A minireview of 1,2,3‐triazole hybrids with O‐heterocycles as leads in medicinal chemistry DOI

Bhavna Saroha,

Gourav Kumar, Ramesh Kumar

et al.

Chemical Biology & Drug Design, Journal Year: 2021, Volume and Issue: 100(6), P. 843 - 869

Published: Sept. 30, 2021

Abstract Over the past few decades, dynamic progress in synthesis and screening of heterocyclic compounds against various targets has made a significant contribution field medicinal chemistry. Among wide array compounds, triazole moiety attracted attention researchers owing to its vast therapeutic potential easy preparation via copper ruthenium‐catalyzed azide‐alkyne cycloaddition reactions. Triazole skeletons are found as major structural components different class drugs possessing diverse pharmacological profiles including anti‐cancer, anti‐bacterial, anti‐fungal, anti‐viral, anti‐oxidant, anti‐inflammatory, anti‐diabetic, anti‐tubercular, anti‐depressant among others. Furthermore, years, significantly large number hybrids were synthesized with moieties order gain added advantage improved profile, overcoming multiple drug resistance reduced toxicity from molecular hybridization. these hybrids, many available commercially used for treating infections/disorders like tazobactam cefatrizine potent anti‐bacterial agents while isavuconazole ravuconazole anti‐fungal activities name few. In this review, we will summarize biological 1,2,3‐triazole copious oxygen‐containing heterocycles lead This review be very helpful working modeling, design development,

Language: Английский

Ethosomes as Nanocarriers for the Development of Skin Delivery Formulations DOI
Ana Cláudia Paiva‐Santos, Ana Luísa Silva, Catarina Guerra

et al.

Pharmaceutical Research, Journal Year: 2021, Volume and Issue: 38(6), P. 947 - 970

Published: May 25, 2021

Language: Английский

Citations

141
A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives DOI Creative Commons
Shejuti Rahman Brishty, Md. Jamal Hossain, Mayeen Uddin Khandaker

et al.

Frontiers in Pharmacology, Journal Year: 2021, Volume and Issue: 12

Published: Nov. 3, 2021

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore naturally occurring active biomolecules, derivatives significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers synthesized plenty the last decades, amidst large share compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we summarized reported recent literature (2012–2021) available structure-activity relationship. Compounds bearing nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects world’s most virulent diseases. Several promising therapeutic candidates undergoing human trials, some going be approved for use. However, notable challenges, such drug resistance, costly tedious synthetic methods, little structural information receptors, lack advanced software, so on, still viable overcome further research.

Language: Английский

Citations

119
Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives DOI Creative Commons
Diana Becerra, Rodrigo Abonı́a, Juan‐Carlos Castillo

et al.

Molecules, Journal Year: 2022, Volume and Issue: 27(15), P. 4723 - 4723

Published: July 23, 2022

Pyrazole and its derivatives are considered a privileged

Language: Английский

Citations

75
Insights into the structure activity relationship of nitrogen-containing heterocyclics for the development of antidepressant compounds: An updated review DOI
Karanvir Singh, Rohit Pal, Shah Alam Khan

et al.

Journal of Molecular Structure, Journal Year: 2021, Volume and Issue: 1237, P. 130369 - 130369

Published: March 27, 2021

Language: Английский

Citations

84
Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview DOI Creative Commons
Ravichandran Veerasamy, Anitha Roy, Rohini Karunakaran

et al.

Pharmaceuticals, Journal Year: 2021, Volume and Issue: 14(7), P. 663 - 663

Published: July 11, 2021

A significant number of the anti-inflammatory drugs currently in use are becoming obsolete. These exceptionally hazardous for long-term because their possible unfavourable impacts. Subsequently, ebb-and-flow decade, analysts and researchers engaged developing new drugs, many such agents later phases clinical trials. Molecules with heterocyclic nuclei similar to various natural antecedents, thus acquiring immense consideration from scientific experts researchers. The arguably most adaptable cores benzimidazoles containing nitrogen a bicyclic scaffold. Numerous benzimidazole broadly used treatment numerous diseases, showing promising therapeutic potential. Benzimidazole derivatives exert effects mainly by interacting transient receptor potential vanilloid-1, cannabinoid receptors, bradykinin specific cytokines, 5-lipoxygenase activating protein cyclooxygenase. Literature on structure–activity relationship (SAR) investigations highlight that substituent’s tendency position ring significantly contribute activity. Reported SAR analyses indicate substitution at N1, C2, C5 C6 positions scaffold greatly influence For example, substituted anacardic acid C2 inhibits COX-2, 5-carboxamide or sulfamoyl sulfonyl antagonises receptor, whereas diarylamine C3 carboxamide result antagonism receptor. In this review, we examine insights regarding SARs compounds, which will be helpful designing target inflammation-promoting enzymes.

Language: Английский

Citations

80
Thiophene-Based Compounds with Potential Anti-Inflammatory Activity DOI Creative Commons
Ryldene Marques Duarte da Cruz, Francisco Jaime Bezerra Mendonça,

Natália Barbosa de Mélo

et al.

Pharmaceuticals, Journal Year: 2021, Volume and Issue: 14(7), P. 692 - 692

Published: July 19, 2021

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) the most prescribed clinical treatments, despite their severe side effects exclusive action in improving symptoms, without effectively promoting cure. However, recent advances fields of pharmacology, medicinal chemistry, chemoinformatics have provided valuable information opportunities for development new drug candidates. For design discovery, thiophene derivatives privileged structures. Thiophene-based compounds, like commercial Tinoridine Tiaprofenic acid, known properties. The present review provides an update on role thiophene-based inflammation. Studies mechanisms action, interactions with receptors (especially against cyclooxygenase (COX) lipoxygenase (LOX)), structure-activity relationships also presented discussed. results demonstrate importance compounds as structures discovery novel agents. studies reveal important structural characteristics. presence carboxylic acids, esters, amines, amides, well methyl methoxy groups, has been frequently described, highlights these groups activity biological target recognition, especially inhibition COX LOX enzymes.

Language: Английский

Citations

77
Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities DOI Creative Commons
Maria Marinescu

Antibiotics, Journal Year: 2021, Volume and Issue: 10(8), P. 1002 - 1002

Published: Aug. 19, 2021

The synthesis of new compounds with antimicrobial and antiviral properties is a central objective today in the context COVID-19 pandemic. Benzimidazole pyrazole have remarkable biological properties, such as antimicrobial, antiviral, antitumor, analgesic, anti-inflammatory, anti-Alzheimer’s, antiulcer, antidiabetic. Moreover, recent literature mentions syntheses some benzimidazole–pyrazole hybrids, well other thereof. In this review, we aim to review methods these activities compounds, their correlation various groups present on molecule, pharmaceutical properties.

Language: Английский

Citations

77
Design, synthesis and molecular docking of new pyrazole-thiazolidinones as potent anti-inflammatory and analgesic agents with TNF-α inhibitory activity DOI
Somaia S. Abd El‐Karim, Hanaa S. Mohamed, Mohamed F. Abdelhameed

et al.

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 111, P. 104827 - 104827

Published: March 18, 2021

Language: Английский

Citations

74
A facile approach synthesis of benzoylaryl benzimidazole as potential α-amylase and α-glucosidase inhibitor with antioxidant activity DOI
Lotfi M. Aroua, Hind R. Almuhaylan, Fahad M. Alminderej

et al.

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 114, P. 105073 - 105073

Published: June 12, 2021

Language: Английский

Citations

72
Foliar Applications of Bacillus subtilis HA1 Culture Filtrate Enhance Tomato Growth and Induce Systemic Resistance against Tobacco mosaic virus Infection DOI Creative Commons
Hamada El‐Gendi, Abdulaziz A. Al–Askar, Lóránt Király

et al.

Horticulturae, Journal Year: 2022, Volume and Issue: 8(4), P. 301 - 301

Published: March 31, 2022

The application of microbial products as natural biocontrol agents for inducing systemic resistance against plant viral infections represents a promising strategy sustainable and eco-friendly agricultural applications. Under greenhouse conditions, the efficacy culture filtrate Bacillus subtilis strain HA1 (Acc# OM286889) protecting tomato plants from Tobacco mosaic virus (TMV) infection was assessed. results showed that dual foliar this (HA1-CF) 24 h before after TMV inoculation most effective treatment enhancing development, with substantial improvements in shoot root parameters. Furthermore, compared to non-treated plants, HA1-CF-treated had significant increase total phenolic flavonoid contents up 27% 50%, respectively. In addition, considerable activities reactive oxygen species scavenging enzymes (PPO, SOD, POX) decrease non-enzymatic oxidative stress markers (H2O2 MDA) were reported. comparison untreated control all reduction accumulation systemically infected leaves, 91% at 15 dpi. qRT-PCR confirmed HA1-CF stimulated transcription several defense-related genes (PR-1, PAL, CHS, HQT), pointing their potential role induced TMV. GC–MS analysis phenol, 2,4-bis (1,1-dimethylethyl)-, Pyrrolo [1,2-a] pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl)- eicosane are primary ingredient compounds ethyl acetate extract, suggesting these molecules take part stimulating plants. Our imply is inducer infections, growth promoter, source bioactive disease management.

Language: Английский

Citations

51