Category: 54346-19-9

Kobe, Joze; Robins, Roland K.; O’Brien, Darrell E. published the artcile< Synthesis and chemical reactions of certain pyrazolo[1,5-a]-1,3,5-triaziness>, Product Details of C6H5ClN4S, the main research area is pyrazolotriazine; adenine analog pyrazolotriazine; hypoxanthine analog pyrazolotriazine; xanthine analog pyrazolotriazine; substitution pyrazolotriazine.

3-Aminopyrazole was used to prepare pyrazolo[1,5-a]-1,3,5-triazines. 4-Chloro-2-methylthiopyrazolo[1,5-a]-1,3,5-triazine was prepared and used for studies of nucleophilic displacement reactions; both the Cl and MeS groups may be displaced by nucleophiles. Adenine, hypoxanthine, and xanthine analogs of the pyrazolo[1,5-a]-1,3,5-triazine ring were prepared similarly. Electrophilic substitution occurs at C-8. The Me group was introduced at C-4 by a novel ring opening and closing of the triazine ring.

Journal of Heterocyclic Chemistry published new progress about Substitution reaction. 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Product Details of C6H5ClN4S.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Kobe, Joze; Robins, Roland K.; O’Brien, Darrell E. published the artcile< Synthesis and chemical reactions of certain pyrazolo[1,5-a]-1,3,5-triaziness>, Product Details of C6H5ClN4S, the main research area is pyrazolotriazine; adenine analog pyrazolotriazine; hypoxanthine analog pyrazolotriazine; xanthine analog pyrazolotriazine; substitution pyrazolotriazine.

3-Aminopyrazole was used to prepare pyrazolo[1,5-a]-1,3,5-triazines. 4-Chloro-2-methylthiopyrazolo[1,5-a]-1,3,5-triazine was prepared and used for studies of nucleophilic displacement reactions; both the Cl and MeS groups may be displaced by nucleophiles. Adenine, hypoxanthine, and xanthine analogs of the pyrazolo[1,5-a]-1,3,5-triazine ring were prepared similarly. Electrophilic substitution occurs at C-8. The Me group was introduced at C-4 by a novel ring opening and closing of the triazine ring.

Journal of Heterocyclic Chemistry published new progress about Substitution reaction. 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Product Details of C6H5ClN4S.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elie, Jonathan; Fruit, Corinne; Besson, Thierry published the artcile< Microwave-assisted sequential one-pot synthesis of 8-substituted pyrazolo[1,5-a][1,3,5]triazines>, Application of C6H5ClN4S, the main research area is aminopyrazole ethoxycarbonyl isothiocyanate microwave assisted heterocyclization; methylsulfanyl pyrazolotriazinone preparation; 5-aza-9-deazapurines; microwave-assisted chemistry; one-pot synthesis; pyrazolo[1,5-a][1,3,5]triazines.

A convenient sequential one-pot approach for the synthesis of an array of 14 pyrazolo[1,5-a][1,3,5]triazines, I [R = H, Br, CN, etc] substituted in C8 by halogen (Br), various functions (CN and CO2Et) and alkyl or (het)aryl groups was reported. This study confirmed the interest of combining the efficient heating obtained under dielec. microwave heating and the achievement of sequential one-pot reactions, avoiding the tedious work-up and purification of intermediate compounds, achieving sustainable synthesis processes. Considering usual conventional methods, this microwave protocol was featured by advantages in terms of yields, reaction times, and convenient gram scale synthesis.

Molecules published new progress about Fused heterocyclic compounds Role: SPN (Synthetic Preparation), PREP (Preparation). 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Application of C6H5ClN4S.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Senga, Keitaro; O’Brien, Darrell E.; Scholten, Mieka B.; Novinson, Thomas; Miller, Jon P.; Robins, Roland K. published the artcile< Synthesis and enzymic activity of various substituted pyrazolo[1,5-a]-1,3,5-triazines as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors>, COA of Formula: C6H5ClN4S, the main research area is pyrazolotriazine cAMP phosphodiesterase inhibitor preparation; pyrazolylamidine cyclization; amidine pyrazolyl cyclization.

I (R1 = H, Me, Et, SMe; R2 = H, Ph, Pr, SMe, NHEt, NHBu, NEt2 piperidino, OH, NHPr, SH, OCHMe2, Me, SEt, OMe, OPr; R3 = Ph, C6H4OMe-4, H; R4 = H, Br, C6H4Me-3, Ph, cyano, CO2Et, Cl), prepared by cyclizing II with (R2CO)2O or R2C(OEt)3, followed by electrophilic substitution in the pyrazole ring and/or nucleophilic substitution in the 1,3,5-triazine moiety, were studied as inhibitors of cAMP phosphodiesterase (PDE) isolated from bovine brain, bovine heart, and rabbit lung. A number of compounds were superior to theophylline. 2-Ethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine was 97 times more potent than theophylline as an inhibitor of bovine brain PDE. 8-Bromo-2,4-dimethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine showed αlung = 40 compared to αheart = 3.0. Thus, various substituents could increase or decrease the inhibition relative to the type and source of tissue from which the PDE was isolated. The most active compound was 8-bromo-4-(diethylamino)-7-phenylpyrazolo[1,5-a]-1,3,5-triazine which was 185 times more potent than theophylline as an inhibitor of PDE isolated from rabbit lung. Structure-activity relationships were reviewed.

Journal of Medicinal Chemistry published new progress about Structure-activity relationship. 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, COA of Formula: C6H5ClN4S.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Bongard, Jens; Schmitz, Anna Laura; Wolf, Alex; Zischinsky, Gunther; Pieren, Michel; Schellhorn, Birgit; Bravo-Rodriguez, Kenny; Schillinger, Jasmin; Koch, Uwe; Nussbaumer, Peter; Klebl, Bert; Steinmann, Joerg; Buer, Jan; Sanchez-Garcia, Elsa; Ehrmann, Michael; Kaiser, Markus published the artcile< Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action>, Computed Properties of 54346-19-9, the main research area is DegS drug target antibiotic preparation; antibiotics; drug discovery; small molecules; synergism; synthesis.

Despite the availability of hundreds of antibiotic drugs, infectious diseases continue to remain one of the most notorious health issues. In addition, the disparity between the spread of multidrug-resistant pathogens and the development of novel classes of antibiotics exemplify an important unmet medical need that can only be addressed by identifying novel targets. Herein we demonstrate, by the development of the first in vivo active DegS inhibitors based on a pyrazolo[1,5-a]-1,3,5-triazine scaffold, that the serine protease DegS and the cell envelope stress-response pathway σE represent a target for generating antibiotics with a novel mode of action. Moreover, DegS inhibition is synergistic with well-established membrane-perturbing antibiotics, thereby opening promising avenues for rational antibiotic drug design.

ChemMedChem published new progress about Antibacterial agent resistance. 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Computed Properties of 54346-19-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.

To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, e.g. I (X = CH), triazolo[1,5-a]pyrimidines, e.g. I (X = N), imidazo[1,2-a]pyrimidines, e.g. II, and a pyrazolo[1,5-a][1,3,5]triazine, III, were designed, synthesized and evaluated as CRF1 receptor antagonists. Several compounds showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound I (X = CH) was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chem. modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidines, e.g. IV. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.

Bioorganic & Medicinal Chemistry published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics