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Sheorey R.V.,Karpagam University | Alagarsamy V.,Medicinal Chemistry Research Laboratory
Tropical Journal of Pharmaceutical Research | Year: 2013

Purpose: To synthesize a series of novel 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones and evaluate them for their analgesic and anti-inflammatory activities. Methods: The compounds, 3-ethyl-2-substituted amino-quinazolin-4(3H)-ones, were synthesized by reacting the amino group of 3-ethyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The synthesized compounds were characterized by Fourier transform infrared (FTIR), protonnuclear magnetic resonance spectroscopy (1H-NMR) and mass spectrometry. The purity of the compounds was determined by elemental analysis. Test for analgesic activity was performed by tail-flick technique using Wistar albino mice while anti-inflammatory activity was evaluated by carrageenaninduced paw oedema test in rats. Diclofenac sodium was used as positive control for both analgesic and anti-inflammatory activities. Results: The compound, 3-ethyl-2-(cyclohexylidene-hydrazino)-3H-quinazolin-4-one (AS1), emerged as the active analgesic (activity, 63.89 %) and anti-inflammatory (activity, 60.00 %) compound of the series, and compared well with the reference standard, diclofenac sodium, which exbited analgesic and anti-inflammatory activities of 62.04 and 65.11 %, respectively Conclusion: The compound (AS1) can serve as a lead molecule for further development to a clinically useful novel class of analgesic and anti-inflammatory agents. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria.


Alagarsamy V.,Medicinal Chemistry Research Laboratory | Sathesh Kumar S.,Tamil University | Nisha J.C.,Manonmaniam Sundaranar University | Narsimha Reddy Y.,Kakatiya University
Journal of Ethnopharmacology | Year: 2011

Ethnopharmacological relevance: The rhizomes of Alpinia galanga (L.) Willd (Zingiberaceae), a ginger substitute for flavouring food was traditionally used as nervine tonic and stimulant. Aim of the study: This investigation is designed to screen cognitive improvement of Alpinia galanga (AG) fractions in Alzheimer's type of amnesia in mice induced by Aβ (25-35). Materials and methods: Alzheimer's disease induced mice treated with fractions (n-hexane, chloroform and ethyl acetate) of AG in 200 and 400 mg/kg. Neurotoxicity was induced by intracerebroventricular injection of Aβ (25-35) on the 14th day of 21 days drug treatment. Open field and water maze were carried to determine habituation memory and hippocampal memory. Na +/K +-ATPase, acetylcholinesterase (AChE) and antioxidant enzymes (SOD, GPx, catalase and vitamin C) were determined in brain tissue homogenate to estimate the brain biochemical changes and its anti-amnesic potential with intensity of oxidative stress signaling. Further bioactive (chloroform) fraction was eluted through column chromatography to identify the lead molecules. Results: Increased habituation memory and decreased escape latency in behavioral parameter are the indicative of the cognitive enhancement after treatment with Alpinia galanga fractions. Increment in Na +/K +-ATPase and antioxidant activity depicts brain membrane integrity improvement and free radical scavenging property. AChE level was decreased to improve the cognition by enhancing cholinergic transmission. Conclusion: Anti-amnesic effect was exerted by various fractions of Alpinia galanga. Among all fractions, preeminent neuroprotection was exerted by chloroform fraction, which has compound, 1′δ-1′-acetoxyeugenol acetate and it may be a potential therapeutic agent for Alzheimer's type of amnesia. These results further motivate us to explore the activity of lead compound's anti-amnesic effect on transgenic mice model of AD. © 2011 Elsevier Ireland Ltd.


Prakash C.R.,DCRM Pharmacy College | Raja S.,Gandhi Institute of Technology and Management | Saravanan G.,Medicinal Chemistry Research Laboratory
Chinese Chemical Letters | Year: 2012

A new series of isatin semicarbazide derivatives (7a-7j) were synthesized and characterized by spectroscopic means and elemental analysis. Analgesic and anti-inflammatory screening was performed using tail-flick technique and the carrageenan-induced foot paw edema test respectively. The ulcerogenicity was also determined for all the compounds. Some of the compounds showed moderate enhancement of the activity. Among the synthesized derivatives, compound 7d showed higher analgesic, antiinflammatory and one-third of ulcer index of the reference drug. © 2012 Chinnasamy Rajaram Prakash.


Sivakumar D.,HIGH-TECH | Shankar D.,Medicinal Chemistry Research Laboratory
Agris On-line Papers in Economics and Informatics | Year: 2012

Textile industry processes are among the most environmentally unfriendly industrial processes, because they produce coloured wastewaters that are heavily polluted the environment. Therefore, wastewater from textile industry has to be treated before being discharged into the environment. In this study, experiments were performed at pH of 7 to investigate the adsorption capacities of locally available low cost bio-adsorbents like neem leaves, orange peels, peanut hulls and coconut coir pith powders to remove colour in a textile industry wastewater. The experiments were conducted by different process parameters like adsorbent dosage, temperature, contact time and agitator speed using batch adsorption method and for both with and without aeration. From the experimental investigations, the maximum colour removal percentage for both with and without aeration in a textile industry wastewater was obtained at an optimum bio-adsorbent dosage of 300 mg, an optimum contact time of 75 min., an optimum temperature of 330 K and an optimum agitator speed of 600 rpm. Further, from the validation experiments, it was found that results were higher than the results obtained by different process parameters for both with and without aeration. From the results of various process parameters, peanut hulls powder achieved the maximum colour removal percentage for both with and without aeration followed by coconut coir pith, orange peels and neem leaves powders. However, the order of increased in colour removal percentage with aeration is orange peels powder followed by neem leaves, peanut hulls and coconut coir pith powders. © 2010.


Ravichandran V.,AIMST University | Jain A.,Dr. H. S. Gour Vishwavidyalaya | Kumar K.S.,Medicinal Chemistry Research Laboratory | Rajak H.,Guru Ghasidas University | Agrawal R.K.,Dr. H. S. Gour Vishwavidyalaya
Chemical Biology and Drug Design | Year: 2011

A series of 1,3-thiazolidin-4-one derivatives were prepared by the reaction of respective aromatic amine, aromatic aldehyde, and thioglycolic acid in dry benzene/toluene. The newly synthesized compounds were characterized on the basis of elemental analysis, IR, 1HNMR, and mass spectra. The newly synthesized final compounds were evaluated for their in vitro antibacterial, antifungal, and anti-viral activities. Preliminary results indicated that some of the compounds demonstrated antibacterial activity in the range of 7-13μg/mL, antifungal activity in the range of 13-17μg/mL, comparable with the standard drugs, ciprofloxacin and fluconazole. Structure-activity relationship studies revealed that the nature of the substituents at the 2 and 3 positions of the thiazolidinone nucleus had a significant impact on the in vitro antimicrobial and anti-viral activity of these classes of agents. © 2011 John Wiley & Sons A/S.


Kumar K.S.,Medicinal Chemistry Research Laboratory | Ganguly S.,Birla Institute of Technology | Veerasamy R.,AIMST University | De Clercq E.,Rega Institute for Medical Research
European Journal of Medicinal Chemistry | Year: 2010

A new series of 3-(benzylideneamino)-2-phenylquinazoline-4(3H)-ones were prepared through Schiff base formation of 3-amino-2-phenyl quinazoline-4(3)H-one with various substituted carbonyl compounds. Their chemical structures were elucidated by spectral studies. Cytotoxicity and antiviral activity were evaluated against herpes simplex virus-1 (KOS), herpes simplex virus-2 (G), vaccinia virus, vesicular stomatitis virus, herpes simplex virus-1 TK- KOS ACVr, para influenza-3 virus, reovirus-1, Sindbis virus, Coxsackie virus B4, Punta Toro virus, feline corona virus (FIPV), feline herpes virus, respiratory syncytial virus, influenza A H1N1 subtype, influenza A H3N2 subtype, and influenza B virus. Compound 2a showed better antiviral activity against the entire tested virus. © 2010 Elsevier Masson SAS. All rights reserved.


Gawande S.S.,Medicinal Chemistry Research Laboratory | Warangkar S.C.,M.R.Research | Bandgar B.P.,University of Solapur | Khobragade C.N.,M.R.Research
Bioorganic and Medicinal Chemistry | Year: 2013

As a part of ongoing studies in developing new Tyrosinase inhibitors, a class of structurally novel 2-(2,4-dimethoxy phenylamino)-5 methylene-4- thiazolinone derivatives were synthesized by incorporating 2-(2,4-dimethoxy- phenylamino)-thiazol-4-one with various 1-(1-methyl-buta-1,3-dienyl)-3-phenyl- 1H-pyrazole-4-carbaldehyde. The results showed that some of the synthesized compounds exhibited significant inhibitory activities. Especially, 5-[3-(2-chloro-phenyl)-1-phenyl-1H-pyrazol-4-ylmethylene]-2-(2, 4-dimethoxy-phenylamino)-thiazol-4-one (5h) and 5-[3-(3-chloro-phenyl)-1-phenyl- 1H-pyrazol-4-ylmethylene]-2-(2,4-dimethoxy-phenylamino)-thiazol-4-one (5g) possessing 2-chloro-phenyl and 3-chloro-phenyl group exhibited the most potent tyrosinase inhibitory activity with an IC50 value of 34.12 and 52.62 μM, respectively. The inhibition mechanism analysis of 5h and 5g thiazolidinone derivatives demonstrated that the inhibitory effects of the compounds on tyrosinase were reversible and competitive. Preliminary structure-activity relationships (SAR) analysis suggested that further development of such compounds might be of interest, as it manifests simple reversible slow binding inhibition against monophenolase and diphenolase. © 2013 Elsevier Ltd.All rights reserved.


Chandra Sekhar K.B.,JNTUA OTRI | Nivedhitha S.,Ratnam Institute of Pharmacy | Alagarsamy V.,Medicinal Chemistry Research Laboratory | Gobinath M.,Ratnam Institute of Pharmacy
International Journal of Pharma and Bio Sciences | Year: 2015

Ficus dalhousiae Miq.(Family:Moraceae) known as Somalvalkam in Sanskrit is an endemic to peninsular India and very rare plant of Andhra Pradesh. It is found growing in rock crevices of dry deciduous forest. It is used in traditional system of Indian medicine in the treatment of liver disorders and cardiac problems. Ficus species are rich source of flavonoids and polyphenolic compounds that are responsible for the treatment of oxidative stress related diseases. As there are no reports available on the morphology and phytochemical studies of the leaves and stem bark of Ficus dalhousiae, the present investigation was carried out to lay down the standards, which could be very useful in the future experimental studies. The study includes macroscopy, microscopy, preliminary phytochemical screening, fluorescence analysis and physicochemical constants. The chief features of the transverse section of leaves are the presence of single layered palisade layer, cyclic stomata, druses of calcium oxalate and vascular bundles. Stem bark shows prismatic calcium oxalate, high tannin content in periderm, abundant starch. The main powder characters are calcium oxalate, unicellular covering trichomes, isolated cystoliths, laticifers. The preliminary phytochemical screening shows the presence of steroids, cardiac glycosides, alkaloids, flavonoids, tannins and carbohydrates. This study along with the quantitative microscopic data can be useful in the detection and evaluation of the leaf and stem bark material in any form or formulations of this rare and endemic species.


Alagarsamy V.,Medicinal Chemistry Research Laboratory | Narendhar B.,Medicinal Chemistry Research Laboratory | Sulthana M.T.,Medicinal Chemistry Research Laboratory | Raja Solomon V.,Medicinal Chemistry Research Laboratory
Medicinal Chemistry Research | Year: 2014

A series of novel 3-(4-chlorophenyl)-2-(2-(4-substituted)-2-oxoethylthio)quinazolin-4(3H)-one was synthesized by the reaction of 2-(3-(4-chlorophenyl)-4-oxo-3,4-dihydroquinazolin-2-ylthio)acetyl chloride with various amines. The starting material, (3-(4-chlorophenyl)-4-oxo-3,4-dihydroquinazolin-2-ylthio)acetyl chloride was synthesized from 4-chloroaniline by a multistep synthesis. All the title compounds were tested for their in vivo H1-antihistaminic activity on conscious guinea pigs at the dose level of 10 mg/kg using chlorpheniramine maleate as the reference standard. The results of the biological activity indicate that the test compounds protected the animals from histamine-induced bronchospasm significantly. Compound 3-(4-chlorophenyl)-2-(2-(4-methylpiperazin-1-yl)-2-oxo-ethylthio) quinazolin-4(3H)-one (1) emerged as the most potent compound of the series (71.13 % protection) when compared to the reference standard chlorpheniramine maleate (70.09 % protection). Interestingly, compound A1 shows negligible sedation (12 %) compared to chlorpheniramine maleate (32 %). Therefore, compound A1 can serve as the lead molecule for further development. © Springer Science+Business Media 2014.


Krishnan S.K.,Medicinal Chemistry Research Laboratory | Ganguly S.,Birla Institute of Technology | Veerasamy R.,AIMST University | Jan B.,Rega Institute for Medical Research
European Review for Medical and Pharmacological Sciences | Year: 2011

Objectives: A series of 3-(benzylideneamino)-2-phenyl quinazoline-4(3H)- ones was synthesized by reaction of 3-amino-2-phenyl-3H-quinazoline-4-one with various carbonyl compounds. Materials and Methods: Chemical structures of the synthesized compounds were confirmed by IR, 1H-NMR and mass spectral analysis. Title compounds were investigated for cytotoxicity and antiviral activity against herpes simplex virus-1 (KOS), herpes simplex virus-2 (G), vaccinia virus, vesicular stomatitis virus, herpes simplex virus-1 TK- KOS ACVr, para influenza-3 virus, reovirus-1, Sindbis virus, Coxsackie virus B4, Punta Toro virus, feline corona virus (FIPV), feline herpes virus, respiratory syncytial virus, influenza A H1N1 subtype, influenza A H3N2 subtype, influenza B and vesicular stomatitis virus. Results and Conclusion: Compound 3d was found inhibit viral replication of para influenza-3virus, reovirus-1, Sindbis virus, Coxsackie virus B4, Punta Toro virus in Vero cell cultures. (Chemical Equation Presented).

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