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Tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5- dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H +/K+-ATPase inhibitors

Amino acids are known to possess variable efficacy against ulceration. Considering the good antiulcer activity of amino acids, a series of urea/thiourea derivatives of glutamic acid conjugated benzisothiazole analogue 3a-u with various substituents on aryl ring were synthesized, spectroscopically characterized and evaluated for in vitro H+/K+-ATPase inhibition. Majority of the compounds possessed potency compared to that of omeprazole, a reference drug. In particular, methoxy derivatives 3p-u were the most active compounds possessing a significant 15-fold increase for para substituent thus, contributing positively to gastric H+/K +-ATPase inhibition.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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HETEROCYCLIC SUBSTITUTED INDANE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF SCHIZOPHRENIA

This invention relates to compounds of the formula (I) wherein J, M, G, m, X, R”, R2, R4, R5, R6, R7, R8, R9, Y, n, z, and R”” are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 87691-88-1, and how the biochemistry of the body works.category: isothiazole

Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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1,2,4-TRIAZOL-3-ONE ANTIDEPRESSANTS

Phenoxyalkyl substituted-1,2,4-triazolones having anti-depressant properties typified by 2-3-4-(3-chlorophenyl)-1-piperazinyl!propyl!-5-ethyl-4-(2-phenoxyethyl)-2H-1,2, 4-triazol-3(4H)-one are disclosed.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 3-Piperazinobenzisothiazole hydrochloride, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 87691-88-1, name is 3-Piperazinobenzisothiazole hydrochloride. In an article£¬Which mentioned a new discovery about 87691-88-1

Indole – aryl heterocyclic piperazine (acridine) derivatives and their use in anti-depression (by machine translation)

The invention discloses a indole – aryl heterocyclic piperazine (acridine) compound or its pharmaceutically acceptable salt, has the following structure: The compounds and compositions containing the same to the 5 – HT reuptake, 5 – HT1 A Receptor and 5 – HT7 Receptor has activity, it can be applied to the preparation of novel anti-depression drug. (by machine translation)

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Isothiazole – Wikipedia,
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Opioid Receptor Modulators with a Cinnamyl Group

To obtain selective and potent opioid receptor ligands, we synthesized dehydro derivatives of alvimopan and found compound (28f), a selective but modest affinity MOR antagonist weaker than alvimopan (1). We replaced the arylpiperidine unit by an arylpiperazine to obtain the 1-(alpha-carboxycinnamyl)-4-arylpiperazines like 13h, which to our surprise had no MOR or DOR activity but was a KOR agonist with moderate affinity. In contrast, literature examples of arylpiperazines 4 and 5 were reported to be pan opioid receptor antagonists, while 6 was a MOR agonist. Two compounds (13l and 11b) showed analgesic response in tail flick test which was blocked by pretreatment with norbinaltorphimine (norBNI). Among 10 1-(alpha-carboxycinnamyl)-4-arylpiperidines, compound 28g and five others were specific MOR antagonists. Interestingly, compound 26b of this series was found to be more potent than naloxone but weaker than 1. Docking studies have explained differential activities of the above piperazines and piperidines.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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CONDENSED THIOPHENE COMPOUND AND PHARMACEUTICAL USE THEREOF

A condensed thiophene compound represented by general formula: STR1 or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R 1 represents hydrogen, halogen, alkyl, etc.; R 2 represents hydrogen, alkyl, acyl, etc.; G represents–CH. sub.2–,–CH(OH)–,–CO–, etc.; Q represents alkylene; T represents–N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents–CH. sub. 2–or–S–; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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PRO-DRUGS OF 5-(2-(4-(1,2-BENZISOTHIAZOL-3-YL)-1-PIPERAZINYL)ETHYL)-6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE

The present invention relates to a pro-drug of ziprasidone or pharmaceutically acceptable salts thereof, processes for its preparation, and pharmaceutical compositions and methods of treatment comprising said pro-drug.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Application of 87691-88-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.87691-88-1, Name is 3-Piperazinobenzisothiazole hydrochloride, molecular formula is C11H14ClN3S. In a article£¬once mentioned of 87691-88-1

ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES

Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Scale gear heterocyclic derivatives and their application in the multi-target anti- depression (by machine translation)

The invention discloses a scale gear heterocyclic compound or its pharmaceutically acceptable salt, has the following structure, The compounds and compositions containing the same to the 5 – HT reuptake, 5 – HT1 A Receptor and 5 – HT7 Receptor has activity, it can be applied to the preparation of novel anti-depression drug. (by machine translation)

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 87691-88-1

Synthetic Route of 87691-88-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.87691-88-1, Name is 3-Piperazinobenzisothiazole hydrochloride, molecular formula is C11H14ClN3S. In a article£¬once mentioned of 87691-88-1

Tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5- dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H +/K+-ATPase inhibitors

Amino acids are known to possess variable efficacy against ulceration. Considering the good antiulcer activity of amino acids, a series of urea/thiourea derivatives of glutamic acid conjugated benzisothiazole analogue 3a-u with various substituents on aryl ring were synthesized, spectroscopically characterized and evaluated for in vitro H+/K+-ATPase inhibition. Majority of the compounds possessed potency compared to that of omeprazole, a reference drug. In particular, methoxy derivatives 3p-u were the most active compounds possessing a significant 15-fold increase for para substituent thus, contributing positively to gastric H+/K +-ATPase inhibition.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 87691-88-1

Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com