Synthesis and Antitumor Evaluation of Novel 5-Bromo Indole-Aryl Keto Hydrazide-Hydrazone Analogues

Rudavath, Durgesh; Sreenivasulu, Reddymasu; Pinapati, Srinivasa Rao; Raju, Rudraraju Ramesh

doi:10.14233/ajchem.2018.21114

Cited by 36 publications

(4 citation statements)

References 28 publications

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“…The made ready wells were made full with equal amount of an answer toto put together substances made of a number of things and quality example Drugs separately []. After a stretch of time of pre-incubation diffusion, the plates were incubated face up for a certain and clear time about (48-72 hr) under special conditions (32-360C) [49]. The bands, parts of putting off were worked out as parameters 5 of antimicrobial 6 properties of put together comings from [].…”

Section: Preparation Of Inoculumsmentioning

confidence: 99%

Design and synthesis of anti-convulsant and anti-bacterial activity of new hydrazone derivatives

2020

Biointerface Res Appl Chem

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Synthesis of new hydrazone derivatives, starting from 2-(3, 4-Dichloro-benzoyl)-benzoic acid to 2-(3, 4-dichloro-benzoyl) - benzoic acid ethyl ester than converted into 2- (3, 4-Dichloro-benzoyl)-benzoic acid hydrazide with a substituted aldehyde. The structure of newly synthesized compounds was confirmed by analytical and spectral analysis IR, 1HNMR and MASS. For docking study, we took structures of ligand compounds (i.e. AK-series Compounds) and target protein structures into ‘pdb’ file format. Three compounds as possible anti-convulsant AK-1, AK-2 &Ak-4 were considered for compounds Ak-1 was not found suitable for anti-convulsant activity; while AK-2 & AK-4 have the capacity to show anti-convulsant activity with lesser affinity than controls. As an overall conclusion, except Ak-1, other compounds can be further used for anti- convulsant activity. Anti-convulsant activities were performed on rats by using maximal Electroshock Seizure test and minimal Neurotoxicity. Compound 2- (3, 4 – Dichloro-benzoyl)-benzoic acid (4- chloro-benzylidene) (AK-2) shows good anti-convulsant activity. The in-vitro antibacterial strains Escherichia coli MTCC 1573), and staphylococcus aureus (MTCC 1430), were used. Compound 2-(3, 4-Dichloro-benzoyl)-benzoic acid (2-notro-benzylidene-hydrazide (AK-1) gives the highest activity against Escherichia coli (MTCC 1573) and Staphylococcus aureus (MTCC-1430).

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Section: Preparation Of Inoculumsmentioning

confidence: 99%

Design and synthesis of anti-convulsant and anti-bacterial activity of new hydrazone derivatives

2020

Biointerface Res Appl Chem

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“…[29][30][31] Presently we are targeting the Indazole nucleus which offers wide substitution pattern on the ring and can be further explored for the development of the newer efficient and safe molecules. Indazoles are found to have a wide range of biological activities such as analgesic and anti-inflammatory, [32] antibacterial, [33] antifungal, [34] anticancer, [35,36] antiviral, [37] antimycobacterial, [38] antiplatelet, [39] and 5-HT6 antagonists etc.., [40] In this context, our study focuses on the approach of rational drug design in the search of novel ligands against S. aureus complexed with nicotinamide adenine dinucleotide phosphate (NADPH) and trimethoprim (TMP) and has been targeted for the development of some useful molecules. Antibacterial activity and antifungal activity dual action were evaluated by docking scores were selected, and the stability of their interactions (Π-Π, Π-alkyl, Π-sigma, van der Waals, Hbonds, CÀ H bonds etc..,) with the target protein (3FRE) was determined by an MD simulation study and to calculate the binding free energies (ΔG) as well as dissociation constant (K i ) of selected complexes.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and in Silico Studies of Some New 1,2,3‐Triazolyltetrazole Bearing Indazole Derivatives as Potent Antimicrobial Agents

Gujja,

Sadineni,

Epuru

et al. 2023

Chemistry & Biodiversity

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Abstract1,2,3‐Triazole and tetrazole derivatives bearing pyrrolidines are found to exhibit notable biological activity and have become useful scaffolds in medicinal chemistry for application in lead discovery and optimization. Novel indazole bearing 1,2,3‐triazolyltetrazoles were designed as potential antimicrobial candidates. The structure of duel heterocyclics was validated by a spectroscopic technique of infrared (IR), nuclear magnetic resonance (1H and 13C NMR), and mass spectral data. Compounds 4b, 4c, 4d, and 4h were found to have a stronger antibacterial effect against Gram‐positive (S. aureus, B. subtilis, M. Luteus) and Gram‐negative (E. coli, P. aeruginosa) microorganisms with MICs ranging from 5±0.03–18±0.02 μM, respectively. Moreover, scaffolds 4a, 4h showed potent antifungal activity against A. flavus, M. gypsuem strains with MIC values of 10±0.02, 11±0.01 μM, which are similar activity that of the standard Itraconazole (MIC=8±0.02, 10±0.01 μM). The binding mode for compound 4 inside the catalytic pocket of S. aureus complexed with nicotinamide adenine dinucleotide phosphate and trimethoprim and produced a network of hydrophobic and hydrophilic interactions (3FRE). From in silico results, 4b demonstrated highly stable hydrogen binding amino acids Leu62(X) [N18…O, 2.47 Å], Arg44(X) [N17…N, 3.11 Å], Thr96(X) [N10…OG1, 3.05 Å], Gly94(X) [F7…N, 2.82 Å], and Gly43(X) [F7…N, 2.90 Å], which are plays a crucial role in ensuring efficient binding of the ligand in a crystal structure of antibacterial receptor. Furthermore, the physicochemical and ADME filtration molecular properties, estimation of toxicity, and bioactivity scores of these novel scaffolds were evaluated by using SwissADME and ADMETlab2.0 online protocols. Thus, the significant antimicrobial activity of indazole linked to duel heterocyclic compounds can be used for development of new antimicrobial agents with further modifications.

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“…Notably, the known synthetic procedures toward indazoles may suffer from multistep routes, severe conditions, and relatively low substrate diversity [ 32 , 33 , 34 ]. Therefore, considerable attempts have been devoted to constructing these biologically critical scaffolds more efficiently, although the exploration of novel atom-economical strategies to produce these unique scaffolds is still a challenging topic.…”

Section: Introductionmentioning

confidence: 99%

Recent Strategies in Transition-Metal-Catalyzed Sequential C–H Activation/Annulation for One-Step Construction of Functionalized Indazole Derivatives

et al. 2022

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Designing new synthetic strategies for indazoles is a prominent topic in contemporary research. The transition-metal-catalyzed C–H activation/annulation sequence has arisen as a favorable tool to construct functionalized indazole derivatives with improved tolerance in medicinal applications, functional flexibility, and structural complexity. In the current review article, we aim to outline and summarize the most common synthetic protocols to use in the synthesis of target indazoles via a transition-metal-catalyzed C–H activation/annulation sequence for the one-step synthesis of functionalized indazole derivatives. We categorized the text according to the metal salts used in the reactions. Some metal salts were used as catalysts, and others may have been used as oxidants and/or for the activation of precatalysts. The roles of some metal salts in the corresponding reaction mechanisms have not been identified. It can be expected that the current synopsis will provide accessible practical guidance to colleagues interested in the subject.

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Synthesis and Antitumor Evaluation of Novel 5-Bromo Indole-Aryl Keto Hydrazide-Hydrazone Analogues

Cited by 36 publications

References 28 publications

Design and synthesis of anti-convulsant and anti-bacterial activity of new hydrazone derivatives

Design and synthesis of anti-convulsant and anti-bacterial activity of new hydrazone derivatives

Synthesis and in Silico Studies of Some New 1,2,3‐Triazolyltetrazole Bearing Indazole Derivatives as Potent Antimicrobial Agents

Recent Strategies in Transition-Metal-Catalyzed Sequential C–H Activation/Annulation for One-Step Construction of Functionalized Indazole Derivatives

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