SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEW BENZIMIDAZOLE DERIVATIVES AS ANTIMICROBIAL AGENTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 25-29
Author(s):  
S. G Jadhav ◽  
◽  
S. R. Pattan
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Antimicrobial Agents ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Benzimidazole Derivatives ◽  
Structure Activity ◽  
Relationship Of

A new series of substituted benzimidazole derivatives were synthesized and the structures of these compounds were established on the basis of spectral data. The title compounds were evaluated for antimicrobial activity. Some of these compounds have shown excellent antimicrobial activity.

Variability of the antibacterial potential among analogue diterpenes against Gram-positive bacteria: considerations on the structure–activity relationship

2019 ◽  
Vol 97 (7) ◽  
pp. 568-575 ◽  
Author(s):  
Ana Carolina Ferreira Soares ◽  
Priscilla Mendonça Matos ◽  
Herbert Júnior Dias ◽  
Gabriela de Paula Aguiar ◽  
Eliene Silvério dos Santos ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Public Health Problem ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Gram Positive ◽  
Structure Activity ◽  
Esterification Reactions ◽  
Relationship Of ◽  
Synthetic Derivatives

The search for new antibacterial agents and a better comprehension of substances with antimicrobial behavior is mandatory nowadays due to the serious public health problem of infection diseases. In the present work, 30 diterpenes were studied, with 2 natural derivatives, named ent-16-kauren-19-oic acid and ent-pimara-8(14),15-dien-19-oic acid, and 28 semi-synthetic derivatives. The natural diterpenes were isolated from Mikania glomerata and Viguiera arenaria, respectively. All diterpenes were submitted to antimicrobial assays against six different Gram-positive microorganisms to better understand the structure–activity relationship of antimicrobial diterpenes. The semi-synthetic derivatives were all obtained from the two natural derivatives by structural modifications, mainly esterification reactions. Both natural derivatives, together with the derivative ent-8(14)-pimaren-19-oic acid, displayed the most relevant antibacterial activities, with minimal inhibitory concentration (MIC) values that were less than 10 μg mL–1 for most pathogens; thus, they were considered promising antimicrobial agents. Moreover, in light of the hypothesis of Urzúa and colleagues, several considerations about the structure–activity relationship of antimicrobial diterpenes could be stated.

Quantitative Structure Activity Relationship studies of Antimicrobial Compounds:A Review

2021 ◽  
Vol 19 ◽  
Author(s):  
Sahaya Asirvatham ◽  
Jyoti Thakur ◽  
Savita Tauro ◽  
Bharat Dhokchawle
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Quantitative Structure Activity Relationship ◽  
Structure Activity Relationship ◽  
Structural Features ◽  
Activity Relationship ◽  
Antimicrobial Compounds ◽  
Quantitative Structure ◽  
Qsar Studies ◽  
Structure Activity

: With the current scenario of emerging drug-resistant microbial strains, there prevails a continuous threat to health and the development of new antimicrobial agents is a challenging task. Quantitative Structure Activity Relationship (QSAR) has proven to elevate the likelihood of finding a new pharmacophore. Intermolecular binding like hydrophobic bond, electrostatic and steric interactions helps to understand drug interaction with the receptors. Some common conclusions have been drawn after analyzing diverse case studies. Few descriptors were identified to be common in enhancing the antimicrobial activity. The structural features modifying the antimicrobial activity were analyzed using critically published results from significant QSAR studies on antimicrobial compounds. This commentary will assist the synthetic chemist to synthesize novel derivatives which could be potential antimicrobial compounds.

scholarly journals Modification and Targeted Design of N-Terminal Truncates Derived from Brevinin with Improved Therapeutic Efficacy

Biology ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 209
Author(s):  
Haoyang He ◽  
Yuqing Chen ◽  
Zhuming Ye ◽  
Xiaoling Chen ◽  
Chengbang Ma ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Immune Regulation ◽  
Structure Activity Relationship ◽  
Innate Immune ◽  
Activity Relationship ◽  
Potential Toxicity ◽  
Structure Activity ◽  
Starting Point ◽  
Haemolytic Assay ◽  
Relationship Of

Antimicrobial peptides (AMPs) are a class of molecules that play an essential role in innate immune regulation. The Brevinin-1 family are AMPs that show strong pharmacological and antimicrobial potential. A novel peptide, B1A, was designed based on the primary structure of brevinin-1PLb and brevinin-1PLc. Subsequently, a synthesised replicate was subjected to a series of bioassays and was found to display antimicrobial activity. However, it also displayed high levels of haemolysis in a horse red blood cell haemolytic assay, suggesting potential toxicity. Therefore, we rationally designed a number of B1A analogues with aim of retaining antimicrobial activity, lowering toxicity, and to explore the structure–activity relationship of its N-terminus. B1A and its analogues still retained the “Rana Box” and the FLP-motif, which is a feature of this subfamily. However, the introduction of Lys and Trp residues into the peptide sequences revealed that antimicrobial activity of these analogues remained unchanged once the hydrophobicity and the charge reached the threshold. Hence, the idea that the hydrophobicity saturation in different situations is related to antimicrobial activity can be understood via the structure–activity relationship. Meanwhile, it could also be the starting point for the generation of peptides with specific antimicrobial activity.

scholarly journals Structure-activity relationship of HP (2–20) analog peptide: Enhanced antimicrobial activity by N-terminal random coil region deletion

Biopolymers ◽  
2007 ◽  
Vol 88 (2) ◽  
pp. 199-207 ◽  
Author(s):  
Yoonkyung Park ◽  
Seong-Cheol Park ◽  
Hae-Kyun Park ◽  
Song Yub Shin ◽  
Yangmee Kim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Structure Activity Relationship ◽  
Random Coil ◽  
Activity Relationship ◽  
Structure Activity ◽  
Analog Peptide ◽  
Relationship Of

scholarly journals Structure-Activity Relationship of Benzophenanthridine Alkaloids from Zanthoxylum rhoifolium Having Antimicrobial Activity

PLoS ONE ◽  
2014 ◽  
Vol 9 (5) ◽  
pp. e97000 ◽  
Author(s):  
Luciana de C. Tavares ◽  
Graciane Zanon ◽  
Andréia D. Weber ◽  
Alexandre T. Neto ◽  
Clarice P. Mostardeiro ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Benzophenanthridine Alkaloids ◽  
Structure Activity ◽  
Relationship Of
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