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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. Source


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. Source


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. Source


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. Source


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. Source

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