Antimicrobial and Cytotoxic Activities of Some Novel Heterocycles Bearing Pyrazole Moiety

Abstract

in Wiley Online Library (wileyonlinelibrary.com).Enaminonitrile derivatives 1a and 1b were used as a versatile material for the synthesis of different heterocyclic compounds such as pyrazoloacetamide, pyrazolopyrimidinone, pyrazolobenzamide, pyrazolopyrimidines, pyrazolothiazinethione, pyrazolopyrimidinedithione, pyrazolocyanoacetamide, pyrazolopyrazole, tetrazolopyrazole, pyrazolotetrazolopyrimidine, and pyrazolotetrazolodiazepine derivatives, through the reaction with different electrophiles and nucleophiles. The newly synthesized compounds were tested against Gram-positive and Gram-negative bacteria, fungi, and two human tumor cell lines. Scheme 3. Synthetic routes for the preparation of compounds 10-12. Scheme 4. Synthetic routes for the preparation of compounds 13-17.

Conventional and microwave reactions of 1,3‐diaryl‐5,4‐enaminonitrile‐pyrazole derivative with expected antimicrobial and anticancer activities

“…Each treatment was replicated three times with SD ±0.04 mm. The standard antibiotic ampicillin was also recorded using the same procedure as above at the same concentration and solvents “1 mg/mL.” The % activity index for the complex was calculated by the formula as under: …”

“…For the above‐mentioned importance and according to our interest in synthesize new heterocyclic compounds having biological and pharmacological activities . The present work aim to prepare some novel pyrazole derivatives via reaction of 5‐amino‐3‐(4‐(dimethylamino)phenyl)‐1‐phenyl‐1H‐pyrazole‐4‐carbonitrile 1 “starting material” with different nucleophilic and electrophilic reagents, also comparison between conventional and microwave techniques in synthesis by using physical data as YE, AE, and RME.…”

Access and modulation of substituted 1-methyl-1,6-dihydropyrazolo[3,4-c]pyrazoles

“…Among this group, the pyrazolo [3,4-c]pyrazole nucleus stands out from the little attention it was given, despite previous reports of interesting biologically activities. [3][4][5][6][7] Differences in the distribution of ring electron densities and in spatial orientation between [5:5] bicyclic aromatic rings and their [6:5] and [6:6] analogs could explain these interesting therapeutic effects. 8 The synthesis of this bicyclic scaffold are scarcely found in the literature and are almost exclusively based on an existing pyrazole motif.…”

Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity

“…Besides, literature displayed many pyrazoles that have a wide array of biological activities such as neuraminidase inhibitors against influenza H1N1 virus [13], apoptotic inducers [14], antimicrobial, cytotoxic [15], and antimalarial [16] activities. Pyrazole moiety attached to enaminonitrile pyridine derivative (IV) showed anticancer activity against both HePG-2 and MCF-7 lines [17].…”