title: Implication of novel thiazolo-thiophene derivative (MCD-KV-10) for management of asthma.
abstract: BACKGROUND
  Asthma is multifaceted disease where many targets contribute towards its development and progression. Among these, adenosine receptor subtypes play a major role.
  
  
  OBJECTIVE
  MCD-KV-10, a novel thiazolo-thiophene was designed and evaluated pre-clinically for its implication in management of asthma.
  
  
  METHODS
  This compound showed good affinity and selectivity towards A(2A)/A3 adenosine receptor (AR) subtypes. Furthermore, MCD-KV-10 was evaluated for in vitro lipoxygenase inhibition activity; in vivo mast cell stabilization potential and in vivo anti-asthmatic activity was done in ovalbumin-induced airway inflammation model in guinea pigs.
  
  
  RESULTS
  The compound showed good (>57%) inhibition of lipoxygenase enzyme and also effectively protected mast cell degranulation (>63%). The compound showed good anti-asthmatic activity as inferred from the in vivo studies.
  
  
  CONCLUSIONS
  These results indicate that MCD-KV-10 has an inhibitory effect on airway inflammation.
  
  
  CONCLUSIONS
  Though, we have identified a potential candidate for management of asthma, further mechanistic studies are needed.
authors.affiliation: Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research - Ahmedabad, C/O - B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre , S. G. Highway, Thaltej, Ahmedabad, Gujarat , India .
authors.forename: Dhiraj
authors.initials: D
authors.lastname: Patil
authors.forename: Ranjeet Prasad
authors.initials: RP
authors.lastname: Dash
authors.forename: Sandeep Kumar
authors.initials: SK
authors.lastname: Thakur
authors.forename: Amit N
authors.initials: AN
authors.lastname: Pandya
authors.forename: P
authors.initials: P
authors.lastname: Venkatesh
authors.forename: Kamala K
authors.initials: KK
authors.lastname: Vasu
authors.forename: Manish
authors.initials: M
authors.lastname: Nivsarkar
mesh_terms: D000818:Animals; D018927:Anti-Asthmatic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001249:Asthma / Q000188:drug therapy* / Q000276:immunology / Q000378:metabolism / Q000473:pathology; D016207:Cytokines / Q000097:blood; D006168:Guinea Pigs; D006632:Histamine / Q000378:metabolism; D058945:Lipoxygenases / Q000378:metabolism; D008168:Lung / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D008297:Male; D008407:Mast Cells / Q000187:drug effects; D015394:Molecular Structure; D010047:Ovalbumin / Q000276:immunology; D058915:Purinergic P1 Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D043705:Receptor, Adenosine A2A / Q000378:metabolism; D043684:Receptor, Adenosine A3 / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D018927:Anti-Asthmatic Agents; D016207:Cytokines; C000604111:MCD-KV-10; D058915:Purinergic P1 Receptor Antagonists; D043705:Receptor, Adenosine A2A; D043684:Receptor, Adenosine A3; D013844:Thiazoles; D013876:Thiophenes; D006632:Histamine; D010047:Ovalbumin; D058945:Lipoxygenases
keywords: Adenosine; asthma; cytokines; lipoxygenase; thiazolo-thiophene