Novel pyrazole–pyrazoline hybrids endowed with thioamide as antimalarial agents: their synthesis and 3D-QSAR studies

Abstract

One of the most viable options to tackle the growing resistance to the antimalarial drugs is hybrid molecules. It involves combination of different scaffolds in one frame that may lead to compounds with diverse biological profiles. In this context, new hybrids of three different scaffolds viz pyrazole, pyrazoline and thiosemicarbazone moiety were incorporated into one single compound and evaluated for their in vitro schizontocidal activity against the CQ-sensitive 3D7 strain of Plasmodium falciparum. Compounds with significant in vitro antimalarial activity were further evaluated for cytotoxicity against VERO cell lines. The best active compound 48 exhibited an IC 50 of 1.13 mM. The in vitro results were further validated by quantitative structure-activity relationship (QSAR).

Water Mediated Direct Thioamidation of Aldehydes at Room Temperature

“…With sustained interest in the development of novel synthetic strategies, we intended to develop an innovative protocol for the synthesis of thioamides. Structurally diverse thioamides are the precursor for the synthesis of many heterocyclic and natural products. , Thioamides, the synthetic isostere of amides, are being exploited to have improved pharmacological properties to that of amide-containing drugs . The thiocarbonyl group is an integral part of many active drugs such as antithyroid, antituberculosis, androgen receptor agonist, and antimetabolite .…”

Novel Bis(2‐cyanoketene‐S,S‐/S,N‐acetals): Versatile Precursors for Novel Bis(aminopyrazole) Derivatives

“…Pyrazole ring also constitutes a basic bit of well‐established drugs with diverse therapeutic activities like zoniporide, betazole, celecoxib, lonazolac, fezolamine, difenamizole, mepirizole, and rimonabant (Fig. ) . In addition, pyrazole ring is included in well‐known natural products that have various pharmacological properties .…”

Synthesis, Structure‐Activity Relationship and Antimicrobial Evaluation of Methyl‐Substituted Tetrazoloquinoline‐Based Pyrazolinethioamides

“…The anti‐influenza activities of thioamides have been elucidated . Additionally, the thioamides exhibit higher in vitro anti‐malarial, anti‐tumoral, antimycobacterial and antifungal activity than the corresponding amides . Pyrazoles gained much attention as antimicrobial agents after the discovery of natural pyrazole C‐glycoside pyrazofurin which showed broad spectrum of antimicrobial activity .…”