From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies

The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to tre...
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Autor*in:	Serge Mignani [verfasserIn] Jean-Pierre Majoral [verfasserIn] Jean-François Desaphy [verfasserIn] Giovanni Lentini [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2020

Schlagwörter:	riluzole amyotrophic lateral sclerosis (ALS) dexpramipexole 1,3-benzothiazole (BTZ) indoles DrugBank

Übergeordnetes Werk:	In: Molecules - MDPI AG, 2003, 25(2020), 15, p 3320
Übergeordnetes Werk:	volume:25 ; year:2020 ; number:15, p 3320

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/molecules25153320

Katalog-ID:	DOAJ040697606

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allfieldsGer	10.3390/molecules25153320 doi (DE-627)DOAJ040697606 (DE-599)DOAJcbf575459d1845c3b8f0384a53c18374 DE-627 ger DE-627 rakwb eng QD241-441 Serge Mignani verfasserin aut From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to treat amyotrophic lateral sclerosis (ALS) but its efficacy is marginal. Several clinical studies have demonstrated only limited improvements in survival, without benefits to motor function in patients with ALS. Despite significant clinical trial efforts to understand the genetic, epigenetic, and molecular pathways linked to ALS pathophysiology, therapeutic translation has remained disappointingly slow, probably due to the complexity and the heterogeneity of this disease. Many other drugs to tackle ALS have been tested for 20 years without any success. Dexpramipexole is a BTZ structural analog of riluzole and was a great hope for the treatment of ALS. In this review, as an interesting case study in the development of a new medicine to treat ALS, we present the strategy of the development of dexpramipexole, which was one of the most promising drugs against ALS. riluzole amyotrophic lateral sclerosis (ALS) dexpramipexole 1,3-benzothiazole (BTZ) indoles DrugBank Organic chemistry Jean-Pierre Majoral verfasserin aut Jean-François Desaphy verfasserin aut Giovanni Lentini verfasserin aut In Molecules MDPI AG, 2003 25(2020), 15, p 3320 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:15, p 3320 https://doi.org/10.3390/molecules25153320 kostenfrei https://doaj.org/article/cbf575459d1845c3b8f0384a53c18374 kostenfrei https://www.mdpi.com/1420-3049/25/15/3320 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 15, p 3320
allfieldsSound	10.3390/molecules25153320 doi (DE-627)DOAJ040697606 (DE-599)DOAJcbf575459d1845c3b8f0384a53c18374 DE-627 ger DE-627 rakwb eng QD241-441 Serge Mignani verfasserin aut From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to treat amyotrophic lateral sclerosis (ALS) but its efficacy is marginal. Several clinical studies have demonstrated only limited improvements in survival, without benefits to motor function in patients with ALS. Despite significant clinical trial efforts to understand the genetic, epigenetic, and molecular pathways linked to ALS pathophysiology, therapeutic translation has remained disappointingly slow, probably due to the complexity and the heterogeneity of this disease. Many other drugs to tackle ALS have been tested for 20 years without any success. Dexpramipexole is a BTZ structural analog of riluzole and was a great hope for the treatment of ALS. In this review, as an interesting case study in the development of a new medicine to treat ALS, we present the strategy of the development of dexpramipexole, which was one of the most promising drugs against ALS. riluzole amyotrophic lateral sclerosis (ALS) dexpramipexole 1,3-benzothiazole (BTZ) indoles DrugBank Organic chemistry Jean-Pierre Majoral verfasserin aut Jean-François Desaphy verfasserin aut Giovanni Lentini verfasserin aut In Molecules MDPI AG, 2003 25(2020), 15, p 3320 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:15, p 3320 https://doi.org/10.3390/molecules25153320 kostenfrei https://doaj.org/article/cbf575459d1845c3b8f0384a53c18374 kostenfrei https://www.mdpi.com/1420-3049/25/15/3320 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 15, p 3320
language	English
source	In Molecules 25(2020), 15, p 3320 volume:25 year:2020 number:15, p 3320
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topic_facet	riluzole amyotrophic lateral sclerosis (ALS) dexpramipexole 1,3-benzothiazole (BTZ) indoles DrugBank Organic chemistry
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container_title	Molecules
authorswithroles_txt_mv	Serge Mignani @@aut@@ Jean-Pierre Majoral @@aut@@ Jean-François Desaphy @@aut@@ Giovanni Lentini @@aut@@
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callnumber-first	Q - Science
author	Serge Mignani
spellingShingle	Serge Mignani misc QD241-441 misc riluzole misc amyotrophic lateral sclerosis (ALS) misc dexpramipexole misc 1,3-benzothiazole (BTZ) misc indoles misc DrugBank misc Organic chemistry From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies
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topic_title	QD241-441 From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies riluzole amyotrophic lateral sclerosis (ALS) dexpramipexole 1,3-benzothiazole (BTZ) indoles DrugBank
topic	misc QD241-441 misc riluzole misc amyotrophic lateral sclerosis (ALS) misc dexpramipexole misc 1,3-benzothiazole (BTZ) misc indoles misc DrugBank misc Organic chemistry
topic_unstemmed	misc QD241-441 misc riluzole misc amyotrophic lateral sclerosis (ALS) misc dexpramipexole misc 1,3-benzothiazole (BTZ) misc indoles misc DrugBank misc Organic chemistry
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title	From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies
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title_full	From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies
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title_sort	from riluzole to dexpramipexole via substituted-benzothiazole derivatives for amyotrophic lateral sclerosis disease treatment: case studies
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title_auth	From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies
abstract	The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to treat amyotrophic lateral sclerosis (ALS) but its efficacy is marginal. Several clinical studies have demonstrated only limited improvements in survival, without benefits to motor function in patients with ALS. Despite significant clinical trial efforts to understand the genetic, epigenetic, and molecular pathways linked to ALS pathophysiology, therapeutic translation has remained disappointingly slow, probably due to the complexity and the heterogeneity of this disease. Many other drugs to tackle ALS have been tested for 20 years without any success. Dexpramipexole is a BTZ structural analog of riluzole and was a great hope for the treatment of ALS. In this review, as an interesting case study in the development of a new medicine to treat ALS, we present the strategy of the development of dexpramipexole, which was one of the most promising drugs against ALS.
abstractGer	The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to treat amyotrophic lateral sclerosis (ALS) but its efficacy is marginal. Several clinical studies have demonstrated only limited improvements in survival, without benefits to motor function in patients with ALS. Despite significant clinical trial efforts to understand the genetic, epigenetic, and molecular pathways linked to ALS pathophysiology, therapeutic translation has remained disappointingly slow, probably due to the complexity and the heterogeneity of this disease. Many other drugs to tackle ALS have been tested for 20 years without any success. Dexpramipexole is a BTZ structural analog of riluzole and was a great hope for the treatment of ALS. In this review, as an interesting case study in the development of a new medicine to treat ALS, we present the strategy of the development of dexpramipexole, which was one of the most promising drugs against ALS.
abstract_unstemmed	The 1,3-benzothiazole (BTZ) ring may offer a valid option for scaffold-hopping from indole derivatives. Several BTZs have clinically relevant roles, mainly as CNS medicines and diagnostic agents, with riluzole being one of the most famous examples. Riluzole is currently the only approved drug to treat amyotrophic lateral sclerosis (ALS) but its efficacy is marginal. Several clinical studies have demonstrated only limited improvements in survival, without benefits to motor function in patients with ALS. Despite significant clinical trial efforts to understand the genetic, epigenetic, and molecular pathways linked to ALS pathophysiology, therapeutic translation has remained disappointingly slow, probably due to the complexity and the heterogeneity of this disease. Many other drugs to tackle ALS have been tested for 20 years without any success. Dexpramipexole is a BTZ structural analog of riluzole and was a great hope for the treatment of ALS. In this review, as an interesting case study in the development of a new medicine to treat ALS, we present the strategy of the development of dexpramipexole, which was one of the most promising drugs against ALS.
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title_short	From Riluzole to Dexpramipexole via Substituted-Benzothiazole Derivatives for Amyotrophic Lateral Sclerosis Disease Treatment: Case Studies
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