Tag: 100-200

Synthesis and antimuscarinic activity of some 1-cycloalkyl-1-hydroxy-1-phenyl-3-(4-substituted piperazinyl)-2-propanones and related compounds was written by Kaiser, Carl;Audia, Vicki H.;Carter, J. Paul;McPherson, Daniel W.;Waid, Philip P.;Lowe, Valerie C.;Noronha-Blob, Lalita. And the article was included in Journal of Medicinal Chemistry in 1993.COA of Formula: C7H16N2 This article mentions the following:

A new class of substituted 1-phenyl-3-piperazinyl-2-propanones I (R = cyclobutyl, cyclohexyl, iso-Bu, cyclopropyl, Ph, cyclopentyl, R¹ = H, Me, CH₂CCH, CH₂Ph, CH₂CN, CH₂C₆H₄NO₂-4, etc.) and PhCR(OH)COCH₂R² [II, R = cyclopropyl, cyclobutyl, cyclopentyl, Ph, R² = 4-hydroxy-1-piperidinyl, 4-(1-pyrrolidinyl)piperidinyl, NH(CH₂)₂NMe₂) with antimuscarinic activity were prepared Thus, PhCR(OH)COMe were brominated to give PhCR(OH)COCH₂Br which were aminated to give I and II. As part of a structure-activity relationship study of this class, various structural modifications, particularly one involving substitution of position 1 and the terminal piperazine nitrogen, were investigated. The objective of this study was to derive new antimuscarinic agents with potential utility in treating urinary incontinence associated with bladder muscle instability. These compounds were examined for M₁, M₂, and M₃ muscarinic receptor selectivity in isolated tissue assay and for in vivo effects on urinary bladder contraction, mydriasis, and salivation in guinea pigs. Potency and selectivity in these assays were influenced most notably by the nature of the substituent group on the terminal nitrogen of the piperazine moiety. Benzyl substitution was particularly advantageous in producing compounds with functional M₃ receptor (smooth muscle) and bladder selectivity; it provided several candidates for clin. study. In vivo, I (R = cyclobutyl, R¹ = CH₂Ph) demonstrated 11- and 37-fold separations in its effect on bladder function vs. mydriatic and salivation responses, resp. The corresponding 2-chlorobenzyl derivative was more than 178-fold selective for M₃ vs. M₁ and M₂ muscarinic receptors. I (R = Ph, R¹ = CH₂Ph) was 18-fold selective for M₃ vs. M₁ and 242-fold selective for M₃ vs. M₂ receptors. It was also selective in guinea pigs, where it displayed 20- and 41-fold separations between bladder function and effect on mydriasis and salivation, resp. In general, the results of this study are consistent with the proposition that the described piperazinylpropanones interact with muscarinic receptors in a hydrogen-bonded form that presents a conformation similar to that apparently adopted by classical antimuscarinic agents. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1COA of Formula: C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C7H16N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Benzophenone-Based Farnesyltransferase Inhibitors with High Activity against Trypanosoma cruzi was written by Esteva, Monica I.;Kettler, Katja;Maidana, Cristina;Fichera, Laura;Ruiz, Andres M.;Bontempi, Esteban J.;Andersson, Bjoern;Dahse, Hans-Martin;Haebel, Peter;Ortmann, Regina;Klebe, Gerhard;Schlitzer, Martin. And the article was included in Journal of Medicinal Chemistry in 2005.Category: piperazines This article mentions the following:

Less toxic drugs are needed to combat the human parasite Trypanosoma cruzi (Chagas’s disease). One novel target for antitrypanosomal drug design is farnesyltransferase. Several farnesyltransferase inhibitors based on the benzophenone scaffold were assayed in vitro and in vivo with the parasite. The common structural feature of all inhibitors is an amino function which can be protonated. Best in vitro activity (LC₅₀ values 1 and 10 nM, resp.) was recorded for the R-phenylalanine derivative 4a and for the N-propylpiperazinyl derivative 2f. These inhibitors showed no cytotoxicity to cells. When tested in vivo, the survival rates of infected animals receiving the inhibitors at 7 mg/kg body weight/day were 80 and 60% at day 115 postinfection, resp. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis of New 5-(1,4-Benzodioxan-2-yl)thieno[2,3-d]pyrimidine Derivatives was written by Vardanyan, S. O.;Aghekyan, A. A.;Avagyan, A. S.;Sargsyan, A. B.;Panosyan, H. A.;Harutyunyan, S. A.;Gasparyan, H. V.. And the article was included in Russian Journal of Organic Chemistry in 2022.Name: 1-Propylpiperazine This article mentions the following:

Cyclization of previously synthesized Et 2-amino-4-(1,4-benzodioxan-2-yl)thiophene-3-carboxylate with formamide gave 5-(1,4-benzodioxan-2-yl)thieno[2,3-d]pyrimidin-4(3H)-one which was treated with phosphoryl chloride in pyridine to obtain the corresponding 4-chloro derivative The latter reacted with various primary and secondary amines to produce a series of new thieno[2,3-d]pyrimidines containing a pharmacophoric fragment at the 4-position. The reaction of 5-(1,4-benzodioxan-2-yl)-4-chlorothieno[2,3-d]pyrimidine with hydrazine hydrate afforded the corresponding 4-hydrazinyl derivative which was cyclized with formic acid to thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivative Antihypoxic properties of the synthesized compounds were studied. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Name: 1-Propylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Piperazinyl Bicyclic Derivatives as Selective Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels was written by Fernandez, Ariadna;Diaz, Jose Luis;Garcia, Monica;Rodriguez-Escrich, Sergi;Lorente, Adriana;Enrech, Raquel;Dordal, Albert;Portillo-Salido, Enrique;Porras, Monica;Fernandez, Begona;Reinoso, Raquel F.;Vela, Jose Miguel;Almansa, Carmen. And the article was included in ACS Medicinal Chemistry Letters in 2021.COA of Formula: C6H14N2 This article mentions the following:

The synthesis and pharmacol. activities of a new series of piperazinyl quinazolin-4-(3H)-one derivatives I [R¹ = H, 5-Br, 6-(4-pyridinyl), 8-Br, etc.; R² = 2-methoxyethyl, benzyl, 2-furylmethyl, etc.; R³ = H, Me, Pr, n-Bu, etc.; R⁴ = piperazin-1-yl, (3R,5S)-3,5-dimethylpiperazin-1-yl, (S)-3-methylpiperazin-1-yl, etc.] acting toward the α2δ-1 subunit of voltage-gated calcium channels (Cavα2δ-1) were reported. Different positions of a micromolar HTS hit were explored, and best activities were obtained for compounds I containing a small alkyl group in position 3 of the quinazolin-4-(3H)-one scaffold and a 3-methyl-piperazin-1-yl- or 3,5-dimethyl-piperazin-1-yl-Bu group in position 2. The activity was shown to reside in the R enantiomer of the chain in position 2, and several eutomers reached single digit nanomolar affinities. Final modification of the central scaffold to reduce lipophilicity provided the pyrido[4,3-d]pyrimidin-4(3H)-one II, which showed high selectivity for Cavα2δ-1 vs. Cavα2δ-2, probably linked to its improved analgesic efficacy-safety ratio in mice over pregabalin. In the experiment, the researchers used many compounds, for example, (S)-2-Ethylpiperazine (cas: 207284-20-6COA of Formula: C6H14N2).

(S)-2-Ethylpiperazine (cas: 207284-20-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C6H14N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Design, synthesis and biological evaluation of 3-arylisoquinoline derivatives as topoisomerase I and II dual inhibitors for the therapy of liver cancer was written by Deng, Xuemei;Luo, Tian;Zhang, Xi;Li, Yuehua;Xie, Liming;Jiang, Weifan;Liu, Linyi;Wang, Zhen. And the article was included in European Journal of Medicinal Chemistry in 2022.COA of Formula: C7H16N2 This article mentions the following:

To explore novel topoisomerase inhibitors with high activity and druggability, 3-aryl isoquinoline alkaloids based on the corydamine modification and preliminary SARs of isoquinoline alkaloids in our previous works were re-designed. Currently, the design strategy is mainly revolved around the rigidity and flexibility of the mol. side chain and the mol. size. Consequently, not only the activity and druggability of the compound could be further improved, also the mechanism behind could been discovered. In vitro pharmacol. studies, the outstanding nature with the excellent activity and the researchable depth of azepane-substituted compound has been found through the vitro cytotoxicity test (IC₅₀ = 1.93μM in HuH7 cells and 2.10μM in LM9 cells) and topoisomerase test. It was found that azepane-substituted compound had dual inhibitory effects on topoisomerase I and II, and its inhibitory activity on topoisomerase II is stronger than the pos. drug etoposide. From the perspective of mol. docking, it had been verified that azepane-substituted compound could insert between DNA base pairs, which was consistent with the results of the DNA unwinding experiment Meanwhile, azepane-substituted isoquinoline could inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Therefore, this study may lay a foundation for the discovery of 3-arylisoquinoline compounds with anti-liver cancer potential. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1COA of Formula: C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.COA of Formula: C7H16N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis of piperazine derivatives. XII. Preparation of N¹-substituted N⁴-(3-phenylpropyl)piperazines was written by Zikolova, S.. And the article was included in Trudove na Nauchnoizsledovatelskiya Khimikofarmatsevtichen Institut in 1978.Application In Synthesis of 1-Propylpiperazine This article mentions the following:

N-(3-Phenylpropyl)piperazine was alkylated with alkyl halides (e.g., EtI) in refluxing solvent containing Na₂CO₃ to give 26 title compounds [I; R = C₁-C₈ alkyl, allyl, crotyl, cycloalkyl, aralkyl, (aryloxy)alkyl, XCH₂CH₂; X = Et₂N, piperidino, morpholino] in 65-98% yield, isolated as hydrochlorides and oxalates. I (R = Me) was also prepared from N-methylpiperazine and Pr(CH₂)₃Br (II) and I [R = Ph(CH₂)₃], from II and piperazine. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application In Synthesis of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application In Synthesis of 1-Propylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Glutathione. X. Human erythrocyte membrane diffusion coefficients for diazene derivatives of the DIP [diazenedicarboxylic acid bis(N’-methylpiperazide)] series via intracellular thiol oxidation was written by Kosower, Nechama S.;Kosower, Edward M.;Saltoun, Gilda;Lev, Lilly. And the article was included in Biochemical and Biophysical Research Communications in 1975.Application of 21867-64-1 This article mentions the following:

The thiol-oxidizing agent, DIP and its homologs with different N’-alkyl groups can be used to obtain membrane diffusion coefficients for human erythrocytes at 1°. From the initial rates of intracellular glutathione oxidation and the 2-octanol partition coefficients for the specific DIP homolog, diffusion coefficients of ∼1 × 10-8 cm2/sec were observed The method (irreversible loss of permeant through well-defined intracellular reaction) may be used to evaluate membrane properties and possibly for the study of substituent effects on drug entry into cells. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application of 21867-64-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis and biological properties of heterylalkylamides of 4-substituted piperazin-1-ylacetic acids was written by Vartanyan, S. O.;Avakyan, A. S.;Sargsyan, A. B.;Arutyunyan, S. A.;Gukasyan, T. G.;Tsatinyan, A. S.;Noravyan, O. S.;Markaryan, I. A.. And the article was included in Hayastani Kimiakan Handes in 2010.Related Products of 21867-64-1 This article mentions the following:

Reaction of chloroacetyl chloride with 1,4-benzodioxan-2-yl or isochroman-1-yl-containing aliphatic amines gave the corresponding N-substituted chloroacetamides. Subsequent treatment of the latter with monosubstituted piperazines afforded the corresponding substituted piperazineacetamides. The biol. properties of these compounds have been investigated. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Related Products of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Related Products of 21867-64-1

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Design, Synthesis and Evaluation of Antidepressant Activity of Novel 2-Methoxy 1, 8 Naphthyridine 3-Carboxamides as 5-HT₃ Receptor Antagonists was written by Mahesh, Radhakrishnan;Dhar, Arghya Kusum;Jindal, Ankur;Bhatt, Shvetank. And the article was included in Chemical Biology & Drug Design in 2014.Application In Synthesis of 1-Propylpiperazine This article mentions the following:

A series of novel 1,8-naphthyridine-3-carboxamides as 5-HT₃ receptor antagonists were synthesized with an intention to explore the antidepressant activity of these compounds The title carboxamides were designed using ligand-based approach keeping in consideration the structural requirement of the pharmacophore of 5-HT₃ receptor antagonists. The compounds were synthesized using appropriate synthetic route from the starting material nicotinamide. 5-HT₃ receptor antagonism of all the compounds, which was denoted in the form of pA₂ value, was determined in longitudinal muscle myenteric plexus preparation from guinea-pig ileum against 5-HT₃ agonist, 2-methyl-5-HT. 2-Methoxy-1, 8-naphthyridin-3-yl (2-methoxy Ph piperazine-1-yl) methanone was identified as the most active compound, which expressed a pA₂ value of 7.67. The antidepressant activity of all the compounds was examined in mice model of forced swim test (FST); importantly, none of the compounds was found to cause any significant changes in the locomotor activity of mice at the tested dose levels. In FST, the compounds with considerably higher pA₂ value exhibited promising antidepressant-like activity, whereas compounds with lower pA₂ value did not show antidepressant-like activity as compared to the control group. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application In Synthesis of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Application In Synthesis of 1-Propylpiperazine

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

M₃ muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines was written by Budzik, Brian;Wang, Yonghui;Shi, Dongchuan;Wang, Feng;Xie, Haibo;Wan, Zehong;Zhu, Chongye;Foley, James J.;Nuthulaganti, Parvathi;Kallal, Lorena A.;Sarau, Henry M.;Morrow, Dwight M.;Moore, Michael L.;Rivero, Ralph A.;Palovich, Michael;Salmon, Michael;Belmonte, Kristen E.;Laine, Dramane I.;Jin, Jian. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2009.Category: piperazines This article mentions the following:

Exploration of multiple regions of a bi-aryl amine template led to the identification of highly potent M₃ muscarinic acetylcholine receptor antagonists such as (I) (pA₂ = 11.0) possessing good sub-type selectivity for M₃ over M₂. The structure-activity relationships (SAR) and optimization of the bi-aryl amine series are described. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Category: piperazines).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics