Design, Synthesis, and <i>In Vitro</i> Antioxidant Activity of 1,3,5‐Trisubstituted‐2‐pyrazolines Derivatives

Jagadish, P C; Soni, Neeraj; Verma, Amita

doi:10.1155/2013/765768

Cited by 18 publications

(18 citation statements)

References 15 publications

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“…N-Mannich base 281 derived from a 3,5-disubstituted pyrazoline (Fig. 53) had DPPH scavenging and nitric oxide scavenging activities comparable to standard antioxidants ascorbic acid and rutin; the presence of the phenolic hydroxyl group could be responsible for the antioxidant activity of this compound [435]. Finally, antioxidant activity of two C-Mannich bases 282 of uracil ( Fig.…”

Section: Antioxidant Activitymentioning

confidence: 96%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

281

110

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The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Section: Antioxidant Activitymentioning

confidence: 96%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

281

110

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“…The synthesized compounds were tested at 50 and 100 µg/mL.The results ( Table-1) show that compounds b, c and e were highly active against Aspergillus flavus, while compounds a and d were active highly against Aspergillus niger at lower concentration 50 µg/mL. in silico Studies on drug-like properties and bioactivity score on different human targets like GPCR, ion channel, kinase, nuclear receptor, protease and enzyme were predicted for newly proposed imadazole benzothiazole derivatives using OSIRIS Property Explorer and Molinspiration online tools to select best possible drug candidates [21][22][23][24]. They were subjected to predict the mutagenic, tumorigenic, irritant, reproductive risks, and drug-relevant properties and bioactivity score.…”

Section: Resultsmentioning

confidence: 99%

Antifungal Activity of Synthesized Benzothiazole Derivatives using Structure Activity Relationship

Toshniwal¹,

Bundel

Ravikant

et al. 2019

Asian J. Chem.

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Heterocyclic compounds containing N and S hetero atoms are useful material in drug research. Being a heterocyclic compound benzothiazole find use in research as a starting material for the synthesis of many bioactive structures. Several benzothiazole derivatives have been used against antiproliferative and DNA binding properties [1], anticancer and antioxidant activity against pancreatic cancer cell [2], antitumor and antiviral [3], antiinfective [4], human MCF-7cancer cell line [5], novel non-sulfamide NEDD8 activating enzyme inhibitors [6], antidepressant [7], hypoglycaemic and hypolipidemic [8], cervical cancer [9], anticonvulsant [10], anti-acetyl cholinesterase [11], kinase inhibitor [12], antituberculotic [13], antifungal [14], Candida albicans N-myristoyl transferase inhibition [15], antitumor [16], antimicrobial [17], diuretic activity [18], etc. Considering the importance of this nuclei, we have reported synthesis of some new benzothiazole derivatives by conventional method. All synthesized compounds were tested for their antifungal activity using standard drug. QSAR models first summarize a supposed relationship between chemical structures and biological activity in a data-set of chemicals. In order to select the best drug candidates for the next level of research,

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“…Hamada et al has synthesized acetoxysulfonamide pyrazole derivatives starting from substituted vanillin chalcones and were tested for antimicrobial activity against Staphylococcus aureus, Candida albicans, and for antioxidant activity, compound 24, 25 which are bearing lipophilic properties and having electron withdrawing groups exhibit great antimicrobial and antioxidant activity [38]. Furan containing pyrzoline compounds (26) having para hydroxyl group in ring A have shown better antioxidant activity than ascorbic acid and reutin [39]. Whereas 2-pyrazoline compounds (27) bearing hydroxyl and methoxy groups in ring A have shown good free radical scavenging activity [40].…”

Section: Analogues Of Chalcones Pyrazoline Analogues With Various Phamentioning

confidence: 99%

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

Sapra¹,

Sharma²

2016

Chem Sci J

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Although chalcones symbolize an important pharmacophore for variety of biological actions, however their analogues are also reported to be equally important for plethora of biological actions. In the present review, a comprehensive study of chalcones derived molecules (like pyrazoles, isoxazoles, pyridine, pyrimidine) their pharmacological actions, mechanism of action, structure activity relationship studies have been described. which includes anti-proliferative, anti-inflammatory, antioxidant, proapoptotic, anti-bacterial and anti-adhesive effects [18]. Analogues of chalcones Pyrazoline analogues with various pharmacological activities:Pyrazole nucleus present in compounds exhibit wide range of biological activity. Introduction of a pyrazole ring in the chalcones between the two aryl rings increase the cytotoxic activity against a series of human cancer cell lines. Dhar et al. [19] synthesized a series of 1-acetyl-3,5-diaryl-4,5-dihydro-(H)-pyrazoles and assayed for in vitro cytotoxicity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines, compound 1 showed broad spectrum cytotoxic activity against all the four cell lines. The activity shown by the compounds conclude that (i) Substitution on phenyl ring showed marked effect on cytotoxic activity, (ii) Presence of electron donating groups on phenyl ring led to enhanced activity whereas electron withdrawing group except NO 2 reduces the cytotoxic activity, (iii) Replacement of phenyl ring with heterocyclic ring also reduces the cytotoxic potential and napthyl ring on both sides are more beneficial for cytotoxic potential Chemical Sciences JournalChem ic a l S cience s J o u rnal

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Design, Synthesis, and In Vitro Antioxidant Activity of 1,3,5‐Trisubstituted‐2‐pyrazolines Derivatives

Cited by 18 publications

References 15 publications

Mannich bases in medicinal chemistry and drug design

Mannich bases in medicinal chemistry and drug design

Antifungal Activity of Synthesized Benzothiazole Derivatives using Structure Activity Relationship

Chalconoid Derived Heterocycles as Potent Bioactive Molecules: A Review

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