitor of human cancer leukemia K562 cells
In order to understand the essential structural features for inhibitors of human cancer leukemia K562 cells, three-dimensional pharmacophore hypotheses were built on the basis of a set of inhibitors of human c...
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Article
Synthesis and antimicrobial activity of bischalcone derivatives
Several bischalcones (2a–h and 5a–e) and flavones (3a–f) were synthesized and evaluated for their antimicrobial actions. Bischalcones were prepared by condensing 1,1′-(4,6-dimethyl-1,3-phenylene)diethanone (1) or...
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Article
Quinolone derivatives as antitubercular drugs
New chemotherapeutic drugs are the need to improve tuberculosis (TB) control particularly due to the emergence of multidrug-resistant strains and extensively drug-resistant strains of TB. These antitubercular ...
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Article
Studies on fused heterocyclic 3,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazoles: synthesis and biological evaluation
In this study, a series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles (5a–t) were synthesized by condensing 4-amino-3-mercapto-(4H)-1,2,4-triazoles (4a–c) with different aromatic or aroyl acids t...