The Experts below are selected from a list of 273 Experts worldwide ranked by ideXlab platform

H. Wagner - One of the best experts on this subject based on the ideXlab platform.

W. Dorsch - One of the best experts on this subject based on the ideXlab platform.

Samuel Estradasoto - One of the best experts on this subject based on the ideXlab platform.

  • semisynthesis ex vivo evaluation and sar studies of coumarin derivatives as potential Antiasthmatic Drugs
    European Journal of Medicinal Chemistry, 2014
    Co-Authors: Amanda Sanchezrecillas, Gabriel Navarretevazquez, Sergio Hidalgofigueroa, Maria Yolanda Rios, Maximiliano Ibarrabarajas, Samuel Estradasoto
    Abstract:

    Abstract Asthma is a chronic inflammatory disorder that causes contraction in the smooth muscle of the airway and blocking of airflow. Reversal the contractile process is a strategy for the search of new Drugs that could be used for the treatment of asthma. This work reports the semisynthesis, ex vivo relaxing evaluation and SAR studies of a series of 18 coumarins. The results pointed that the ether derivatives 1–3, 7–9 and 13–15 showed the best activity (Emax = 100%), where compound 2 (42 μM) was the most potent, being 4-times more active than theophylline (positive control). The ether homologation (methyl, ethyl and propyl) in position 7 or positions 6 and 7 of coumarins lead to relaxing effect, meanwhile formation of esters generated less active compounds than ethers. The SAR analysis showed that it is necessary the presence of two small ether groups and the methyl group at position 4 (site 3) encourage biological activity through soft hydrophobic changes in the molecule, without drastically affecting the cLogP.

Peter H. Howarth - One of the best experts on this subject based on the ideXlab platform.

  • What is the nature of asthma and where are the therapeutic targets
    Respiratory Medicine, 1997
    Co-Authors: Peter H. Howarth
    Abstract:

    The characterisation of chronic asthma as an inflammatory condition of the human airway, associated with heightened airway responsiveness to a variety of bronchial stimuli, has lead to the clarification of therapeutic strategies. These strategies have focused on bronchodilation and attenuation of airway inflammation. Inhaled corticosteroids effectively reduce chronic inflammation and produce substantial symptomatic relief in most patients. This article examines the pathophysiology of asthma and discusses the interpretation of current methods of assessment, and the targets and actions of inhaled Antiasthmatic Drugs in relationship to central and peripheral airway events.

Sarah N. Gasmi - One of the best experts on this subject based on the ideXlab platform.