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Aminoquinoline

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Diwan S. Rawat – One of the best experts on this subject based on the ideXlab platform.

  • 4 Aminoquinoline based molecular hybrids as antimalarials an overview
    Current Topics in Medicinal Chemistry, 2014
    Co-Authors: Sunny Manohar, Mohit Tripathi, Diwan S. Rawat

    Abstract:

    In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is
    fast becoming an alternative to other existing strategies of drug development. These hybrids also known as ‘dual drugs’ or
    ‘double drugs’ are especially found to be effective in overcoming drug resistance problems. Towards this end, a lot of effort
    has been put for generating 4-Aminoquinoline based hybrid molecules as next generation antimalarial drugs effective
    in malarial chemotherapy. This short review deals about the recent advances carried in the field of 4-Aminoquinoline
    based molecular hybrids as potential antimalarial agents. It also presents a brief and simplified story on the development
    of 4-Aminoquinolines as a mainstay in malarial research programmes.

  • synthesis of 4 Aminoquinoline 1 2 3 triazole and 4 Aminoquinoline 1 2 3 triazole 1 3 5 triazine hybrids as potential antimalarial agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Sunny Manohar, Shabana I. Khan, Diwan S. Rawat

    Abstract:

    : We report herein synthesis of a series of 4-Aminoquinoline-1,2,3-triazole and 4-Aminoquinoline-1,2,3-triazole-1,3,5-triazine hybrids and evaluate their antimalarial activity against D6 and W2 strains of Plasmodium falciparum. To study the structure-activity relationship of substituted 4-Aminoquinoline-based hybrids, 34 structurally diverse compounds were synthesized and tested against D6 and W2 strains of P. falciparum. Some of the compounds have shown promising antimalarial activity without toxicity against Vero cells.

  • Synthesis of 4‐Aminoquinoline‐1,2,3‐triazole and 4‐Aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine Hybrids as Potential Antimalarial Agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Sunny Manohar, Shabana I. Khan, Diwan S. Rawat

    Abstract:

    : We report herein synthesis of a series of 4-Aminoquinoline-1,2,3-triazole and 4-Aminoquinoline-1,2,3-triazole-1,3,5-triazine hybrids and evaluate their antimalarial activity against D6 and W2 strains of Plasmodium falciparum. To study the structure-activity relationship of substituted 4-Aminoquinoline-based hybrids, 34 structurally diverse compounds were synthesized and tested against D6 and W2 strains of P. falciparum. Some of the compounds have shown promising antimalarial activity without toxicity against Vero cells.

Prem M S Chauhan – One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of new 4-Aminoquinolines and quinoline-acridine hybrids as antimalarial agents.
    Bioorganic & Medicinal Chemistry Letters, 2010
    Co-Authors: Ashok Kumar, Kumkum Srivastava, S. Raja Kumar, Surendra Puri, Prem M S Chauhan

    Abstract:

    Abstract Despite emergence of resistance to CQ and other 4-Aminoquinoline drugs in most of the endemic regions, research findings provide considerable support that there is still significant potential to discover new affordable, safe, and efficacious 4-Aminoquinoline antimalarials. In present study, new side chain modified 4-Aminoquinoline derivatives and quinoline–acridine hybrids were synthesized and evaluated in vitro against NF 54 strain of Plasmodium falciparum. Among the evaluated compounds, compound 17 (MIC = 0.125 μg/mL) was equipotent to standard drug CQ (MIC = 0.125 μg/mL) and compound 21 (MIC = 0.031 μg/mL) was four times more potent than CQ. Compound 17 showed the curative response to all the treated swiss mice infected with CQ-resistant N-67 strain of Plasmodium yoelii at the doses 50 mg/kg and 25 mg/kg for four days by intraperitoneal route and was found to be orally active at the dose of 100 mg/kg for four days. The promising antimalarial potency of compound 17 highlights the significance of exploring the privileged 4-Aminoquinoline class for new antimalarials.

  • synthesis of novel thiourea thiazolidinedione and thioparabanic acid derivatives of 4 Aminoquinoline as potent antimalarials
    Bioorganic & Medicinal Chemistry Letters, 2009
    Co-Authors: Naresh Sunduru, Kumkum Srivastava, Sundaresan Rajakumar, Sunil K Puri, J K Saxena, Prem M S Chauhan

    Abstract:

    In search of new 4-Aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-Aminoquinoline were synthesized and screened for their antimalarial activity. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of P. falciparum in an in vitro model with an IC50 of 6.07 ng/mL and also showed in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of P. yoelii. Malaria is a devastating disease caused by four species of genus plasmodium which afflicts more than 40% of the world population, causing an estimated mortality of 1.5-2.7 million people annually. 1 The current epidemic is fueled about the parasite Plasmodium falciparum, responsible for the most deadly cases of malaria and its resistance to the antimalarial drugs. Chloroquine (CQ) has historically been mainstay of malaria treatment, particularly with P. falciparum in pregnant women and children under the age of five. 2 It acts by binding to heme molecules released from the hemoglobin that is digested by malaria parasites as they grow within their host red blood cells. This binding interferes with the process by which heme is normally incorporated into inert crystals (β-hematin) and detoxified, thereby accumulation of toxic levels of heme leads to the death of parasite.

  • synthesis of novel thiourea thiazolidinedione and thioparabanic acid derivatives of 4 Aminoquinoline as potent antimalarials
    Bioorganic & Medicinal Chemistry Letters, 2009
    Co-Authors: Naresh Sunduru, Kumkum Srivastava, Sundaresan Rajakumar, Sunil K Puri, J K Saxena, Prem M S Chauhan

    Abstract:

    Abstract In search of new 4-Aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-Aminoquinoline were synthesized and screened for their antimalarial activities. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC50 of 6.07 ng/mL and also showed an in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.

Sunny Manohar – One of the best experts on this subject based on the ideXlab platform.

  • 4 Aminoquinoline based molecular hybrids as antimalarials an overview
    Current Topics in Medicinal Chemistry, 2014
    Co-Authors: Sunny Manohar, Mohit Tripathi, Diwan S. Rawat

    Abstract:

    In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is
    fast becoming an alternative to other existing strategies of drug development. These hybrids also known as ‘dual drugs’ or
    ‘double drugs’ are especially found to be effective in overcoming drug resistance problems. Towards this end, a lot of effort
    has been put for generating 4-Aminoquinoline based hybrid molecules as next generation antimalarial drugs effective
    in malarial chemotherapy. This short review deals about the recent advances carried in the field of 4-Aminoquinoline
    based molecular hybrids as potential antimalarial agents. It also presents a brief and simplified story on the development
    of 4-Aminoquinolines as a mainstay in malarial research programmes.

  • synthesis of 4 Aminoquinoline 1 2 3 triazole and 4 Aminoquinoline 1 2 3 triazole 1 3 5 triazine hybrids as potential antimalarial agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Sunny Manohar, Shabana I. Khan, Diwan S. Rawat

    Abstract:

    : We report herein synthesis of a series of 4-Aminoquinoline-1,2,3-triazole and 4-Aminoquinoline-1,2,3-triazole-1,3,5-triazine hybrids and evaluate their antimalarial activity against D6 and W2 strains of Plasmodium falciparum. To study the structure-activity relationship of substituted 4-Aminoquinoline-based hybrids, 34 structurally diverse compounds were synthesized and tested against D6 and W2 strains of P. falciparum. Some of the compounds have shown promising antimalarial activity without toxicity against Vero cells.

  • Synthesis of 4‐Aminoquinoline‐1,2,3‐triazole and 4‐Aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine Hybrids as Potential Antimalarial Agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Sunny Manohar, Shabana I. Khan, Diwan S. Rawat

    Abstract:

    : We report herein synthesis of a series of 4-Aminoquinoline-1,2,3-triazole and 4-Aminoquinoline-1,2,3-triazole-1,3,5-triazine hybrids and evaluate their antimalarial activity against D6 and W2 strains of Plasmodium falciparum. To study the structure-activity relationship of substituted 4-Aminoquinoline-based hybrids, 34 structurally diverse compounds were synthesized and tested against D6 and W2 strains of P. falciparum. Some of the compounds have shown promising antimalarial activity without toxicity against Vero cells.