Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

Kamal, Aehmed; Reddy, K. Laxma; Devaiah,; Shankaraiah, N.; Rao, Mandava V. Basaveswara

doi:10.2174/138955706775197839

Cited by 69 publications

(27 citation statements)

References 99 publications

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“…Furthermore, some reports on the solid-phase synthesis of this class of compounds has been recently reviewed by Kamal et al [159]. Several heterocyclic compounds, as furanones, oxazoles, benzoindoles and benzothiopyranes variously substituted, have been condensed with 1,2-diaminobenzenes to afford in good yield interesting quinoxalinone derivatives (Fig.…”

Section: Preparations Of Quinoxalin-2-onesmentioning

confidence: 99%

Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

Carta

Piras²,

Loriga

et al. 2006

MRMC

221

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Quinoxaline derivatives have received much attention in recent years owing to their both biological properties and pharmaceutical applications. In this review we focus the attention on quinoxalin-2(3)-ones and quinoxalin-2,3-diones. These derivatives are particularly interesting since some of them showed antimicrobial (against several bacteria, viruses, fungi, etc), or anticancer activities. Furthermore, others are reported to be potent no-NMDA glutamate receptor antagonists, endowed with anxiolytic, deconditioning, analgesic, antispastic, antiallergic, antithrombotic activities. In this article we also report SAR studies and the most important methods of synthesis of the quinoxalin-2(3)-(di)ones.

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Section: Preparations Of Quinoxalin-2-onesmentioning

confidence: 99%

Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

Carta

Piras²,

Loriga

et al. 2006

MRMC

221

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“…Rho kinase augments contraction by inhibiting myosin light chain phosphatase (MLCP), a process referred to as “calcium sensitization”. The role of Rho kinase in ASM contraction has been well documented (Gosens, et al, 2006). Rho kinase inhibitors have been shown to inhibit ASM contraction both ex vivo (including human tissues) (Gosens, et al, 2004a; Gosens, et al, 2004b; Iizuka, et al, 1999; Schaafsma, et al, 2005; Yoshii, et al, 1999) and in vivo (animals) (Iizuka, et al, 2000; Tokuyama, et al, 2002).…”

Section: Not-so-new Targets But With New Lifementioning

confidence: 99%

Bronchoprotection and bronchorelaxation in asthma: New targets, and new ways to target the old ones

Pera

Penn

2016

Pharmacology & Therapeutics

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Despite over 50 years of inhaled beta-agonists and corticosteroids as the default management or rescue drugs for asthma, recent research suggests that new therapeutic options are likely to emerge. This belief stems from both an improved understanding of what causes and regulates airway smooth muscle (ASM) contraction, and the identification of new targets whose inhibition or activation can relax ASM. In this review we discuss the recent findings that provide new insight into ASM contractile regulation, a revolution in pharmacology that identifies new ways to “tune” G protein-coupled receptors to improve therapeutic efficacy, and the discovery of several novel targets/approaches capable of effecting bronchoprotection or bronchodilation.

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“…Properly substituted 2,4-diaminoquinazolines have been labeled as privileged substructures and they are protonated at a physiological pH (Bordner et al, 1988). Numerous quinazoline-based libraries have been developed, and have provided useful ligands for receptor and enzymatic targets (Kamal et al, 2006), also in the field of antiparasitics (Davoll et al, 1972). On these bases, a series of 2-piperazin-1-yl-quinazolin-4-ylamine derivatives (11-17 in Table 1) were, for the first time, designed and tested against TR.…”

Section: Lead Discovery Cyclementioning

confidence: 99%

Complementary medicinal chemistry-driven strategies toward new antitrypanosomal and antileishmanial lead drug candidates

Cavalli

Lizzi

Bongarzone

et al. 2010

FEMS Immunology &Amp; Medical Microbiology

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Trypanosomiases and Leishmaniases are neglected tropical diseases that affect the less developed countries. For this reason, they did not and still do not have high visibility in Western societies. The name neglected diseases also refers to the fact that they often received little interest at the level of public investment, research and development. The drug discovery scenario, however, is changing dramatically. After a period in which different socioeconomic factors have prevented massive research efforts in this field, such efforts have increased considerably in the very recent years, with significant scientific advancements. In this context, we have embarked on a new drug discovery project devoted to identification of new small molecules for the treatment of trypanosomal and leishmanial diseases. Two complementary approaches have been pursued and are reported here. The first deals with a structure-based drug design, and a privileged structure-guided synthesis of quinazoline compounds able to modulate trypanothione reductase activity was accomplished. In the second, a combinatorial library, built on a natural product-based strategy, was synthesized. Using whole parasite assays, different quinones have been identified as promising lead compounds. A combination of both approaches to hopefully overcome some of the challenges of anti-trypanosomatid drug discovery has eventually been proposed.

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Recent Advances in the Solid-Phase Combinatorial Synthetic Strategies for the Quinoxaline, Quinazoline and Benzimidazole Based Privileged Structures

Cited by 69 publications

References 99 publications

Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

Chemistry, Biological Properties and SAR Analysis of Quinoxalinones

Bronchoprotection and bronchorelaxation in asthma: New targets, and new ways to target the old ones

Complementary medicinal chemistry-driven strategies toward new antitrypanosomal and antileishmanial lead drug candidates

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