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Kūkatpalli, India

Reddy L.V.,Jawaharlal Nehru Technological University Anantapur | Suman A.,Jawaharlal Nehru Technological University Anantapur | Beevi S.S.,Sudan University of Science and Technology | Mangamoori L.N.,Sudan University of Science and Technology | And 2 more authors.
Journal of the Brazilian Chemical Society | Year: 2010

We report the design and synthesis of 1-aroyl-2-(alkenyl/aryl)idene hydrazines as hybrid molecules derived from mefenamic acid and substituted hydrazones. A number of compounds based on this new scaffold were prepared in good yields. The key intermediate N-acylhydrazine, prepared from mefenamic acid, was coupled with a variety of aldehydes under conventional as well as microwave irradiation conditions. The second approach, that requires short reaction time, can be carried out under a solvent free condition and does not require the use of an acid catalyst or solid support. Some of the compounds synthesized showed cytotoxic activities in vitro. © 2010 Sociedade Brasileira de Química.

Pal S.,MNR Degree and PG College | Durgadas S.,Sudan University of Science and Technology | Nallapati S.B.,Sudan University of Science and Technology | Mukkanti K.,Sudan University of Science and Technology | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized are presented. © 2011 Elsevier Ltd. All rights reserved.

Pal S.,MNR Degree and PG College | Chatare V.,Dr. Reddys Laboratories Ltd | Pal M.,University of Hyderabad
Current Organic Chemistry | Year: 2011

The prevalence of isocoumarins in numerous natural products that exhibit a wide range of biological activities has generated a continued and enormous interest among synthetic and medicinal chemists. The isocoumarin framework represents one of the privileged structures for the development of natural product-inspired compounds of potential biological interest. Considerable efforts have been devoted towards the synthesis of isocoumarins via either traditional or transition-metal catalyzed reactions. Among the metal catalyzed reactions, the use of Cu, Pd, Ag, Ru, Rh or Ir salts/complexes for the construction of isocoumarin ring are noteworthy. Among the other methodologies, halo-lactonization emerged as a practical process. Apart from preparing a variety of isocoumarins and thienopyranones, synthesis of naturally occurring and bioactive isocoumarins have been carried out by using cutting edge technologies. This review article will briefly cover all these aspects along with the synthetic utility of isocoumarins, highlighting recent developments. © 2011 Bentham Science Publishers Ltd.

Bhattacharya A.,Jadavpur University | Kankanala K.,Jawaharlal Nehru Technological University Anantapur | Kankanala K.,MNR Degree and PG College | Pal S.,MNR Degree and PG College | Mukherjee A.K.,Jadavpur University
Journal of Molecular Structure | Year: 2010

A nimesulide derivative, N-[4-(2,5-dioxo-2,5-dihydropyrrol-1-yl)-2-phenoxyphenyl]methanesulfonamide (2), was synthesized and its crystal structure has been determined from X-ray powder diffraction data following direct-space global optimization technique and refined by the Rietveld method. The molecular geometry and electronic structure of the title compound were calculated at the DFT level using the hybrid exchange-correlation functional, BLYP. The optimized molecular geometry of 2 corresponds closely to that obtained from the X-ray structure analysis. Intermolecular N-H···O and C-H···O hydrogen bonds in 2 form one-dimensional polymeric chains of R2 2(8) rings propagating along the [1 0 0] direction. Further linking between parallel chains via C-H···π (arene) hydrogen bonds generates a two-dimensional supramolecular assembly in the (1 1 0) plane. The title compound exhibits potential anti-inflammatory activity and can induce 64% edema inhibition in rat paws. © 2010 Elsevier B.V. All rights reserved.

Praveena K.S.S.,MNR Degree and PG College | Durgadas S.,MSN Pharmachem Pvt. Ltd | Suresh Babu N.,Jawaharlal Nehru Technological University | Akkenapally S.,Indian Institute of Chemical Technology | And 5 more authors.
Bioorganic Chemistry | Year: 2014

The 2,2,4-trimethyl-1,2-dihydroquinolinyl substituted 1,2,3-triazole derivatives were designed as potential inhibitors of PDE4B. These compounds were synthesized via a multi-step sequence consisting of copper-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step in aqueous media. The required alkynes were prepared from nimesulide via N-propargylation and then nitro group reduction followed by a CAN mediated modified Skraup reaction of the resulting amine. All the synthesized compounds showed PDE4B inhibitory properties in vitro at 30 μM with two compounds showing >50% inhibition that were supported by the in silico docking results of these compounds at the active site of PDE4B. Three of these PDE4 inhibitors showed promising cytotoxic properties against A549 human lung cancer cells in vitro with IC50 ∼8-9 μM. © 2013 Elsevier Inc. All rights reserved.

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