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Article ; Online: Antimicrobial activities of spirooxindolopyrrolidine tethered dicarbonitrile heterocycles against multidrug resistant nosocomial pathogens

Natarajan Arumugam / Abdulrahman I. Almansour / Raju Suresh Kumar

Journal of Infection and Public Health, Vol 14, Iss 12, Pp 1810-

2021 Volume 1814

Abstract: Background: Microbial infections together with rising drug resistance pose a threat to immunocompromised individual. In this perspective, compounds with spirooxindolopyrrolidine play a significant role in research on antimicrobial drug delivery research ... ...

Abstract	Background: Microbial infections together with rising drug resistance pose a threat to immunocompromised individual. In this perspective, compounds with spirooxindolopyrrolidine play a significant role in research on antimicrobial drug delivery research owing to their various pharmaceutical activities. Spiroheterocyclic compounds are present in number of medications as active motif due to their exceptional structural properties which enable for easy interaction with the protein of the biological target. Inspired by this biological precedent encouraged to synthesize a new class of dispirooxindole fused pyrrolidine heterocycles via a three-component cycloaddition strategy. Materials and Methods: The new class of structurally intriguing spirooxindolopyrrolidines were synthesized through three component cycloaddition process and the structure of products were assigned through spectroscopic analysis. The newly synthesized compounds were assessed for their antimicrobial sensitivity test with standard Kirby Bauer method with common drugs. Results: The structurally unexplored hybrid heterocycles fused spirooxindolopyrrolidine exhibited excellent antimicrobial activity against the common nosocomial microbial pathogens. Of four compounds, the compound bearing a chlorine atom on the aryl ring (4a) exhibited significant antimicrobial activity (zone of inhibition: 9.00 ± 1.00–17.00 ± 0.35 mm and MIC: 16.00–256.00 μg/mL) against selected nosocomial infection causing microbial pathogens. Hence, the compound 4a has been considered as an effective drug of interest in therapeutic field for compacting infectious diseases causing pathogens. Conclusion: With an aim of developing more effective and economically more affordable antimicrobial leads with a unique mechanism of action, we have designed and synthesized structurally diverse spirooxindolopyrrolidine tethered hybrids that has been assayed against multidrug resistant nosocomial pathogens. The regioisomer having chloro substituted on the phenyl ring showed potent activity when ...
Keywords	Spiropyrrolidine ; 1,3-Dipolar cycloaddition methodology ; Antimicrobial activity ; Multidrug resistant ; Nosocomial pathogens ; Infectious and parasitic diseases ; RC109-216 ; Public aspects of medicine ; RA1-1270
Subject code	540
Language	English
Publishing date	2021-12-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Molecular structure, stability and spectroscopic properties of verteporfin and its derivatives – A theoretical insight

Raju Suresh Kumar / Abdulrahman I. Almansour / Natarajan Arumugam / Khloud Ibrahim Al-Shemaimari / Sakkarapalayam M. Mahalingam / Sakkarapalayam Murugesan Senthil Kumar

Journal of King Saud University: Science, Vol 36, Iss 1, Pp 103031- (2024)

1481

Abstract: The electronic and geometrical structure of the well-known photosensitizer verteporfin VD (1), as well as its guanidine and dicarboxylic acid derivatives VD(Gua)1 (2), VD(COOH)2 (3), and VD(Gua)3 (4) are analyzed using density functional theory (DFT) ... ...

Abstract	The electronic and geometrical structure of the well-known photosensitizer verteporfin VD (1), as well as its guanidine and dicarboxylic acid derivatives VD(Gua)1 (2), VD(COOH)2 (3), and VD(Gua)3 (4) are analyzed using density functional theory (DFT) calculations. The investigation of compound’s thermal and kinetic stability supports their potential use as photodynamic therapeutics. Though there are reports about the biological applications of verteporfin and its derivatives, the basic structural futures at molecular level which play a crucial role in their potential applications, are not well-explored. The results of electronic and spectral analyses by DFT calculation in this work reveal important points underlying the applications of these compounds.
Keywords	DFT ; NMR ; PDT ; Verteporfin ; Guanidine derivative ; Science (General) ; Q1-390
Language	English
Publishing date	2024-01-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: In vitro mechanistic investigation of polycyclic cage-like heterocyclic hybrid possessing diverse pharmacophoric units

Raju Suresh Kumar / Abdulrahman I. Almansour / Natarajan Arumugam

Journal of King Saud University: Science, Vol 32, Iss 4, Pp 2406-

2020 Volume 2413

Abstract: A novel polycyclic cage-like heterocyclic hybrid comprising several privileged structures such as pyrroloisoquinoline, 4-pyridinone and a α,β -unsaturated ketone moiety has been synthesized in good yield employing a microwave mediated [3 + 2]- ... ...

Abstract	A novel polycyclic cage-like heterocyclic hybrid comprising several privileged structures such as pyrroloisoquinoline, 4-pyridinone and a α,β -unsaturated ketone moiety has been synthesized in good yield employing a microwave mediated [3 + 2]-cycloaddition/annulation strategy in 1-butyl-3-methylimidazolium bromide ([bmim]Br). The compound thus synthesized was analyzed for in vitro anticancer activity employing MCF-7, Jurkat, HCT 116 and NCI-H460 cell lines. The effect of polycyclic cage-like heterocyclic hybrid on cells viability was analyzed by MTT assay and its DNA damage efficiency was confirmed by several examinations like apoptosis study, cell cycle analysis, caspase-3 expression analysis and TUNEL assay. Mitochondrial membrane potential was determined by JC-1 staining. The polycyclic cage-like heterocyclic hybrid bearing diverse functionalities played a major role in DNA damage of cancerous cells and in consequence inhibited the DNA cells proliferation.
Keywords	Anticancer activity ; Broad spectrum activity ; [3 + 2] Cycloaddition ; Annulation ; Polycyclic cage-like heterocyclic hybrid ; Science (General) ; Q1-390
Language	English
Publishing date	2020-06-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: An efficient, sustainable approach to the chemo and regioselective synthesis of novel spiroindenoquinoxaline grafted piperidone hybrid heterocycles

Abdulrahman I. Almansour / Natarajan Arumugam / Raju Suresh Kumar

Journal of King Saud University: Science, Vol 32, Iss 7, Pp 3059-

2020 Volume 3064

Abstract: An efficient, eco-friendly and sustainable approach for the synthesis of novel spiroindeno[1,2-b]quinoxaline-3-phenylspiro[4,3″]benzylidenepiperidone ring system has been developed by a one-pot four component [3 + 2] cycloaddition strategy. The 1,3- ... ...

Abstract	An efficient, eco-friendly and sustainable approach for the synthesis of novel spiroindeno[1,2-b]quinoxaline-3-phenylspiro[4,3″]benzylidenepiperidone ring system has been developed by a one-pot four component [3 + 2] cycloaddition strategy. The 1,3-dipole generated in situ from quinoxalinone and l-phenylalanine reacts with the highly functionalized dipolarophiles, bisarylidene piperidones affording spirohybrid heterocycles in good yields. The unexplored novel class of dispirohybrid heterocycles obtained possess three CN and two CC bonds with four adjacent stereogenic carbons, out of which two is spirocarbons. The structure of compounds was elucidated using 1H, 13C and mass spectroscopic studies.
Keywords	Azomethine ylide ; Spiroindenoquinoxalinone ; Spiropyrrolidines ; Benzylidene piperidone ; Ionic liquids ; Science (General) ; Q1-390
Language	English
Publishing date	2020-10-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: A simple, rapid, expedient and sustainable green strategy for the synthesis of benz-/naphthimidazoles

Abdulrahman I. Almansour / Raju Suresh Kumar / Natarajan Arumugam

Journal of King Saud University: Science, Vol 32, Iss 7, Pp 3153-

2020 Volume 3158

Abstract: A versatile green chemical procedure for the highly selective construction of 2-aryl substituted benz-/naphthimidazoles starting from the reaction of aromatic 1,2-diamines with a series of substituted arylthioprolines with three to five drops of water ... ...

Abstract	A versatile green chemical procedure for the highly selective construction of 2-aryl substituted benz-/naphthimidazoles starting from the reaction of aromatic 1,2-diamines with a series of substituted arylthioprolines with three to five drops of water under simple grinding at ambient temperature in good yields is described. The short reaction time, simplified experimental procedure, the absence of extraction and chromatographic purification steps in addition to the environment affability makes this green strategy highly attractive in view of green chemistry. The expected reaction to furnish the thiazole grafted benz-/naphthimidazole did not occur. Perhaps the arylthioprolines could be in zwitterionic form, which could react with 1,2-diamine giving dihyrobenzimidazole, which undergoes air oxidation to furnish the 2-aryl benzimidazole rather than the expected thiazole grafted imidazoles.
Keywords	Green chemistry ; Arylthioprolines ; Benzimidazole ; Naphthimidazole ; Selectivity ; Science (General) ; Q1-390
Subject code	660
Language	English
Publishing date	2020-10-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Bioprospection and secondary metabolites profiling of marine Streptomyces levis strain KS46

Bidhayak Chakraborty / Raju Suresh Kumar / Abdulrahman I. Almansour / Pethaiah Gunasekaran / Sreenivasa Nayaka

Saudi Journal of Biological Sciences, Vol 29, Iss 2, Pp 667-

2022 Volume 679

Abstract: The quest for novel broad spectrum bioactive compounds is needed continuously because of the rapid advent of pathogenic multi drug resistant organisms. Actinomycetes, isolated from unexplored habitats can be a solution of this problem. The motive of this ...

Abstract	The quest for novel broad spectrum bioactive compounds is needed continuously because of the rapid advent of pathogenic multi drug resistant organisms. Actinomycetes, isolated from unexplored habitats can be a solution of this problem. The motive of this research work was isolation of actinomycetes having potential antimicrobial activities from unexplored regions of Devbag and Tilmati beach. The isolated actinomycetes were screened against pathogenic microbes for antimicrobial activities through cross streak method. Enzyme production activity was checked for these actinomycetes for amylase, protease, cellulase and lipase enzymes. Further antimicrobial activity of ethyl acetate extract of the potent strain KS46 was performed. The strain KS46 was identified with 16S rRNA gene sequencing and secondary structure was analysed. Gas chromatography–Mass spectrometry (GC–MS) profiling was conducted to ascertain the presence of bioactive metabolites in the ethyl acetate extract. The collected samples were pre-treated and 70 actinomycetes were isolated. The Streptomyces sp. strain KS46 showed the best antimicrobial activity in primary screening. Ethyl acetate extract of the strain KS46 revealed antimicrobial activity against S. aureus, B. subtilis, B. cereus, E. faecalis, K. pneumoniae, E. coli, S. flexneri, C. albicans and C. glabrata. The 16S rRNA gene sequencing identified the strain KS46 as Streptomyces levis strain KS46. The GC–MS metabolite profiling of the ethyl acetate extract revealed the availability of 42 compounds including fatty acid esters, fatty acid anhydrides, alkanes, steroids, esters, alcohols, carboxylic ester, etc. having antibacterial, antifungal, antiproliferative, antioxidant activities. This study indicated that Devbag and Tilmati beaches being untapped habitats have enormous diversity of promising antimicrobial metabolite producing actinomycetes. Therefore, further exploration should be carried out to characterize the potential actinomycetes, which can be optimistic candidates for generation of novel antimicrobial drugs.
Keywords	Actinomycetes ; Streptomyces levis ; Antimicrobial ; Enzymes ; 16S rRNA gene sequencing ; GC–MS ; Biology (General) ; QH301-705.5
Subject code	500
Language	English
Publishing date	2022-02-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: In-vitro investigation on the biological activities of squalene derived from the soil fungus Talaromyces pinophilus

Meghashyama Prabhakara Bhat / Muthuraj Rudrappa / Anil Hugar / Pooja Vidyasagar Gunagambhire / Raju Suresh Kumar / Sreenivasa Nayaka / Abdulrahman I. Almansour / Karthikeyan Perumal

Heliyon, Vol 9, Iss 11, Pp e21461- (2023)

2023

Abstract: The consistent increase in multidrug resistance among pathogens and increased cancer incidence are serious public health concerns and threaten humans by killing countless lives. In the present study, Talaromyces pinophilus CJ15 was characterized and ... ...

Abstract	The consistent increase in multidrug resistance among pathogens and increased cancer incidence are serious public health concerns and threaten humans by killing countless lives. In the present study, Talaromyces pinophilus CJ15 was characterized and evaluated for its antibacterial, candidicidal and cytotoxic activities. The selected isolate Talaromyces pinophilus CJ15 with 18S rRNA gene sequence of 1021 base pairs exhibited antifungal activity on plant pathogens via dual culture. The GC-MS profiling of crude extract illustrated the existence of many bioactive macromolecules which include squalene belonging to the terpenoids family. The biological macromolecules in the bioactive fraction of CJ15 exhibited increasing antibacterial activity with an increase in concentration such that the highest activity was recorded against Shigella flexneri with 15, 18, 20, and 24 mm inhibition zones at 25, 50, 75 and 100 μl concentrations, respectively. The squalene, having a molecular weight of 410.718 g/mol, displayed candidicidal activity with a right-side shifted log phase in the growth curve of all the treated Candida species, indicating delayed exponential growth. In cytotoxic activity, the extracted squalene exhibited an IC50 concentration of 26.22 μg/ml against JURKAT cells and induced apoptosis-induced cell death. This study's outcomes encourage the researchers to explore further the development of new and improved bioactive macromolecules that could help to prevent infections and human blood cancer.
Keywords	Talaromyces pinophilus ; Antibacterial activity ; Squalene ; Candidicidal activity ; Anticancer activity ; Human blood cancer ; Science (General) ; Q1-390 ; Social sciences (General) ; H1-99
Subject code	572
Language	English
Publishing date	2023-11-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Highly functionalized dispiropyrrolidine embedded indandione hybrids as potent cholinesterase inhibitors

Shatha Ibrahim Alaqeel / Natarajan Arumugam / Abdulrahman I. Almansour / Raju Suresh Kumar / Rashid Ayub / Dhanaraj Premnath / Karthikeyan Perumal

Journal of King Saud University: Science, Vol 35, Iss 5, Pp 102706- (2023)

2023

Abstract: New class of highly functionalized dispiropyrrolidine tethered indandione heterocycles in good yield were obtained through stereo- and regioselective single-pot three component cycloaddition methodology between benzylidene-indandione and non-stabilized ... ...

Abstract	New class of highly functionalized dispiropyrrolidine tethered indandione heterocycles in good yield were obtained through stereo- and regioselective single-pot three component cycloaddition methodology between benzylidene-indandione and non-stabilized azomethine ylide. The ylide generated from active diketone and aminophenylpropanoic acid via dehydration/decarboxylative pathway. The synthesized dispiropyrroldine comprising indandiones were elucidated through 1H and 13C NMR spectroscopic analysis, the stereo and regioselective formation of the dispiropyrrolidine were unequivocally assigned by X-ray diffraction analysis. Compound thus synthesized were assayed as potential inhibitor for the treatment of AD. Spiropyrrolidine 4h that bearing methoxy group on the phenyl ring showed significant activity, IC50 of 3.24 ± 0.25 and 10.25 ± 0.16 μM against acetyl and butyryl cholinesterase enzyme, respectively. The lead compound 4h executed to investigate for their docking simulation that showed strong binding affinity with binding site of the cholinesterase protein.
Keywords	Spiropyrrolidines ; Cycloaddition reaction ; Cholinestrase inhibitory activity ; Docking simulation ; Science (General) ; Q1-390
Subject code	540
Language	English
Publishing date	2023-07-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: A facile ionic liquid-accelerated, four-component cascade reaction protocol for the regioselective synthesis of biologically interesting ferrocene engrafted spiropyrrolidine hybrid heterocycles

Natarajan Arumugam / Abdulrahman I. Almansour / Raju Suresh Kumar / Necmi Dege

Journal of King Saud University: Science, Vol 32, Iss 4, Pp 2500-

2020 Volume 2504

Abstract: Spiropyrrolidine engrafted ferrocene heterocycles were synthesized in excellent yields in a sustainable fashion employing an ionic liquid, 1-butyl-3-methylimidazoliumbromide accelerated one-pot multicomponent cycloaddition strategy. The in situ 1,3- ... ...

Abstract	Spiropyrrolidine engrafted ferrocene heterocycles were synthesized in excellent yields in a sustainable fashion employing an ionic liquid, 1-butyl-3-methylimidazoliumbromide accelerated one-pot multicomponent cycloaddition strategy. The in situ 1,3-dipole component derived from indenoquinoxalinone and L-phenylalanine that reacts with various substituted ferrocenyl chalcone in [bmim]Br affording spirocycloadduct.
Keywords	Multicomponent cycloaddition strategy ; Ferrocene grafted spiroheterocyles ; Indenoquinoxaline ; Ionic liquids ; Science (General) ; Q1-390
Language	English
Publishing date	2020-06-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Diastereoselective synthesis and anticancer potential of a small library of cage-like heterocyclic hybrids

Raju Suresh Kumar / Abdulrahman I. Almansour / Natarajan Arumugam / Kotresha D / Janardhana Papayya Balakrishna

Journal of King Saud University: Science, Vol 33, Iss 1, Pp 101238- (2021)

2021

Abstract: With an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a three-component [3 + 2]-cycloaddition/ ... ...

Abstract	With an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a three-component [3 + 2]-cycloaddition/annulation strategy. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with noteworthy anticancer activity. Compound 4b inhibited MCF-7 and NCI-H460 cell lines with IC50 values 10.86 ± 0.94 and 9.17 ± 0.63 µM respectively. Further, apoptosis and cell cycle analysis revealed that this compound was able to prompt apoptosis at an early stage in MCF-7 cell line besides increasing the threshold of MMP and % of cells expressing FITC-dUTP. These results suggest that compound 4b is a potential molecule for the further exploration.
Keywords	Cage-like heterocyclic hybrids ; Stereoselective synthesis ; MCF-7 ; Flow cytometry ; Apoptosis ; JC1 ; Science (General) ; Q1-390
Language	English
Publishing date	2021-01-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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