Search Results - "Subasinghe, Nalin L."
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Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain
Published in Bioorganic & medicinal chemistry letters (15-12-2018)“…[Display omitted] •Optimized a novel series of pyrazoles as potent N-type calcium channel blockers.•Compounds 9 and 22 were orally bioavailable in…”
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A novel series of N-(azetidin-3-yl)-2-(heteroarylamino)acetamide CCR2 antagonists
Published in Bioorganic & medicinal chemistry letters (15-02-2013)“…The inflammatory response associated with the activation of C–C chemokine receptor CCR2 via it’s interaction with the monocyte chemoattractant protein-1…”
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A novel series of pyrazolylpiperidine N-type calcium channel blockers
Published in Bioorganic & medicinal chemistry letters (15-06-2012)“…Selective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered…”
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Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s
Published in Bioorganic & medicinal chemistry letters (15-08-2012)“…Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as…”
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Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s
Published in Bioorganic & medicinal chemistry (01-03-2008)“…Complement activation has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury, acute respiratory distress syndrome,…”
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A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s
Published in Bioorganic & medicinal chemistry letters (15-04-2006)“…Inhibiting the classical pathway of complement activation by attenuating the proteolytic activity of the serine protease C1s is a potential strategy for the…”
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A novel series of potent and selective small molecule inhibitors of the complement component C1s
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…Graphic Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and…”
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Design and Synthesis of 4,5-Disubstituted-thiophene-2-amidines as Potent Urokinase Inhibitors
Published in Bioorganic & medicinal chemistry letters (11-02-2002)“…A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of…”
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An efficient and high yield method for the N- tert-butoxycarbonyl protection of sterically hindered amino acids
Published in Tetrahedron letters (13-05-1996)“…An improved method for the N- tert-butoxycarbonyl protection of the amino functionality of α-alkylated prolines and other sterically hindered α,α-disubstituted…”
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Bicyclic thiazolidine lactam peptidomimetics of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2
Published in Journal of medicinal chemistry (06-08-1993)“…Bicyclic thiazolidine lactam peptidomimetics 3-5 have been synthesized as potential analogues of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2…”
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Structure-Based design, synthesis and sAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors
Published in Bioorganic & medicinal chemistry letters (04-06-2001)“…The serine protease urokinase plasminogen activator (uPA) is thought to play a central role in tumor metastasis and angiogenesis. Molecular modeling studies…”
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Stereospecific synthesis of 2-substituted bicyclic thiazolidine lactams
Published in Tetrahedron letters (24-02-1997)“…Bicyclic thiazolidine lactam 1 was used as a model system for developing synthetic methodology into β-turn mimics that would contain side chain functionality…”
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