Structure of Tizanidine
CAS No.: 51322-75-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
Synonyms: Tizanidine
4.5
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Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives
Phelelisiwe S. Dube ; Dylan Hart ; Lesetja J. Legoabe ; Audrey Jordaan ; Digby F. Warner ; Richard M. Beteck
Abstract: Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis, which flourishes in varied environments with different oxygen concentrations. In this work, we investigated six nitrothiazole derivatives for antitubercular activity. The compounds exhibited potent activity, with compounds 9 and 10 possessing an equipotent MIC90 value of 0.24 µM. The compounds were investigated for cytotoxicity against HEK293 cells and hemolysis against red blood cells, and they demonstrated no cytotoxicity nor hemolytic effects, suggesting they possess inherent antitubercular activity.
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Keywords: nitrothiazole ; Mannich bases ; antitubercular activity ; tuberculosis ; Mycobacterium tuberculosis
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CAS No. : | 51322-75-9 |
Formula : | C9H8ClN5S |
M.W : | 253.71 |
SMILES Code : | ClC1=C(NC2=NCCN2)C3=NSN=C3C=C1 |
Synonyms : |
Tizanidine
|
MDL No. : | MFCD00865192 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H361 |
Precautionary Statements: | P201-P202-P264-P270-P280-P301+P312+P330-P308+P313-P220-P405-P501 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT02403687 | - | Completed | - | - | |
NCT01753882 | Spinal Cord Injury | Phase 1 | Unknown | July 2017 | United States, Illinois ... More >> Rehabilitation Institute of Chicago Chicago, Illinois, United States, 60611 Less << |
NCT01547234 | - | Completed | - | Israel ... More >> Multiple Sclerosis Center Carmel Medical Center Haifa, Israel Less << | |
NCT02853240 | Cerebral Palsy | Not Applicable | Recruiting | April 2020 | France ... More >> Hôpital Femme Mère Enfant Recruiting Bron, France, 69500 Contact: Claire MIETTON, MD (0)4 72 12 95 04 ext +33 claire.mietton@chu-lyon.fr Contact: Tiphanie GINHOUX, CRA (0)4 72 35 72 31 ext +33 tiphanie.ginhoux@chu-lyon.fr Less << |
NCT01788969 | Spinal Cord Injury | Phase 1 | Unknown | December 2017 | United States, Illinois ... More >> Rehabilitation Institute of Chicago Chicago, Illinois, United States, 60611 Less << |
NCT01244113 | Cerebral Palsy | Not Applicable | Completed | - | Korea, Republic of ... More >> Severance Hospital Seoul, Korea, Republic of, 120-752 Less << |
NCT02508805 | Vertebrogenic Radiculopathy L5... More >>, S1 Less << | Phase 3 | Completed | - | Russian Federation ... More >> State Autonomous Institution Republican Clinical Centre of Neurology Kazan, Republic of Tatarstan, Russian Federation, 420021 Less << |
NCT02887534 | Acute Muscle Pain | Phase 2 | Withdrawn | December 2017 | - |
NCT03068897 | Low Back Pain | Phase 4 | Completed | - | United States, New York ... More >> Montefiore Medical Center Bronx, New York, United States, 10467 Less << |
NCT02907775 | Muscle Spasticity ... More >> Stroke Less << | Not Applicable | Recruiting | November 30, 2018 | United Kingdom ... More >> Sheffield Teaching Hospitals NHS FT Recruiting Sheffield, United Kingdom Contact: Alisha Patel alisha.patel@sth.nhs.uk Less << |
NCT01068847 | Drug Dependence | Phase 1 | Completed | - | United States, Arkansas ... More >> University of Arkansas for Medical Sciences Little Rock, Arkansas, United States, 72205 Less << |
NCT00430196 | Upper Limb Spasticity | Phase 4 | Completed | - | - |
NCT00047580 | Multiple Sclerosis ... More >> Muscle Spasticity Spinal Cord Injury Stroke Less << | Phase 3 | Completed | - | United States, Arizona ... More >> Radiant Research Tucson, Arizona, United States, 85710 United States, California The Neurology Center Encinitas, California, United States, 92024 Northridge Neurological Center Northridge, California, United States, 91325 The Neurology Center Oceanside, California, United States, 92056 Neurology Medical Group of Diablo Valley Walnut Creek, California, United States, 94598 United States, Colorado Colorado Neurology Movement Disorders Center Englewood, Colorado, United States, 80110 United States, Connecticut Yale Center for MS Treatment and Research New Haven, Connecticut, United States, 06510 United States, Florida Neurology Clinic Research Institution Plantation, Florida, United States, 33324 Axiom Clinical Research Tampa, Florida, United States, 33609 United States, Georgia Comprehensive Neurology Specialists, PC Atlanta, Georgia, United States, 30338 Neurotrials Research, Inc. Atlanta, Georgia, United States, 30342 United States, Illinois Springfield Clinic Neuroscience Institute Springfield, Illinois, United States, 62702 United States, Minnesota The Minneapolis Clinic of Neurology, Ltd. Minneapolis, Minnesota, United States, 55422 United States, Oklahoma Neurological Associates of Tulsa, Inc. Tulsa, Oklahoma, United States, 74136-8327 United States, Oregon Medford Neurological and Spine Clinic Medford, Oregon, United States, 97504-8456 United States, Rhode Island Sargent Rehabilitation Center Warwick, Rhode Island, United States, 02818 Less << |
NCT01979510 | Low Back Pain | Phase 3 | Withdrawn | May 2014 | - |
NCT00287157 | Traumatic Brain Injury | Phase 1 | Completed | - | Israel ... More >> Alyn Hospital Pediatric and Adolescent Rehabilitation Center Jerusalem, Israel, 01090 Less << |
NCT02934061 | Low Back Pain | Phase 3 | Completed | - | Romania ... More >> Opera Contract Research Organization SRL Timisoara, Timis, Romania, 300209 Less << |
NCT00464958 | Spasticity Mu... More >>ltiple Sclerosis Less << | Phase 1 Phase 2 | Terminated(Study was stopped a... More >>s the sponsor is no longer funding this project) Less << | - | Israel ... More >> Tel Aviv Sourasky Medical Center Tel Aviv, Israel, 64239 Less << |
NCT02725359 | Thyroidectomy | Phase 4 | Completed | - | Turkey ... More >> Ataturk University Yakutiye, Erzurum, Turkey, 25100 Less << |
NCT01839279 | Spasticity | Phase 2 | Completed | - | United States, Texas ... More >> Covance- Dallas Dallas, Texas, United States, 75247 Less << |
NCT01844674 | Malignant Melanoma, Neoplasms | Phase 1 | Completed | - | United States, California ... More >> Diablo Valley Oncology and Hematology Pleasant Hill, California, United States, 94523 United States, Michigan Karmanos Cancer Center Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Health Systems Durham, North Carolina, United States, 27710 Brazil Instituto Nacional do Cancer - INCA Rio de Janeiro, RJ, Brazil, 20560-120 Hospital de Caridade de Ijui; Oncologia Ijui, RS, Brazil, 98700-000 CITO - Centro Integrado de Terapia Onco-Hematológica - Hospital da Cidade de Passo Fundo Passo Fundo, RS, Brazil, 99010-260 Hospital Sao Lucas - PUCRS Porto Alegre, RS, Brazil, 90610-000 Canada, Quebec CSSS champlain - Charles-Le Moyne Greenfield Park, Quebec, Canada, J4V 2H1 Cyprus Bank of Cyprus Oncology Center Nicosia, Cyprus, 2006 Korea, Republic of Severance Hospital, Yonsei University Health System Seoul, Korea, Republic of, 03722 Samsung Medical Center Seoul, Korea, Republic of, 06351 Asan Medical Center. Seoul, Korea, Republic of, 138-736 Less << |
NCT01405950 | Spasticity Due to Cerebral Pal... More >>sy Less << | Phase 1 | Terminated(Please see 'Further... More >> study details as provided by Acorda Therapeutics' for explanation of why study stopped.) Less << | - | United States, Kentucky ... More >> University of Louisville Department of Neurology dba Kentucky Neuroscience Research Health Care Outpatient Center (HCOC) Louisville, Kentucky, United States, 40202 Less << |
NCT01146028 | Healthy | PHASE1 | COMPLETED | 2025-11-01 | Anapharm Inc., Sainte-Foy (Que... More >>bec), Canada Less << |
NCT00358293 | Muscle Spasticity | Phase 1 Phase 2 | Completed | - | Israel ... More >> Tel Aviv Sourasky Medical Center- Neurology Department Tel Aviv, Israel Less << |
NCT01839279 | - | Completed | - | - | |
NCT02016443 | Unilateral Inguinal Hernia | Phase 4 | Completed | - | Turkey ... More >> Diskapi Yildirim Beyazit training and research hospital Ankara, Turkey Less << |
NCT01405950 | - | Terminated(Please see 'Further... More >> study details as provided by Acorda Therapeutics' for explanation of why study stopped.) Less << | - | - | |
NCT01065987 | Healthy | PHASE1 | COMPLETED | 2025-11-01 | Anapharm Inc., Sainte-Foy (Que... More >>bec), Canada Less << |
NCT06258785 | Postoperative Urinary Retentio... More >>n|Sacrospinous Vaginal Vault Suspension|Reconstructive Pelvic Surgery Less << | PHASE3 | RECRUITING | 2025-04-01 | NorthShore University Health S... More >>ystem, Skokie, Illinois, 60076, United States Less << |
Tags: Tizanidine | Adrenergic Receptor | Neuronal Signaling | GPCR/G Protein | Endocrinology/Hormones | 51322-75-9
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
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P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
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P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
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P370 + P378 | In case of fire: |
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P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
P371 + P380 + P375 | In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion. |
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H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
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H303 | May be harmful if swallowed |
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H311 | Toxic in contact with skin |
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H314 | Causes severe skin burns and eye damage |
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H320 | Causes eye irritation |
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H412 | Harmful to aquatic life with long-lasting effects |
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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