Day: September 8, 2021

Electric Literature of 64987-08-2. Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 64987-08-2, Name is Ethyl 2-(2-aminothiazol-4-yl)-2-oxoacetate. In a document type is Patent, introducing its new discovery.

A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a beta-lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, (I) wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C1-6)alkylcarbonyloxy, (C1-6)alkoxycarbonyl, formyl or (C1-6)alkylcarbonyl group, (C3-7)cycloalkyl, (C3-7) cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7) cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CHR10)m¿X¿(CHR11)n, heterocyclyl or heterocyclyl-(CHR10)m¿X¿(CHR11)n, where m is 0 to 3, n is 1 to 3, each R10 and R11 is independently hydrogen or (C1-4)alkyl and X is O, S(O)x where x is 0-2, or a bond; R4 is hydrogen, or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)p where p is 2 to 5. Some compounds are claimed per se.

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Reference：
Thiazole | C3H7750NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 5304-21-2, Name is 6-Bromo-2-methylbenzo[d]thiazole,molecular formula is C8H6BrNS, is a conventional compound. this article was the specific content is as follows.category: thiazole

The invention relates to inhibitors of neutral endopeptidase enzyme (NEP), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of male and female sexual dysfunction, particularly female sexual dysfunction (FSD), especially wherein the FSD is female sexual arousal disorder (FSAD).

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Reference：
Thiazole | C3H6801NS – PubChem,
Thiazole | chemical compound | Britannica

Related Products of 38585-74-9, An article , which mentions 38585-74-9, molecular formula is C4H5NOS. The compound – Thiazol-5-ylmethanol played an important role in people’s production and life.

The human immunodeficiency virus (HIV) has been shown to be the causative agent for AIDS. The HIV virus encodes for a unique aspartyl protease that is essential for the production of enzymes and proteins in the final stages of maturation. Protease inhibitors have been useful in combating the disease. The inhibitors incorporate a variety of isosteres including the hydroxyethylurea at the protease cleavage site. We have shown that the replacement of t-butylurea moiety by benzothiazolesulfonamide provided inhibitors with improved potency and antiviral activities. Some of the compounds have shown good oral bioavailability and half-life in rats. The synthesis of benzothiazole derivatives led us to explore other heterocycles. During the course of our studies, we also developed an efficient synthesis of benzothiazole-6-sulfonic acid via a two-step procedure starting from sulfanilamide.

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Reference：
Thiazole | C3H9176NS – PubChem,
Thiazole | chemical compound | Britannica

Reference of 105827-91-6. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 105827-91-6, Name is 2-Chloro-5-(chloromethyl)thiazole

A cyano compound useful as an insecticide, of the formula (I) STR1 wherein R1 is hydrogen, cyano or C1-4 alkyl, m is 0 or 1, R2 is hydrogen, C1-6 alkyl, C3-4 alkenyl optionally substituted by halogen, C3-4 alkynyl, C3-8 cycloalkyl optionally substituted by methyl, optionally substituted phenyl, optionally substituted benzyl, hydroxy, C1-4 alkoxy or –CH2 –Z, in which Z has the same meanings as stated below, R3 is STR2 in which R4 is C1-6 alkyl, C3-4 alkenyl, C3-4 alkynyl, C3-8 cycloalkyl, optionally substituted phenyl, optionally substituted benzyl or –(CH2)n-Z, in which n is 1 or 2 and Z has the same meanings as stated below, and R5 and R6 are hydrogen, C1-9 alkyl optionally substituted by at least one selected from a group consisting of halogen, hydroxy, mercapto, C1-2 alkoxy, C1-2 alkylthio, C3-6 cycloalkyl, amino, C1-2 monoalkylamino, C2-4 (in total)di-alkylamino, carboxy, C1-2 alkoxy-carbonyl and cyano, C3-4 alkenyl optionally substituted by halogen, C3-4 alkynyl, optionally substituted phenyl, optionally substituted benzyl, C1-4 alkoxy, hydroxy, formyl, C1-4 alkoxy-carbonyl, C1-4 alkylamino, C2-4 (in total)di-alkylamino, amino, acyl or STR3 in which R1 and m have the same meanings as stated above, and Z has the same meanings as stated below, and in addition, R5 and R6 may form, together with the N-atom to which they are bonded, a 3 to 7 membered ring which may be substituted by C1-2 alkyl and may contain N, O or S as the member of said ring, besides the N-atom to which they are bonded, and Z is a substituted 5 or 6 membered heterocyclic group which contains at least one heteroatom selected from N, O and S as a ring member, provided that where Z is pyridyl substituted by halogen, m is 1, R2 is C1-6 alkyl and R3 is –S–alkyl(C1-6) or –S–benzyl, then R1 is cyano or C1-4 alkyl.

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Reference：
Thiazole | C3H2993NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 4175-77-3, Name is 2,4-Dibromothiazole,molecular formula is C3HBr2NS, is a conventional compound. this article was the specific content is as follows.SDS of cas: 4175-77-3

The present invention provides a compound having ALXR agonist activity. Specifically, the invention provides a compound having ALXR agonist activity represented by general formula (I) wherein all the symbols are as defined in the specification, a salt thereof, a solvate thereof, or a prodrug thereof as well as an agent containing the same as an active ingredient for preventing and/or treating an ALXR-associated disease, such as an inflammatory bowel disease, an autoimmune disease, a chronic inflammatory disease, asthma, pulmonary fibrosis, atopic dermatitis, ischemia-reperfusion injury, myocardial infarction, or Alzheimer’s disease.

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Reference：
Thiazole | C3H1302NS – PubChem,
Thiazole | chemical compound | Britannica

Electric Literature of 10200-59-6, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 10200-59-6, Name is 2-Thiazolecarboxaldehyde, molecular formula is C4H3NOS. In a Article，once mentioned of 10200-59-6

A new series of fifteen 5-, 6-, and 8-appended 4-methylquinolines were synthesized and evaluated for their neural protective activities. Selected compounds were further examined for their inhibition of glycogen synthase kinase-3beta (GSK-3beta) and protein kinase C (PKC). Two most potent analogs, compounds 3 and 10, show nanomolar protective activities in amyloid beta-induced MC65 cells and enzymatic inhibitory activities against GSK-3beta, but poor PKC inhibitory activities. Using normal mouse model, the distribution of the most potent analog 3 in various tissues and possible toxic effects in the locomotors and inhibition of liver transaminases activities were carried out. No apparent decline of locomotor activity and no inhibition of liver transaminases were found. The compound appears to be safe for long-term use in Alzheimer’s disease mouse model.

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Reference：
Thiazole | C3H4480NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 202932-04-5, Name is 5-Methyl-2-thiazolemethanol,molecular formula is C5H7NOS, is a conventional compound. this article was the specific content is as follows.Product Details of 202932-04-5

We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4- triazolo[3,4-a]phthalazine (1) as a potent partial agonist for the 0.3 receptor subtype with 5-fold selectivity in binding affinity over alpha1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the alpha3 subtype over the alpha1 subtype was 12-fold (for 57). Although most analogues showed no selectivity in terms of efficacy, some did show partial agonism at alpha1 and antagonism at alpha3 (e.g., 25 and 75). However, two analogues tested (93 and 96), both with triazole substituents in the 6-position, showed significantly higher efficacy for the alpha3 subtype over the alpha1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.

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Reference：
Thiazole | C3H6467NS – PubChem,
Thiazole | chemical compound | Britannica

Application of 38585-74-9, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 38585-74-9, Name is Thiazol-5-ylmethanol, molecular formula is C4H5NOS. In a Article，once mentioned of 38585-74-9

Reduced cognitive abilities are often characterized by an impairment of flexibility, i.e., the ability to switch from learned rules or categories that were important in certain contexts to different new modalities that rule the task. Drugs targeting the dopamine transporter (DAT) are widely used for their potential to enhance cognitive abilities. However, commercially available drugs are of limited specificity for DAT, blocking also noradrenaline and serotonine transporters, that can lead to unwanted side effects in healthy subjects. Therefore, we tested a newly synthetized compound (CE-123) with higher specificity for DAT in male rats in an attentional set-shifting task (ASST), that proves for cognitive flexibility and a 5-choice serial-reaction time task (5-CSRTT) assessing visuospatial attention and impulsivity. Treated rats at a dose of 0.3 and 1.0 but not 0.1 mg/kg bodyweight showed reduced extra-dimensional shifts in the ASST compared to controls indicating increased cognitive flexibility. Rats treated with R-Modafinil, a commercially available DAT inhibitor at a dose of 10 mg/kg bodyweight showed increased premature responses, an indicator of increased impulsivity, during a 10 s but not a 2.5, 5, or 7.5 s intertrial interval when compared to vehicle-treated rats in the 5-CSRTT. This was not found in rats treated with CE-123 at the same dose as for R-Modafinil. Visuospatial attention, except premature responses, did not differ between R-Modafinil and CE-123-treated rats and their respective controls. Thus, CE-123 increased cognitive flexibility with diminished impulsivity.

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Reference：
Thiazole | C3H9185NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 18640-74-9, Name is 2-Isobutylthiazole,molecular formula is C7H11NS, is a conventional compound. this article was the specific content is as follows.name: 2-Isobutylthiazole

A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of p38 kinase.

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Reference：
Thiazole | C3H3469NS – PubChem,
Thiazole | chemical compound | Britannica

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.82294-70-0, Name is 4-Methylthiazole-5-carbaldehyde, molecular formula is C5H5NOS. In a Patent，once mentioned of 82294-70-0, Product Details of 82294-70-0

The present invention relates to crystalline intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins and processes for their preparation. In particular, the present invention relates to crystalline ylides of Formula I, processes for their preparation, and their use as an intermediate in thepreparation of 3-(2-substituted vinyl) cephalosporins.

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Reference：
Thiazole | C3H5715NS – PubChem,
Thiazole | chemical compound | Britannica