Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

Desai, N. C.; Bhatt, Malay J.

doi:10.18052/www.scipress.com/ilcpa.66.109

Cited by 5 publications

(3 citation statements)

References 34 publications

(30 reference statements)

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“…In the synthesis of pyrazoline derivate, various factors affected the parameters that needed to be considered when synthesis took place to get better product results, one of which was: [ 40 ]…”

Section: Pyrazoline Derivate Synthesis Parametersmentioning

confidence: 99%

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

Praceka

Megantara

Maharani

et al. 2021

J Adv Pharm Technol Res

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Pyrazoline plays an important role in the development of heterocyclic chemistry theory and is widely used as a synthesis useful in organic synthesis. The structure of the pyrazoline derivative compound contains a 5-membered heterocyclic framework with two nitrogen atoms and one endocyclic double bond. The function of pyrazoline as a fragment was stable enough in the bioactive group to synthesize new compounds with various biological activities. Various methods that could be used for the synthesis of pyrazole derivatives were ultrasonic irradiation, microwave assistance, ionic liquids, grinding techniques, and conventional methods. However, the synthesis of pyrazoline derivatives using conventional methods had many problems, one of which is the product yield, which was <70%. Therefore, this article will discuss the importance of optimizing the synthesis reaction conditions by taking into account several synthesis parameters to get the best organic product results based on conventional methods. A literature search was conducted by employing PubChem, Chemspider Google Scholar, Research Gate, Science Direct, and Elsevier by selecting pyrazoline synthesis based on physicochemical profile, reaction mechanism, and synthesis method.

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Section: Pyrazoline Derivate Synthesis Parametersmentioning

confidence: 99%

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

Praceka

Megantara

Maharani

et al. 2021

J Adv Pharm Technol Res

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show abstract

“…In particular, they are described as inhibitors of protein glycation, antimicrobial [37,38], antidepressant [39,40], anticonvulsant [41], antifungal [42,43], and antitubercular [44,45], anticonvulsant [46], DPPH radical Scavenging, anti-diabetic [47], antiamebic [48], as well as antiviral agents [49]. Pyrazole analogoues can selectively inhibit (cyclooxygenase enzyme) COX-2 [50] they are also expressing antiinflammatory [51], analgesic [52], antihypertensive, antipyretic, sedatives, and antidiabetic activities [53][54][55].…”

Section: Introductionmentioning

confidence: 99%

<i>In vitro</i> Anti Leukemia Cancer Activity of Some Novel Pyrazole Derivatives and Pyrazoles Containing Thiazole Moiety

Moustafa¹

2019

AJHC

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The design and syntheses of several novel pyrazole derivatives (2, 5, 6 and 7) and pyrazole derivatives (3 and 4) containing thiazole moiety via by ethyl β-(p-chlorophenyl)-α-cyanoacrylate (1) and thiosemicarbazide as starting materials. Pyrazole derivatives (3 and 4) containing thiazole moiety were synthesized via cyclization of pyrazole derivative (2) with bromomethyl arylketones, to give compound 3, followed by acetylation. N-(3-methoxy-2-hydroxybenzal) -3-(pchlorophenyl)-4-cyano-5-oxopyrazol-1-thiocarboxamide (6) was synthesized via reaction of compound 2 with 3-methoxy-2hydroxybenzaldehyde. Structures of all compounds were confirmed by elemental analysis, FT-IR, 1 H-NMR, 13 C-NMR and mass spectrometry. The cytotoxic activity of all the synthetic compounds were evaluated against Leukemia HL-60 compared with Doxorubicicn. The cytotoxic activity was checked in vitro for the recently prepared compounds by using the MTT assay. Compounds 4, 6 and 9 were the most active against Leukemia HL-60. The IC 50 values of them were less than 5 µM in the range of 1.35-4.78 µM. In addition, compounds 3 and 5 showed less antiproliferative activity against Leukemia HL-60 cells with IC 50 values in the range 5.39-8.82 µM. Compound 6 was the most potent cytotoxic activity. The studies biological activity includes cell cycle analysis, apoptosis detection assay and Topoisomerase II inhibition activity assay explained that compound 6 is a strong Topo II inhibitor.

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“…Encouraged by the above-mentioned explanation, we have focused onto construct some novel antimicrobial derivatives containing pyrazole, 1,3,4-oxadiazole and pyridine scaffolds screened for antimicrobial activity. Previously our research group has worked on the synthesis of pyrazole and their derivatives as potential antimicrobials [22][23][24]. In furtherance to this, N- (…”

Section: Introductionmentioning

confidence: 99%

Hybrid Approach for Synthesis and Antimicrobial Activity of Heterocyclic Compounds

Desai¹,

Vaja²

2018

ILCPA

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Abstract. We have synthesized novel series of N- (1-(2-(1-phenyl-3-(p-tolyl)-1H-pyrazol-4-yl)-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl)ethylidene)arylaniline and their derivatives. The structures of synthesized compounds were well characterized by spectroscopic techniques. Antimicrobial activity of the newly synthesized derivatives was evaluated against gram positive (S. aureus and S. pyogenes), gram negative bacteria (E. coli and P. aeruginosa), and strains of fungi (C. albicans, A. niger and A. clavatus). Among the screened derivatives 5c, 5f, 5i, 5l and 5t demonstrated superior antimicrobial activity against microbial strains.

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Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

Cited by 5 publications

References 34 publications

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

<i>In vitro</i> Anti Leukemia Cancer Activity of Some Novel Pyrazole Derivatives and Pyrazoles Containing Thiazole Moiety

Hybrid Approach for Synthesis and Antimicrobial Activity of Heterocyclic Compounds

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Optimized Synthesis of Novel Pyrazole Based Thiazole Derivatives and their Antimicrobial Evaluation

Cited by 5 publications

References 34 publications

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

Comparison of various synthesis methods and synthesis parameters of pyrazoline derivates

&lt;i&gt;In vitro&lt;/i&gt; Anti Leukemia Cancer Activity of Some Novel Pyrazole Derivatives and Pyrazoles Containing Thiazole Moiety

Hybrid Approach for Synthesis and Antimicrobial Activity of Heterocyclic Compounds

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<i>In vitro</i> Anti Leukemia Cancer Activity of Some Novel Pyrazole Derivatives and Pyrazoles Containing Thiazole Moiety