scholarly journals Synthesis and Biological Evaluation of 1,2,3-Triazole Tethered Thymol-1,3,4-Oxadiazole Derivatives as Anticancer and Antimicrobial Agents

2021 ◽  
Vol 14 (9) ◽  
pp. 866
Author(s):  
Abdulraheem S. A. Almalki ◽  
Syed Nazreen ◽  
Azizah M. Malebari ◽  
Nada M. Ali ◽  
Ahmed A. Elhenawy ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Standard Drug ◽  
E Coli ◽  
Hct 116 ◽  
Oxadiazole Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Better Than ◽  
Mcf 7

A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer and antimicrobial activities. Compounds 7, 8, 9, 10, and 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best compound against all three tested cell lines, MCF-7 (IC50 1.1 μM), HCT-116 (IC50 2.6 μM), and HepG2 (IC50 1.4 μM). Compound 9 was found to be better than the standard drugs, doxorubicin and 5-fluorouracil. These compounds showed anticancer activity through thymidylate synthase inhibition as they displayed significant TS inhibitory activity with IC50 in the range 1.95–4.24 μM, whereas the standard drug, Pemetrexed, showed IC50 7.26 μM. The antimicrobial results showed that some of the compounds (6, 7, 9, 16, and 17) exhibited good inhibition on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). The molecular docking and simulation studies supported the anticancer and antimicrobial data. It can be concluded that the synthesized 1,2,3-triazole tethered thymol-1,3,4-oxadiazole conjugates have both antiproliferative and antimicrobial potential.

scholarly journals Synthesis and biological evaluation of (3-arylisoxazol-5-yl) methyl 6-fluoro-4-oxo-4H-chromene-2-carboxylates as antioxidant and antimicrobial agents

2017 ◽  
Vol 82 (1) ◽  
pp. 1-12 ◽  
Author(s):  
Kumaraswamy Battula ◽  
Sirassu Narsimha ◽  
Vasudeva Nagavelli ◽  
Rao Srinivasa
Keyword(s):  
Antioxidant Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
Synthesis And Biological Evaluation ◽  
Antioxidant And Antimicrobial Activities

A series of novel (3-aryl-1,2-oxazol-5-yl) methyl 6-fluoro-4-oxo-4H- -chromene-2-carboxylate derivatives (C1-C12) were synthesized by Cu (I) catalyzed reaction of in situ generated nitrile oxides with prop-2-yn-1-yl 6-fluoro-4-oxo-4H-chromene-2-carboxylate in good yields and investigated their antioxidant and antimicrobial activities. Among all the synthesized compounds, C1 (IC50: 16.43 ? 0.57 ?M) and C12 (IC50:15.98 ? 0.72 ?M) have registered good antioxidant activity as compared to the standard drug Trolox. Compound-C1, C3, and C6 have registered very good inhibition against all gram-positive and gram-negative bacterial strains with MIC values ranging from 9.375 to 37.5 (?g mL-1). Compound-C7, C8, C9, C10, and C11 have registered good inhibition against B. subtilis and S. aureus with MIC values ranging from 18.75 to 37.5 (?g mL-1). Compound-C10 and C11 against P. aero-ginosa have shown prominent activity than the standard drug Penicillin (MIC: 12.5 ?g mL-1) with MIC 9.375 ?g mL-1 (~ 1.33 fold potent than Penicillin). Compound-C7, C8, and C9 have registered good to moderate antifungal activity against four tested fungal strains with MIC values ranging from 18.75 and 37.5 ?g mL-1

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Synthesis and biological evaluation of novel 2-(1H-imidazol-2-ylmethylidene)hydrazinyl- 1,3-thiazoles as potential antimicrobial agents

2015 ◽  
Vol 21 (2) ◽  
Author(s):  
Krzysztof Z. Łączkowski ◽  
Katarzyna Jachowicz ◽  
Konrad Misiura ◽  
Anna Biernasiuk ◽  
Anna Malm
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

AbstractSynthesis, characterization, and investigation of antimicrobial activities of nine novel imidazolylthiazoles are presented. Their structures were determined using

scholarly journals Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 539 ◽  
Author(s):  
Sraa Abu-Melha ◽  
Mastoura Edrees ◽  
Heba Salem ◽  
Nabila Kheder ◽  
Sobhi Gomha ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Hepatoprotective Activity ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Biological Assays ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation

A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, 11c and 6g, being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl4-induced hepatotoxicity.

scholarly journals Naproxen Based 1,3,4-Oxadiazole Derivatives as EGFR Inhibitors: Design, Synthesis, Anticancer, and Computational Studies

2021 ◽  
Vol 14 (9) ◽  
pp. 870
Author(s):  
Mohammad Mahboob Alam ◽  
Syed Nazreen ◽  
Abdulraheem S. A. Almalki ◽  
Ahmed A. Elhenawy ◽  
Nawaf I. Alsenani ◽  
...  
Keyword(s):  
Docking Studies ◽  
Biological Data ◽  
Egfr Inhibitors ◽  
Design Synthesis ◽  
Standard Drug ◽  
Egfr Inhibition ◽  
Hct 116 ◽  
Oxadiazole Derivatives ◽  
Hct 116 Cells ◽  
Mcf 7

A library of novel naproxen based 1,3,4-oxadiazole derivatives (8–16 and 19–26) has been synthesized and screened for cytotoxicity as EGFR inhibitors. Among the synthesized hybrids, compound2-(4-((5-((S)-1-(2-methoxynaphthalen-6-yl)ethyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol(15)was the most potent compound against MCF-7 and HepG2cancer cells with IC50 of 2.13 and 1.63 µg/mL, respectively, and was equipotent to doxorubicin (IC50 1.62 µg/mL) towards HepG2. Furthermore, compound 15 inhibited EGFR kinase with IC50 0.41 μM compared to standard drug Erlotinib (IC50 0.30 μM). The active compound induces a high percentage of necrosis towards MCF-7, HePG2 and HCT 116 cells. The docking studies, DFT and MEP also supported the biological data. These results demonstrated that these synthesized naproxen hybrids have EGFR inhibition effects and can be used as leads for cancer therapy.

scholarly journals Phthalazines and phthalazine hybrids as antimicrobial agents: Synthesis and biological evaluation

2019 ◽  
Vol 44 (1-2) ◽  
pp. 31-41
Author(s):  
Asmaa Kamal Mourad ◽  
Abdelmoneim Abdelsalam Makhlouf ◽  
Ahmed Yousef Soliman ◽  
Samar Ahmed Mohamed
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Standard Drug ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Benzoic Acid Derivative ◽  
Microbial Strains ◽  
Synthesis And Biological Evaluation

Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. Herein, a benzoic acid derivative (2), a benzoxazin-1-one derivative (3), and an oxophthalazin-2(1 H)-yl)acetohydrazide (13) are utilized as precursors to construct a novel series of phthalazinones bearing various valuable functional groups in excellent yields via several simple and promising approaches. Finally, the antimicrobial activity of the newly synthesized phthalazines is screened against different microbial strains; namely, Gram-negative and Gram-positive bacteria utilizing Amoxicillin as a standard drug.

Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohan H. Patil ◽  
Uma D. Kabra ◽  
Krishna R. Gupta ◽  
Milind J. Umekar
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

scholarly journals Design, Synthesis and Biological Evaluation of Pyrimidine Analogues as SecA Inhibitors

2021 ◽  
Author(s):  
FANTE BAMBA ◽  
Jinshan Jin ◽  
Arpana S. Chaudhary ◽  
Phang C. Tai ◽  
Binghe Wang
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
E Coli ◽  
Secretion Pathway ◽  
Antimicrobial Studies ◽  
Pyrimidine Analogues ◽  
Pyrimidine Analogs ◽  
Synthesis And Biological Evaluation

Abstract SecA, a key component of the bacterial Sec-dependent secretion pathway, is an attractive target for the development of new antimicrobial agents. We have previously reported pyrimidine analogs as SecA inhibitors. Herein, we report an extension of the earlier work in the synthesis and evaluation of a series of 15 5-cyanothiouracil derivatives as SecA inhibitors. All the compounds have been evaluated for their inhibition of SecA ATPase (EcSecAN68) and for their antimicrobial activity against Escherichia coli NR698 (a leaky mutant) and Bacillus anthracis Sterne. Twelve compounds showed IC50 of less than 6.3 µM when tested against EcSecAN68. In antimicrobial studies against E. coli NR698, six compounds showed MIC of less than 12.5 µM with three being less than 6.3 µM. Against B. anthracis Sterne, three compounds showed MIC of less than 6.3 µM.

scholarly journals Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

RSC Advances ◽  
2019 ◽  
Vol 9 (33) ◽  
pp. 19065-19074 ◽  
Author(s):  
Hatem A. Abuelizz ◽  
Hanem M. Awad ◽  
Mohamed Marzouk ◽  
Fahd A. Nasr ◽  
Ali S. Alqahtani ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Ms Analysis ◽  
Normal Human ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation ◽  
Mcf 7

A series of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids (1–17) was successfully synthesized and their structures were established by NMR and MS analysis. Their anticancer activity against HCT-116, MCF-7 and normal human RPE-1 cells were examined.

Synthesis and biological evaluation of a new class of quinazolinoneazoles as potential antimicrobial agents and their interactions with calf thymus DNA and human serum albumin

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 222-229 ◽  
Author(s):  
Li-Ping Peng ◽  
Sangaraiah Nagarajan ◽  
Syed Rasheed ◽  
Cheng-He Zhou
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Calf Thymus Dna ◽  
New Class ◽  
Calf Thymus ◽  
Synthesis And Biological Evaluation

A series of quinazolinone azoles were synthesized and screened for their antimicrobial activities, and further studies of their binding behaviors with calf thymus DNA and human serum albumin were investigated.

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