Design, Synthesis and Biological Evaluation of Novel Benzothiazole
Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

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Amidine Sulfonamides and Benzene Sulfonamides: Synthesis and Their Biological Evaluation

Journal of Chemistry ◽

10.1155/2015/524056 ◽

2015 ◽

Vol 2015 ◽

pp. 1-8 ◽

Cited By ~ 5

Author(s):

Muhammad Abdul Qadir ◽

Mahmood Ahmed ◽

Hina Aslam ◽

Sadia Waseem ◽

Muhammad Imtiaz Shafiq

Keyword(s):

Spectral Analysis ◽

New Products ◽

Biological Evaluation ◽

Bacterial Strains ◽

Antifungal Activities ◽

E Coli ◽

Antibacterial And Antifungal Activities ◽

Ft Ir ◽

Antibacterial And Antifungal

New amidine and benzene sulfonamide derivatives were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial and antifungal activities against medically important bacterial strains, namely,S. aureus, B. subtilis, andE. coli, and fungi, namely,A. flavus, A. parasiticus, andA.sp. The antibacterial and antifungal activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds3b,9a, and9bhave most potent activity againstS. aureus, A. flavus, and A. parasiticus, respectively, and were found to be more active than sulfamethoxazole and itraconazole with MIC values 40 μg/mL. In contrast, all the compounds were totally inactive against theA.sp. except10band15bto show activity to some extent.

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Design, Synthesis and Antibacterial Activity of Coumarin-1,2,3-triazole Hybrids Obtained from Natural Furocoumarin Peucedanin

Molecules ◽

10.3390/molecules24112126 ◽

2019 ◽

Vol 24 (11) ◽

pp. 2126 ◽

Cited By ~ 6

Author(s):

Alla V. Lipeeva ◽

Danila O. Zakharov ◽

Liubov G. Burova ◽

Tatyana S. Frolova ◽

Dmitry S. Baev ◽

...

Keyword(s):

Antibacterial Activity ◽

Cycloaddition Reaction ◽

Bacterial Strains ◽

Design Synthesis ◽

Docking Simulations ◽

E Coli ◽

Antibiotic Drugs ◽

In Vitro Antibacterial Activity ◽

Substituted Coumarins

Synthesis of 1,2,3-triazole-substituted coumarins and also 1,2,3-triazolyl or 1,2,3-triazolylalk-1-inyl-linked coumarin-2,3-furocoumarin hybrids was performed by employing the cross-coupling and copper catalyzed azide-alkyne cycloaddition reaction approaches. The synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillius subtilis, Actinomyces viscosus and Escherichia coli bacterial strains. Coumarin-benzoic acid hybrids 4с, 42с and 3-((4-acetylamino-3-(methoxycarbonyl)phenyl)ethynyl)coumarin (29) showed promising activity against S. aureus strains, and the 1,2,3-triazolyloct-1-inyl linked coumarin-2,3-furocoumarin hybrid 37c was endowed with high selectivity against B. subtilis and E. coli species. The in vitro antibacterial activity of 4с, 29, 37c and 42с can potentially be compared with that of a number of modern antibiotic drugs used in the clinic, suggesting promising prospects for further research. A detailed study of the molecular interactions with the targeted protein MurB was performed using docking simulations and the obtained results are quite promising.

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Synthesis and biological evaluation of new hydrazide-Schiff bases

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v10i3.23381 ◽

2015 ◽

Vol 10 (3) ◽

pp. 555 ◽

Cited By ~ 1

Author(s):

Asif Husain ◽

Munendra M. Varshney ◽

Versha Parcha ◽

Aftab Ahmad ◽

Shah Alam Khan

Keyword(s):

Schiff Bases ◽

Anthelmintic Activity ◽

Biological Evaluation ◽

Gram Negative Bacteria ◽

Bacterial Strains ◽

E Coli ◽

New Class ◽

Antibacterial Screening ◽

Synthesis And Biological Evaluation

<div>A new series of N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides were synthesized with a new class of Schiff bases derived from the reaction of substituted phenyl-1-ketohydrazide 2 or 2-(4-chloro-3-methylaryloxy) acetohydrazide 3 with different 5-(substituted aryl)-2-furfuraldehyde (1a-k) to yield substituted N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides-Schiff bases (4a-f, 4g-k). The title compounds were subjected to in vitro antibacterial screening against Gram positive bacterial strains- S. aureus, B. cereus, E. faecalis and S. epidermidis, and Gram negative bacteria strains- E. coli, S. typhi, S. dysenteriae and K. pneumoniae. The synthesized Schiff bases were also evaluated for their anthelmintic activity against two species of earthworms (Pheritima posthuma and Perionyx excavates). Some compounds have shown promising antibacterial and anthelmintic activities.</div>

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Design, synthesis and biological evaluation of new substituted benzofuran-based derivatives via C−H bond activation

Journal of the Serbian Chemical Society ◽

10.2298/jsc191231039p ◽

2020 ◽

Vol 85 (11) ◽

pp. 1405-1415

Author(s):

Behjat Pouramiri ◽

Mahboobeh Zahedifar ◽

Adileh Ayati ◽

Farah Pouramiri ◽

Mahdiyeh Ahmadi

Keyword(s):

Bond Activation ◽

Biological Evaluation ◽

Biologically Active ◽

Spectroscopic Methods ◽

Design Synthesis ◽

Activation Reaction ◽

Chemical Structures ◽

Synthesis And Biological Evaluation

A series of biologically active disubstituted benzofuran derivatives (3a?d) have been designed and synthesized via C?H bond activation reaction. The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro anti acetylcholinesterase (AChE) activities of these novel compounds were evaluated and showed low to moderate results. Among them, compound 3d moderately inhibited AChE activities with 68.12 % value.

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Design, Synthesis, and Biological Evaluation of Camptothecin Loaded Biotinylated Cellulose Nanowhiskers as Anticancer Agents

Journal of Contemporary Medical Sciences ◽

10.22317/jcms.v7i3.960 ◽

2021 ◽

Vol 7 (3) ◽

Keyword(s):

Anticancer Agents ◽

Biological Evaluation ◽

In Vitro Cytotoxicity ◽

Cellulose Nanowhiskers ◽

Design Synthesis ◽

Chemical Structures ◽

Release Assay ◽

Selective Chemotherapy ◽

Mcf 7

Objective: Using biotinylated cellulose nanowhiskers (CNWs), we designed and synthesized a Glutathione (GSH) sensitive- Camptothecin (CPT) prodrug for selective CPT delivery (compound 12). Methods: CPT-biotin (compound 9), was synthesized by direct conjugation of CPT to the biotin via GSH sensitive linkage to evaluate the role of CNWs in compound 12. The chemical structures of the synthesized prodrugs were confirmed by FT-IR, 1H NMR, 13C NMR, and ESI-MS, while the nanoparticles were characterized by DLS and TEM. Results: The in-vitro drug release assay demonstrated that only 18.6% of CPT was released from the nano conjugate under GSH stimulation at micromolar level (100 μM), while 83.1% accumulative release rate was achieved under GSH stimulation at millimolar level (10 mM). The in-vitro cytotoxicity assay (MTT assay) demonstrated that compound 9showed higher inhibition ratios on biotin positive cells, MCF-7, and HepG2, and lower cytotoxicity on biotin negative, CHO. Compound 12 showed good activity against MCF-7, HepG2, and much lower cytotoxicity on CHO. Conclusion: This work demonstrates CPT-biotinylated cellulose nanowhiskers for selective chemotherapy and may have the potential to be used for cancer targeting.

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DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF NOVEL BENZOTHIAZOLE BASED [1, 2, 4]-TRIAZOLO [4, 3-A] QUINOXALINE DERIVATIVES

INDIAN DRUGS ◽

10.53879/id.56.09.11901 ◽

2019 ◽

Vol 56 (09) ◽

pp. 22-29

Author(s):

R. V. Gadhave ◽

B. S Kuchekar ◽

Keyword(s):

Radical Scavenging ◽

Antidepressant Activity ◽

Biological Evaluation ◽

Active Compounds ◽

Design Synthesis ◽

Antioxidant Power ◽

Structural Modifications ◽

Quinoxaline Derivatives ◽

Ferric Reducing Antioxidant Power ◽

Target Molecules

Quinoxaline, triazole and benzothiazole heterocycles plays an important role in modulating biological activity. The present work describes the biological evaluation of target molecules designed using autodock vina docker. Novel benzothiazole based [1, 2, 4]-triazolo [4, 3-a] quinoxalines were synthesized by condensation of substituted 2-amino benzothiazoles and 4-chloro triazoloquinoxalines. The synthesized compounds were characterized by analysis of physical and spectral data. All synthesized compounds were screened for antioxidant activity using 1, 1-Diphenyl-2-picrylhyrazyl radical scavenging, Hydrogen peroxide scavenging and Ferric reducing antioxidant power Method. The compounds 10g and 10i were found to be most active compounds of this series and other compounds showed moderate to less activity when compared with ascorbic acid. Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as antimicrobial, anti-inflammatory, anticancer and antidepressant, activity.

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Novel Triazine Centred Manganese Based Complex: A Photophysical and Biological Studies

Asian Journal of Chemistry ◽

10.14233/ajchem.2020.22302 ◽

2019 ◽

Vol 32 (1) ◽

pp. 91-94

Author(s):

L. Alphonse ◽

P. Tharmaraj ◽

B. Avila Josephine ◽

V. Mary Teresita

Keyword(s):

Antimicrobial Activity ◽

Metal Complex ◽

Diffusion Method ◽

Bacterial Strains ◽

Fluorescent Properties ◽

E Coli ◽

Physico Chemical ◽

Biological Studies ◽

Ft Ir

In this work, Mn(II) complex of triazine based ligand has been synthesized and characterized using various physico-chemical methods including C,H,N elemental analysis, FT-IR, 1H NMR and EI-mass analysis. The synthesized compounds serve as potential photoactive material as indicated from its characteristic fluorescent properties. The ligand and its metal complex were assayed for in vitro antimicrobial activity on four bacterial strains (S. aureus, B. subtilis, E. coli and K. pneumoniae) using well-diffusion method and it was observed that metal complex showed enhanced antimicrobial activity against all tested strains as compared to ligand.

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Design, synthesis and in vitro biological evaluation of oligopeptides targeting E. coli type I signal peptidase (LepB)

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2016.12.003 ◽

2017 ◽

Vol 25 (3) ◽

pp. 897-911 ◽

Cited By ~ 5

Author(s):

Maria De Rosa ◽

Lu Lu ◽

Edouard Zamaratski ◽

Natalia Szałaj ◽

Sha Cao ◽

...

Keyword(s):

Biological Evaluation ◽

Signal Peptidase ◽

Type I ◽

Design Synthesis ◽

E Coli

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Synthesis and antimicrobial activity of some new pyrazoline derivatives bearing sulfanilamido moiety

European Journal of Chemistry ◽

10.5155/eurjchem.10.1.30-36.1791 ◽

2019 ◽

Vol 10 (1) ◽

pp. 30-36 ◽

Cited By ~ 5

Author(s):

Maysoon Mohammed Almahdi ◽

Ahmed Elsadig Mohammed Saeed ◽

Nadia Hanafy Metwally

Keyword(s):

Antimicrobial Activity ◽

Moderate Activity ◽

Gram Positive ◽

Standard Drug ◽

Gram Negative ◽

E Coli ◽

Chemical Structures ◽

In Vitro Antibacterial Activity ◽

Ft Ir

In the present study, a series of new pyrazoline derivatives bearing sulfanilamido moiety were synthesized and obtained in good yields. The chemical structures of the compounds were elucidated by spectral data (FT-IR, MS, UV-VIS and NMR). The synthesized compounds 41-70 were screened for their antimicrobial activity and compared with controls. The in vitro antibacterial activity of compounds 41-45 and 48-57 was checked against two Gram positive microorganisms (S. aureus and S. mutans) and three Gram negative microorganisms (E. coli, K. pneumonia and P. aureginosa), their antifungal activity was checked against C. albicans. The preliminary results showed that these compounds had moderate activity against the tested organisms. Compounds 41, 48, 51 and 56 exhibited promising antimicrobial activity against S. aureus compared to standard drug Ampicilin. Final synthesized compounds 58-70 were tested against two Gram positive (S. aureus and B. subtilis) and two Gram negative (E. coli and P. aureginosa) microorganisms, their activity against C. albicans was also checked and they did not exhibit any antimicrobial activity.

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Synthesis, Characterization, and Antibacterial Activities of Novel Sulfonamides Derived through Condensation of Amino Group Containing Drugs, Amino Acids, and Their Analogs

BioMed Research International ◽

10.1155/2015/938486 ◽

2015 ◽

Vol 2015 ◽

pp. 1-7 ◽

Cited By ~ 2

Author(s):

Muhammad Abdul Qadir ◽

Mahmood Ahmed ◽

Muhammad Iqbal

Keyword(s):

Amino Acids ◽

Spectral Analysis ◽

New Products ◽

Antibacterial Activities ◽

Amino Group ◽

Bacterial Strains ◽

Zone Of Inhibition ◽

E Coli ◽

Ft Ir

Novel sulfonamides were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial activities against medically important gram (+) and gram (−) bacterial strains, namely,S. aureus,B. subtilis,E. coli, andK. pneumoniae. The antibacterial activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds 5a and 9a have most potent activity againstE. coliwith zone of inhibition:31±0.12 mm (MIC: 7.81 μg/mL) and30±0.12 mm (MIC: 7.81 μg/mL), respectively, nearly as active as ciprofloxacin (zone of inhibition:32±0.12 mm). In contrast, all the compounds were totally inactive against the gram (+)B. subtilis.

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