Vinayakrao Patil Mahavidyalaya

Aurangābād, India

Vinayakrao Patil Mahavidyalaya

Aurangābād, India

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Thore S.N.,Vinayakrao Patil Mahavidyalaya | Gupta S.V.,Vinayakrao Patil Mahavidyalaya
Medicinal Chemistry Research | Year: 2013

A series of substituted thiazole derivatives (6-16) were synthesized to obtain new compounds with potential anti-inflammatory and analgesic activities. At equimolar oral doses, compounds 3-(piperidin-1-yl-methyl)-1, 3, 4-oxadiazol-2-thione (14), 5-amino-4-ethyl ester pyrazole (15), and 5-amino-3-phenylpyrazole derivatives (16) displayed anti-inflammatory and analgesic activities significant to those of diclofenac sodium in the carrageenan-induced paw edema test in rat and acetic acid-induced writhing test in mice,-respectively. The most active members of the series (9, 11, 14, 15, and 16) were selected for ulcerogenic potential study. These compounds exhibited quite less ulcerogenic index in the range of 0.44 to 0.62 whereas diclofenac sodium showed 4.67. The docking study results also indicated that the compound 6, 7, 8, 11, and 14 exhibited the docking score ranging from -3.951 to -4.691. © 2012 Springer Science+Business Media New York.


Gupta S.V.,Vinayakrao Patil Mahavidyalaya | Dekhane D.,Vinayakrao Patil Mahavidyalaya | Pawar S.,Vinayakrao Patil Mahavidyalaya | Thore S.N.,Vinayakrao Patil Mahavidyalaya
Medicinal Chemistry Research | Year: 2013

With the aim of developing potential H1-antihistaminic agents, a series of novel 2-substituted-3-carboxamido-4-oxo-4H-pyrimido[2,1-b][1,3] benzothiazole (8a-g) and 2-substituted-3-carboxamido-8-chloro-4-oxo-4H- pyrimido[2,1-b][1,3]benzothiazole (9a-g) were synthesized and evaluated in vitro for H1-antihistaminic activity on guinea pig ileum preparation. IC50 values of the compounds were found to be in the micromolar range. Chlorpheniramine maleate was used as a standard drug. The active derivatives (8d-8g and 9d-9g) were found to have IC50 values comparable to reference standard chlorpheniramine maleate. The sedative potential of both series (8a-g and 9a-g) is less than the reference drug. Hence, it could serve as prototype molecules for further development as a new class of H1-antihistaminic agents. © 2012 Springer Science+Business Media, LLC.


Labade V.B.,Dr. Babasaheb Ambedkar Marathwada University | Pawar S.S.,Vinayakrao Patil Mahavidyalaya | Shingare M.S.,Dr. Babasaheb Ambedkar Marathwada University
Monatshefte fur Chemie | Year: 2011

A green approach to the Aza-Michael addition reaction between an amine and α,β-unsaturated compounds has been achieved by conventional as well as non-conventional methods. The reaction is catalyzed by cesium fluoride (CsF) in aqueous media at ambient temperature to afford the product in excellent yield. Ultrasound irradiation has been used as a non-conventional energy source, which reduces the reaction time with improved product yield. © 2011 Springer-Verlag.


Pardeshi S.D.,Vinayakrao Patil Mahavidyalaya | Sonar J.P.,Vinayakrao Patil Mahavidyalaya | Pawar S.S.,Vinayakrao Patil Mahavidyalaya | Dekhane D.,Vinayakrao Patil Mahavidyalaya | And 3 more authors.
Journal of the Chilean Chemical Society | Year: 2014

Ammonium nickel sulphate [(NH4)2SO4.NiSO4.6H2O] was found as a new catalyst to synthesis 2-aryl benzimidazole, 2-aryl benzothiazole and 2-aryl benzoxazole in aqueous media under sonication irradiation. The procedure is an eco-friendly, efficient and provides simple workup and good yield.


Dixit P.P.,Vinayakrao Patil Mahavidyalaya | Dixit P.P.,Dr. Babasaheb Ambedkar Marathwada University | Thore S.N.,Vinayakrao Patil Mahavidyalaya
European Journal of Medicinal Chemistry | Year: 2016

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of tuberculosis (TB). Although, EI have emerged as innovative approach of treatment for multi drug resistant (MDR) & extensively drug resistant tuberculosis (XDR-TB), toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of TB initially against Mycobacterium smegmatis mc2155. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 144, 145, 154 and 163 were then tested for their GEI action against Mycobacterium tuberculosis (Mtb). Synthesized compounds were also tested for their synergistic action with first line and second line anti-TB drugs and ethidium bromide (EtBr). We arrived at compound 135 as most potent dual inhibitor of tuberculosis. © 2015 Elsevier Masson SAS.


Sonar J.P.,Vinayakrao Patil Mahavidyalaya | Pardeshi S.D.,Vinayakrao Patil Mahavidyalaya | Pawar S.S.,Vinayakrao Patil Mahavidyalaya | Thore S.N.,Vinayakrao Patil Mahavidyalaya
Indian Journal of Heterocyclic Chemistry | Year: 2012

Boric acid (10 mmol%) with TBAB (10 mmol%) in water was used as a catalyst for the synthesis of 2-arylsubstituted benzimidazoles efficiently. Simple and convenient procedure, easy purification and shorter reaction time are the advantageous features of this method.


Bhagaf S.S.,Dr. Babasaheb Ambedkar Marathwada University | Thore S.N.,Vinayakrao Patil Mahavidyalaya | Ghotekar D.S.,Dr. Babasaheb Ambedkar Marathwada University | Josh R.S.P.,Dr. Babasaheb Ambedkar Marathwada University | And 3 more authors.
Indian Journal of Heterocyclic Chemistry | Year: 2012

A new series of 2-acetylphenyl 3,5-diflurobenzoates, 1-(3,5-difluorophenyl) -3-(2-hydroxyphenyl) propane-1,3-diones, 2-(3,5-difluorophenyl)-4H-chromen-4- ones and 2-(5-(3,5-difluorophenyl)-1H-pyrazol-3-yl) phenols have been synthesized and screened as antibacterial agents. In the series 3a, 4a, 4b, 4f, 4h exhibited moderate antibacterial activity against Staphylococcus aureus (ATCC 25923).


Pardeshi S.D.,Vinayakrao Patil Mahavidyalaya | Sonar J.P.,Vinayakrao Patil Mahavidyalaya | Zine A.M.,Vinayakrao Patil Mahavidyalaya | Thore S.N.,Deogiri College
Journal of the Iranian Chemical Society | Year: 2013

In the present study adsorption behavior of methylene blue and rhodamine B from aqueous solution using adsorbent prepared from "Hyptis suaveolens" (Vilayti Tulsi) was investigated as a function of parameters such as initial concentration, adsorbent dose, pH, contact time and temperature. The adsorption process was pH dependent. The thermodynamic parameters such as ΔG, ΔH and, ΔS were calculated to investigate the nature of adsorption, their values indicate that the adsorption process is favorable. The first-order, second-order and intra-particle diffusion models were used to describe the kinetic parameter. The Freundlich and Langmuir adsorption models were applied to describe the adsorption equilibrium. Column study was conducted for both dyes. © 2013 Iranian Chemical Society.


PubMed | Vinayakrao Patil Mahavidyalaya and Dr. Babasaheb Ambedkar Marathwada University
Type: | Journal: European journal of medicinal chemistry | Year: 2015

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of tuberculosis (TB). Although, EI have emerged as innovative approach of treatment for multi drug resistant (MDR) & extensively drug resistant tuberculosis (XDR-TB), toxicity profile limits their wider use. To address this issue, we have attempted synthesizing hybrid molecules those results by combining known EI and triazole. This synthesis was aimed to arrive at structure that possesses pharmacophore from known EI. Synthesized molecules were evaluated as growth inhibitors (GI) and Efflux inhibitor of TB initially against Mycobacterium smegmatis mc(2)155. Pharmacologically active compounds were then tested for their cytotoxicity to further narrow down search. Most active compounds 144, 145, 154 and 163 were then tested for their GEI action against Mycobacterium tuberculosis (Mtb). Synthesized compounds were also tested for their synergistic action with first line and second line anti-TB drugs and ethidium bromide (EtBr). We arrived at compound 135 as most potent dual inhibitor of tuberculosis.

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