Literature DB >> 1656043

New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.

A Monge1, I Aldana, T Alvarez, M Font, E Santiago, J A Latre, M J Bermejillo, M J Lopez-Unzu, E Fernandez-Alvarez.   

Abstract

Some fused 5H-pyridazino[4,5-b]indoles (7-10), substituted in positions 1 and 4 by hydrazine and/or amino groups, have been synthesized. These new compounds present a planar topography, a dipole with an adjacent acidic proton, and a basic hydrogen-acceptor site opposite the dipole. These compounds have some resemblance to carbazeram and other pyridazino agents with cardiotonic activity. Some of the new compounds here described possess inotropic activity (Table I and II), with a complementary effect as inhibitors of platelet aggregation (Table III and IV). 1-Hydrazino-4-(3,5-dimethyl)-1-pyrazolyl-5H-pyridazino[4,5-b ]indole hydrochloride (7a.HCl) is the first compound described in the literature with activities as inhibitor of PDE-IV and as selective inhibitor of TXA2 synthetase (Table V).

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Year:  1991        PMID: 1656043     DOI: 10.1021/jm00114a010

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  4 in total

Review 1.  Alkynoates as Versatile and Powerful Chemical Tools for the Rapid Assembly of Diverse Heterocycles under Transition-Metal Catalysis: Recent Developments and Challenges.

Authors:  Imtiaz Khan; Aliya Ibrar; Sumera Zaib
Journal:  Top Curr Chem (Cham)       Date:  2021-01-05

2.  3-Chloro-6-{4-[3-(4-chloro-phen-oxy)prop-yl]piperazin-1-yl}pyridazine.

Authors:  Hongliang Wang; Junhai Xiao; Xian Zhang; Tiemin Sun; Song Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-02-27

3.  Discovery of hydrazide-based pyridazino[4,5-b]indole scaffold as a new phosphoinositide 3-kinase (PI3K) inhibitor for breast cancer therapy.

Authors:  Ahmed A M Sarhan; Ahmed T A Boraei; Assem Barakat; Mohamed S Nafie
Journal:  RSC Adv       Date:  2020-05-21       Impact factor: 4.036

4.  Electrospray ionization-tandem mass spectrometric study of fused nitrogen-containing ring systems.

Authors:  Gábor Krajsovszky; Borbála Dalmadiné Kiss; Krisztina Ludányi; István M Mándity; Dóra Bogdán
Journal:  J Mass Spectrom       Date:  2022-06       Impact factor: 2.394

  4 in total

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