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Synthesis and antimycobacterial screening of new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives

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Chinese Chemical Letters 2016年第3期27卷 365-369页

作者： Nagabhushana Nayak Jurupula Ramprasad Udayakumar Dalimba perumal Yogeeswari Dharmarajan Sriram Organic Chemistry Laboratory Department of ChemistryNational Institute of Technology Karnataka Medicinal Chemistry and Drug Discovery Research Laboratory Pharmacy GroupBirla Institute of Technology and Science-PilaniHyderabad Campus

This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-（4-（5-aryl-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）-4-amide derivatives（8a–x）. The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv（MTB） revealed that 2-chloro-N-（4-（5-（4-chlorophenyl）-3-（5-methyl-1,3,4-oxadiazol-2-yl）-1H-pyrazol-1-yl）phenyl）benzamide（8n） is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative（8o） is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity（MIC = 3.13 mg/m L）. Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.

关键词： Pyrazole-oxadiazole hybrids Antitubercular activity SC-XRD analysis In vitro cytotoxicity

The Locally Conservative Galerkin (LCG) Method — a Discontinuous Methodology Applied to a Continuous Framework

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Advances in Applied Mathematics and Mechanics 2009年第3期1卷 319-340页

作者： Rhodri L.T.Bevan Raoul vanLoon perumal Nithiarasu Civil and Computational Engineering Centre School of EngineeringSwansea UniversitySwansea SA28PPUK

This paper presents a comprehensive overview of the element-wise locally conservative Galerkin(LCG)*** LCG method was developed to find a method that had the advantages of the discontinuous Galerkin methods,without the large computational and memory *** initial application of the method is discussed,to the simple scalar transient convection-diffusion equation,along with its extension to the Navier-Stokes equations utilising the Characteristic Based Split(CBS)*** element-by-element solution approach removes the standard finite element assembly necessity,with an face flux providing continuity between these elemental *** face flux provides explicit local conservation and can be determined via a simple small post-processing *** LCG method obtains a unique solution from the elemental contributions through the use of simple *** is shown within this paper that the LCG method provides equivalent solutions to the continuous(global)Galerkin method for both steady state and transient *** numerical examples are provided to demonstrate the abilities of the LCG method.

关键词： Explicit local flux conservation element-by-element solution local conservation LCG convection-diffusion CBS artificial compressibility incompressible flow

Antibacterial potential of three seagrasses against human pathogens

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Asian Pacific Journal of Tropical Medicine 2010年第11期3卷 890-893页

作者： Rengasamy Ragupathi Raja Kannan Rajasekaran Arumugam perumal Anantharaman CAS in Marine Biology Faculty of Marine SciencesAnnamalai UniversityParangipettai-608 502TamilnaduIndia

Objective:To evaluate the antibacterial activity of Halophila stipulacea(***), Cymodocea serrulata(***) and Halodule pinifolia(***) against seven human bacterial ***:The antibacterial activities of the extracts on the various test organisms using disc diffusion method and Minimum Inhibitory Concentraction(MIC).Results: Methanol and chloroform extracts of all the three seagrasses were active against all the tested pathogens,whereas the hexane extract of seagrasses was not active against Staphylococcus aureus (***).Antibacterial activity of three seagrass screened,was in the order of *** > ***.> ***:This antibacterial studies can further investigated on seagrasses for purification of bioactive substance and its possible utility in disease control.

关键词： Seagrass Halophila stipulacea Cymodocea serrulata Halodule pinifolia Antibacterial activity MIC

Taurine in semen extender modulates post–thaw semen quality,sperm kinematics and oxidative stress status in mithun(Bos frontalis)spermatozoa

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Asian pacific Journal of Reproduction 2022年第1期11卷 35-43页

作者： perumal Ponraj Kobu Khate Kezhavituo Vupru ICAR-National Research Centre on Mithun MedziphemaNagaland–797106India ICAR-Central Island Agricultural Research Institute Port Blair744105Andaman and Nicobar IslandsIndia

Objective:To assess the effect of taurine on post-thaw semen quality parameters,sperm kinematics,antioxidant and oxidative stress profiles and sperm cholesterol efflux in mithun(Bos frontalis).Methods:A total of 50 ejaculates(n=25 samples)were selected based on biophysical *** sample was split into four equal aliquots after dilution with the Tris-citrate-glycerol ***Ⅰ,Ⅱ,ⅢandⅣcontained 0 mM(the control),25 mM,50 mM and 100 mM of taurine,***-thawed samples were analysed for motility parameters(progressive forward and in bovine cervical mucus penetration test),kinetic and velocity parameters by computer-assisted sperm analyzer,viability,sperm and nuclear abnormalities,acrosome integrity,plasma membrane and nuclear integrities,sperm enzymatic leakage and biochemical(sperm cholesterol and oxidative stress)***:The extender containing 50 mM taurine led to a significant enhancement in viability,acrosomal integrity,plasma membrane integrity,motility(progressive and in cervical mucus),and sperm cholesterol content and notably reduced sperm morphological and nuclear abnormalities,and leakage of intracellular enzymes compared to other taurine treated and untreated control groups(P<0.05).Moreover,in addition to significant improvement in kinetic and velocity profiles,50 mM taurine protected the integrity of acrosome and biochemical membranes than in the untreated control and other taurine treated *** of 50 mM taurine held a clear advantage over the control or 25 mM or 100 mM taurine in cryopreservation of mithun ***:Taurine(50 mM)supplementation in semen extender can be effectively utilized to reduce oxidative stress and improve post-thaw semen quality in mithun.

关键词： Antioxidants Cryopreservation Kinematic profiles Mithun Oxidative stress Spermatozoa Taurine Semen quality Post-thaw

In vitro antioxidant,anti-diabetic,cholinesterase and tyrosinase inhibitory potential of fresh juice from Citrus hystrix and *** fruits

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Food Science and Human Wellness 2014年第1期3卷 16-25页

作者： Arumugam Abirami Gunasekaran Nagarani perumal Siddhuraju Bioresource Technology Lab School of Life SciencesDepartment of Environmental SciencesBharathiar UniversityCoimbatore 641046Tamil NaduIndia

In the present study,antioxidant potential,α-amylase,α-glucosidase,cholinesterase and tyrosinase inhibitory activity of fresh juice from indigenous fruits of Citrus hystrix and ***(Red&White var.)were investigated using an in vitro *** contents of total phenolics,tannins,and total flavonoids ranged between 836.90 and 909.52 mg gallic acid equivalent(GAE)/L,333.33 and 523.21 mg gallic acid equivalent(GAE)/L and 224.88 and 262.22 mg rutin equivalent/L,*** antioxidant activity of fresh juice was evaluated by employing different in vitro assays such as reducing power assay,DPPH•,ABTS•+and•OH radical scavenging capacities,peroxidation inhibition activity,antihemolytic *** addition,75.55%–79.75%ofα-amylase and 70.68%–72.83%ofα-glucosidase enzyme inhibition characteristics were found under in vitro starch digestion ***,all the juice samples exhibited excellent tyrosinase(76.95%–80.79%),acetylcholinesterase(75.71%–79.74%)andβ-glucuronidase inhibitory activity(68.13%–69.38%).These results indicated that fresh juice of *** and ***(Red&White var.)could be used as a source of antioxidant agents,functional food and nutraceuticals.©2014 Beijing Academy of Food *** and hosting by Elsevier *** rights reserved.

关键词： Citrus fruits Fresh juice Antioxidant potential Enzymatic inhibitory activity Nutraceuticals

Microwave-assisted synthesis,anticonvulsant activity and quantum mechanical modelling of N-(4-bromo-3-methylphenyl) semicarbazones

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2007年第1期8卷 45-55页

作者： SHALINI Mehta YOGEESWARI perumal SRIRAM Dharmarajan INDUJA Sridharan Medicinal Chemistry Research Laboratory Pharmacy Group Birla Institute of Technology & Science Pilani-333031 India

Objective: To study the effect of halo substitution on disubstituted aryl semicarbazones on the anticonvulsant potential and model the activity based on quantum mechanics. Methods: A series of twenty-six compounds of N4-(4-bromo-3-methylphenyl) semicarbazones were synthesized and evaluated for the anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Some potential compounds were also tested in the subcutaneous strychnine (scSTY) and subcutaneous picrotoxin (scPIC) seizure threshold tests. The synthesized compounds were tested for behavioral impairment and CNS (central nervous system) depression in mice. Quantum mechanical modelling was carried out on these compounds to gain understanding on the structural features essential for activity. Results: Some compounds possessed broad spectrum anticonvulsant activity as indicated by their effect in pentylenetetrazole, strychnine, picrotoxin and maximal electro- shock seizures models in resemblance to other aryl semicarbazone derivatives reported earlier. The higher the difference in HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital) energy levels was, the greater was the activity profile. Conclusion: The pharmacophoric requirements for compounds to exhibit anticonvulsant activity that includes one aryl unit in proximity to a hydrogen donor-acceptor domain and an electron donor have been justified with the molecular orbital surface analysis of the synthesized compounds.

关键词： Anticonvulsants Aryl semicarbazones Quantum mechanics (QM) Molecular orbital surfaces

A comparative study on antioxidant potentials,inhibitory activities against key enzymes related to metabolic syndrome,and anti-inflammatory activity of leaf extract from different Momordica species

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Food Science and Human Wellness 2014年第1期3卷 36-46页

作者： Gunasekaran Nagarani Arumugam Abirami perumal Siddhuraju Bioresource Technology Lab School of Life SciencesDepartment of Environmental SciencesBharathiar UniversityCoimbatore 641046Tamil NaduIndia

Momordica species are vegetable crops widely distributed in warmer regions of the *** this work,we describe the antioxidant,enzyme inhibitory and anti-inflammatory effects of the leaves from three different species of *** present investigation was initially carried out to explore the possible link between antioxidant,enzyme inhibitory property of Momordica leaf extract and their total phenolic and flavonoid *** anti-inflammatory activity was tested by using carrageenan-induced paw *** results illustrated an enhanced antioxidant power of wild species comparable with a commercial *** addition,the leaf extract of ***(200 mg/kg)presented a significant anti-inflammatory activity toward carrageenan-induced paw edema in Wistar rats in comparison to indomethacin(10 mg/kg).The contents of flavonoids and total phenolic compounds could be correlated with the antioxidant and enzymes inhibition *** major bioactive compounds of phenolic acids and flavonoids such as gallic acid,chlorogenic acid,caffeic acid,ferulic acid,ellagic acid,catechin,rutin,and quercetin were *** findings suggest that wild Momordica species contains higher potential antioxidant and anti-inflammatory activities than a commercial variety does,which could be tested as drug candidates against oxidative and inflammation-related pathological processes.©2014 Beijing Academy of Food *** and hosting by Elsevier *** rights reserved.

关键词： Momordica Antioxidant In vitro antidiabetic Cholinesterase Anti-inflammatory

Food prospects and nutraceutical attributes of Momordica species:A potential tropical bioresources–A review

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Food Science and Human Wellness 2014年第3期3卷 117-126页

作者： Gunasekaran Nagarani Arumugam Abirami perumal Siddhuraju Bioresource Technology Lab Department of Environmental SciencesSchool of Life SciencesBharathiar UniversityCoimbatore 641046Tamil NaduIndia

Plants with potential therapeutic values have been used from time immemorial to cure various ailments and infectious *** late,scientific evidences have been provided on the potential therapeutic agent exhibited by certain traditionally used vegetable *** importance of wild edible plants may be traced to antiquity but systemic studies are *** the Momordica species have been consumed as vegetable and traditionally used for various *** whole plant parts are ascribed to possess the anti-diabetic effect in traditional medicinal *** active constituents of Momordica plant parts were cucurbitane type triterpenoids,phenolics,glycosides,and several kinds of peptides including Momordica anti-HIV protein(MAP 30).Recent reports revealed the presence of several kinds of cucurbitane type triterpenoids in leaf,stem and fruits of Momordica species having several pharmacological *** is lack of scientific information available on the wild species which also having several bioactive components with potential *** the present review compares and highlights the current knowledge of the nutritional value,phytochemistry and physiological effects of wild species with known variety.

关键词： Momordica spp. Anti-diabetic Triterpenoids Momordica anti-HIV protein(MAP-30 protein)

Hepatoprotective effect of leaf extracts from Citrus hystrix and *** against paracetamol induced liver injury in rats

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Food Science and Human Wellness 2015年第1期4卷 35-41页

The present investigation is aimed to evaluate the hepatoprotective effects of Citrus hystrix and Citrus maxima(Red and White variety)methanolic leaf extracts on paracetamol induced *** extracts were given in the dose of 200 mg/kg body weight for 7 days and toxicity was induced by paracetamol(2 g/kg)on day ***(100 mg/kg body weight)was used as reference *** the 7th day animals were sacrificed and liver function markers(ALT,AST,ALP),total bilirubin and total protein in blood serums and hepatic antioxidants(SOD,CAT,GSH and GPx)in liver homogenate were *** leaf extracts restored the liver function markers and hepatic antioxidants to the normal level than elevated levels noticed on paracetamol control at P<*** of hepatoarchitecture has also been *** present study shows that *** and *** leaf extracts possess hepatoprotective action against paracetamol induced hepatotoxicity.©2015 Beijing Academy of Food *** and hosting by Elsevier *** rights reserved.

关键词： Citrus hystrix Citrus maxima Paracetamol Silymarin Hepatoprotection