- Structure-Based Rationale Design and Synthesis of Aurantiamide Acetate Analogues - Towards a New Class of Potent Analgesic and Anti-inflammatory Agents
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A series of new aurantiamide acetate analogues were synthesized by modifying its N-terminal substitution and the amino acid residue. The structure of all these compounds was established on the basis of analytical and spectral studies. All the new derivatives were evaluated in vivo for their analgesic activity by tail flick method in mice and anti-inflammatory activity against carrageenan-induced oedema in albino rats at different doses (25, 50 and 100mg/kg body weight). All the compounds exhibited significant pharmacological activity with no ulcerogenic liability. In particular, pentapeptides and tricosamers (30 amino acids) containing analogues have demonstrated high potency than the reference standards. These compounds hold promise for further development.
- Suhas, Ramesh,Channe Gowda, Dase
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p. 850 - 862
(2012/06/04)
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- Design and synthesis of tryptophan containing peptides as potential analgesic and anti-inflammatory agents
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A new series of smaller peptides with tryptophan at C-terminal and varying N-protected amino acids/peptides were designed, synthesized and characterized by analytical and spectroscopic techniques. Analgesic and anti-inflammatory properties of these peptides were carried out in vivo using tail-flick method and carrageenan-induced paw edema method, respectively, at different doses and different time intervals. Most of the peptides synthesized displayed enhanced activity, and particularly tetra and hexapeptides 29-31 were found to be even more potent than the reference standards used. Moreover, some peptides have exhibited promising activity even after 24h of administration, whereas the reference standards were active only up to 3h. Further, the compounds did not present any ulcerogenic liability.
- Suhas,Gowda, D.Channe
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p. 535 - 540
(2012/09/22)
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- A new family of highly potent inhibitors of microbes: Synthesis and conjugation of elastin based peptides to piperazine derivative
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Elastin protein-based polymers have their origin in repeating sequences of the mammalian elastic protein, elastin. The sequences of elastin peptides chosen are tetrapeptides, pentapeptides and tricosamers (30 amino acids) and also aromatic amino acids. Th
- Suhas,Chandrashekar,Gowda, D. Channe
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experimental part
p. 89 - 98
(2012/09/05)
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- Synthesis of elastin based peptides conjugated to benzisoxazole as a new class of potent antimicrobials - A novel approach to enhance biocompatibility
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The peptides of elastin sequences chosen for the present study included tetrapeptides, pentapeptides and tricosapeptides (30 amino acids), synthesized by classical solution phase method and conjugated to [3-(4-piperidyl)-6-fluoro- 1,2-benzisoxazole]. The
- Suhas,Chandrashekar,Gowda, D. Channe
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p. 704 - 711
(2011/03/22)
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