2,1-Benzothiazine – (quinolin/thiophen)yl hydrazone frameworks as new monoamine oxidase inhibitory agents; synthesis, <i>in vitro</i> and <i>in silico</i> investigation

Javid, Noman; Jalil, Saquib; Munir, Rubina; Zia‐ur‐Rehman, Muhammad; Sahar, Amna; Arshad, Sara; Iqbal, Jamshed

doi:10.1039/d2ra07045f

Cited by 6 publications

(2 citation statements)

References 33 publications

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“…Over the last decade, there has been a rapid increase in CADD-based studies of depression, including docking studies of ligands for serotonin reuptake [171,172], MAO A and MAO B [173,174], dual action on MAO-B/AChE [175], glycogen synthase kinase [176], sodium hNaV1.2 or hNaV1.7 channels [177], serotonin receptors (5HT1A, 5-HT2A, 5-HT2C and 5-HT4) [171,[178][179][180][181], adenosine A1/A2A receptors [182], T-type calcium channels [183], tryptophan 2,3-dioxygenase [184] and sigma receptor [185]. Similarly, application of docking in psychoses involved ligands for serotonin 5HT2 and dopamine D2 receptors [186], α4β2 and α7 nicotinic acetylcholine receptors [187,188], phosphodiesterase 10A [189], MAO A and B [190], a syntaxin-binding protein (STXBP1) [191], NMDA type subunit 1 (GRIN1) [192], fatty acid binding protein 7 (FABP7) [193,194], metabotropic glutamate mGluR5 receptor [195], ionotropic GABA-A receptor [196], glycine transporter type 1 (GlyT1) [197] and kynurenine aminotransferase II (KATII) [198].…”

Section: In Silico-driven Search For Novel Therapeutic Agentsmentioning

confidence: 99%

Towards Novel Potential Molecular Targets for Antidepressant and Antipsychotic Pharmacotherapies

Kositsyn

Abreu

Колесникова

et al. 2023

IJMS

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Depression and schizophrenia are two highly prevalent and severely debilitating neuropsychiatric disorders. Both conventional antidepressant and antipsychotic pharmacotherapies are often inefficient clinically, causing multiple side effects and serious patient compliance problems. Collectively, this calls for the development of novel drug targets for treating depressed and schizophrenic patients. Here, we discuss recent translational advances, research tools and approaches, aiming to facilitate innovative drug discovery in this field. Providing a comprehensive overview of current antidepressants and antipsychotic drugs, we also outline potential novel molecular targets for treating depression and schizophrenia. We also critically evaluate multiple translational challenges and summarize various open questions, in order to foster further integrative cross-discipline research into antidepressant and antipsychotic drug development.

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Section: In Silico-driven Search For Novel Therapeutic Agentsmentioning

confidence: 99%

Towards Novel Potential Molecular Targets for Antidepressant and Antipsychotic Pharmacotherapies

Kositsyn

Abreu

Колесникова

et al. 2023

IJMS

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show abstract

“…In this regard, a renowned anti-urease pharmacophore phenylacetamide was incorporated into the benzothiazine ring. Hence, continuing our previous work to explore new biologically active compounds [49][50][51][52][53][54], we herein present the synthesis and evaluation of the pharmacological potential of a series of new methyl 1,2-benzothiazine-N-arylacetamide derivatives against urease enzyme. The prepared compounds were subjected to characterization through nuclear magnetic resonance spectroscopy ( proton and carbon) as well as mass spectrometry.…”

Section: Introductionmentioning

confidence: 99%

N -Arylacetamide derivatives of methyl 1,2-benzothiazine-3-carboxylate as potential drug candidates for urease inhibition

et al. 2023

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Urease enzyme is an infectious factor that provokes the growth and colonization of virulence pathogenic bacteria in humans. To overcome the deleterious effects of bacterial infections, inhibition of urease enzyme is one of the promising approaches. The current study is designed to synthesize new 1,2-benzothiazine- N -arylacetamide derivatives 5 ( a-n ) that can effectively provide a new drug candidate to avoid bacterial infections by urease inhibition. After structural elucidation by FT-IR, proton and carbon-13 NMR and mass spectroscopy, the synthesized compounds 5 ( a-n ) were investigated to evaluate their inhibitory potential against urease enzyme. In vitro analysis against positive control of thiourea indicated that all the synthesized compounds have strong inhibitory strengths as compared to the reference drug. Compound 5k , being the most potent inhibitor, strongly inhibited the urease enzymes and revealed an IC 50 value of 9.8 ± 0.023 µM when compared with the IC 50 of thiourea (22.3 ± 0.031 µM)—a far more robust inhibitory potential. Docking studies of 5k within the urease active site revealed various significant interactions such as H-bond, π-alkyl with amino acid residues like Val744, Lys716, Ala16, Glu7452, Ala37 and Asp730.

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In vitro/in vivo effects of some new 2,5-disubstituted 1,3,4-oxadiazole and hydrazone analogues targeting Parkinson's disease

Karabelyov,

Angelova,

Sharkov

et al. 2023

Journal of Molecular Structure

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2,1-Benzothiazine – (quinolin/thiophen)yl hydrazone frameworks as new monoamine oxidase inhibitory agents; synthesis, in vitro and in silico investigation

Abstract: Two series of new 2,1-benzothiazine-heteroaryl ethylidene derivatives 7(a–f) and 9(a–k) have been synthesized in excellent yields and tested against MAOs.

Cited by 6 publications

References 33 publications

Towards Novel Potential Molecular Targets for Antidepressant and Antipsychotic Pharmacotherapies

Towards Novel Potential Molecular Targets for Antidepressant and Antipsychotic Pharmacotherapies

N -Arylacetamide derivatives of methyl 1,2-benzothiazine-3-carboxylate as potential drug candidates for urease inhibition

In vitro/in vivo effects of some new 2,5-disubstituted 1,3,4-oxadiazole and hydrazone analogues targeting Parkinson's disease

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