- Discovery of 5-(2-chloro-4′-(1H-imidazol-1-yl)-[1,1′-biphenyl]-4-yl)-1H-tetrazole as potent and orally efficacious S-nitrosoglutathione reductase (GSNOR) inhibitors for the potential treatment of COPD
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Endogenous nitrosothiols (SNOs) including S-nitrosoglutathione (GSNO) serve as reservoir for bioavailable nitric oxide (NO) and mediate NO-based signaling, inflammatory status and smooth muscle function in the lung. GSNOR inhibition increases pulmonary GS
- Muthukaman, Nagarajan,Deshmukh, Sanjay,Tondlekar, Shital,Tambe, Macchindra,Pisal, Dnyandeo,Sarode, Neelam,Mhatre, Siddharth,Chakraborti, Samitabh,Shah, Daisy,Bhosale, Vikram M.,Kulkarni, Abhay,Mahat, Mahamad Yunnus A.,Jadhav, Satyawan B.,Gudi, Girish S.,Khairatkar-Joshi, Neelima,Gharat, Laxmikant A.
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p. 3766 - 3773
(2018/10/20)
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- IMIDAZOLE BIARYL COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
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The present disclosure is directed to compounds of formula (Ie) and pharmaceutically acceptable salts thereof, wherein A, B, R1, R2, m, n, X1, X2, X3 and X4 are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).
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Page/Page column 75; 85; 86
(2016/04/20)
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- ALIPHATIC AMINO BIS-ARYL SQUALENE SYNTHASE INHIBITORS
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This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
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