Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-Naphthyridine Derivatives as an H1-receptor Inhibitor Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-Naphthyridine Derivatives as an H1-receptor Inhibitor

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Dr. Dilipkumar Pal

Abstract

In the present study, 1,8-naphthyridine-3-carboxylic acid derivatives (5a1, 5a2, 5b1, and 5b2) were
designed, synthesized, and screened for their in vitro H1-antihistaminic activity. H1R inhibitory activity
of the synthesized derivatives was calculated by the modified Van Arman technique, histamine-induced
bronchoconstriction in guinea pigs. A good bronchorelaxant effect of compounds was observed in
histamine-contracted guinea pig tracheal chain through H1-receptor antagonism. In addition, the
hypothetically resulted compounds are checked for their reliability on other in silico drug designing
online web services like SwissADME predictor. In silico ADMET analysis results show that all the
derivatives had negligible toxicity, good absorption, and solubility profile. These compounds may serve
as possible lead for establishing safe and effective antihistaminic agent(s).

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How to Cite
Pal, D. D. (2019). Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-Naphthyridine Derivatives as an H1-receptor Inhibitor: Design, Synthesis, Biological Evaluation, and In Silico ADMET Studies of 1,8-Naphthyridine Derivatives as an H1-receptor Inhibitor. International Journal of Pharmaceutical & Biological Archive, 9(04). https://doi.org/10.22377/ijpba.v9i04.1735
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Research Articles