140195-91-1Relevant academic research and scientific papers
The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen der p 1: An innovative approach to the treatment of allergic asthma
Newton, Gary K.,Perrior, Trevor R.,Jenkins, Kerry,Major, Meriel R.,Key, Rebekah E.,Stewart, Mark R.,Firth-Clark, Stuart,Lloyd, Steven M.,Zhang, Jihui,Francis-Newton, Nicola J.,Richardson, Jonathan P.,Chen, Jie,Lai, Pei,Garrod, David R.,Robinson, Clive
, p. 9447 - 9462 (2015/01/16)
Blocking the bioactivity of allergens is conceptually attractive as a small-molecule therapy for allergic diseases but has not been attempted previously. Group 1 allergens of house dust mites (HDM) are meaningful targets in this quest because they are globally prevalent and clinically important triggers of allergic asthma. Group 1 HDM allergens are cysteine peptidases whose proteolytic activity triggers essential steps in the allergy cascade. Using the HDM allergen Der p 1 as an archetype for structure-based drug discovery, we have identified a series of novel, reversible inhibitors. Potency and selectivity were manipulated by optimizing drug interactions with enzyme binding pockets, while variation of terminal groups conferred the physicochemical and pharmacokinetic attributes required for inhaled delivery. Studies in animals challenged with the gamut of HDM allergens showed an attenuation of allergic responses by targeting just a single component, namely, Der p 1. Our findings suggest that these inhibitors may be used as novel therapies for allergic asthma.
Pyruvamide Compounds as Inhibitors of Dust Mite Group 1 Peptidase Allergen and Their Use
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, (2013/02/27)
The present invention pertains generally to the field of therapeutic compounds and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as “PVA compounds”), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.
A fast procedure for the preparation of amides/peptides from carboxylic acids and azides via two redox reactions: Application to the synthesis of methionine enkephalin
Ghosh, Sunil K.,Verma, Rekha,Ghosh, Usha,Mamdapur, Vasant R.
, p. 1705 - 1711 (2007/10/03)
A one-pot self regulated approach for the synthesis of amides/peptides based on two reduction-oxidation (redox) reactions has been described. The primary and secondary amides/peptides are made by using azidotrimethylsilane and alkyl azides/α-azido acid de
One pot amide/peptide synthesis via two redox reactions
Ghosh,Singh,Mamdapur
, p. 805 - 808 (2007/10/02)
A new and highly efficient one-pot self-regulated approach to amide/peptide synthesis has been developed based on two redox reactions using azide as a latent amine component. For the first time, selenophenol, generated in situ has been found to be effecti
