Month: December 2022

Design, synthesis and biological evaluation of oxazolidinone-quinolone hybrids was written by Hubschwerlen, Christian;Specklin, Jean-Luc;Sigwalt, Christine;Schroeder, Susanne;Locher, Hans H.. And the article was included in Bioorganic & Medicinal Chemistry in 2003.Reference of 119285-07-3 This article mentions the following:

Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesized and shown to be active against a variety of resistant and susceptible Gram-pos. and fastidious Gram-neg. organisms. The best compounds in this series overcome all types of resistance in relevant clin. Gram-pos. pathogens. The nature of the spacer greatly influences the antibacterial activity. The dual mode of action could be demonstrated for compounds having a piperazinyl spacer. Antibacterial activity was higher at acidic pH. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Reference of 119285-07-3).

tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. 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.Reference of 119285-07-3

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

Catalytic One-Handed Helix Induction and Subsequent Static Memory of Poly(biphenylylacetylene)s Assisted by a Small Amount of Carboxy Groups Introduced at the Pendants was written by Ikai, Tomoyuki;Takeda, Shoki;Yashima, Eiji. And the article was included in ACS Macro Letters in 2022.Application In Synthesis of (R)-1-Cbz-3-methylpiperazine This article mentions the following:

A dynamically racemic helical copolymer composed of an achiral biphenylylacetylene (BPA) bearing methoxymethoxy groups at the 2,2′-positions and 1 mol % of an achiral BPA carrying 2-carboxy-2′-methoxymethoxy groups at the biphenyl pendants was found to fold into an excess one-handed helix with significant amplification of the helicity in the presence of a small amount of optically active amines. The induced macromol. helicity was retained (“memorized”) after removal of the chiral amines. The copolymer had a significant sensitivity for detecting the chirality of chiral amines with a sensitivity more than 10000-fold higher than that of the corresponding homopolymers with no carboxy group, thus showing Cotton effects even in the presence of a 0.01 equiv of an optically active amine. The effects of the substituents at the 4′-position of the biphenyl pendants of the copolymers and the structures of the chiral amines on the macromol. helicity induction were also investigated. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5Application In Synthesis of (R)-1-Cbz-3-methylpiperazine).

(R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Application In Synthesis of (R)-1-Cbz-3-methylpiperazine

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

Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors was written by Ryu, Je Ho;Kim, Shinae;Lee, Jung A.;Han, Hye Young;Son, Hyun Joo;Lee, Hyun Jung;Kim, Yong Hyuk;Kim, Jae-Sun;Park, Hyeung-geun. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Application In Synthesis of 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

The synthesis and structure-activity relationship of a series of 6-substituted picolinamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 are described. The optimization of the left-hand side of lead compound I resulted in the discovery of the highly potent, selective, and orally available inhibitor II, which demonstrated an excellent activity in a mouse ex vivo pharmacodynamic model. Moreover, II reduced the blood glucose and improved the lipid profiles in ob/ob mice after oral administration. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Application In Synthesis of 6-(Piperazin-1-yl)nicotinonitrile).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Application In Synthesis of 6-(Piperazin-1-yl)nicotinonitrile

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

Protein binding in a congeneric series of antibacterial quinolone derivatives was written by Zlotos, Gabriele;Bucker, Annegret;Jurgens, Jens;Holzgrabe, Ulrike. And the article was included in International Journal of Pharmaceutics in 1998.HPLC of Formula: 21867-64-1 This article mentions the following:

The extent of plasma protein binding was determined in a series of gyrase inhibitors characterized either by a varying substitution on the Ph ring in position N-1 or by an increasing alkyl chain at the N-4′ of the piperazine moiety. An attempt was made to derive QSARs. Especially substituents at the m-position of the N-1-Ph ring influenced the extent of protein binding; an optimum of size was determined The increase of the alkyl group at the outer piperazine nitrogen which is combined with an augmented lipophilicity resulted in an increase in the degree of protein binding. So it can be concluded that the N-1-Ph ring as well as the piperazine ring take part in the interaction with the plasma protein. Both substituents can be used to regulate the extent of protein binding in new gyrase inhibitors. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1HPLC of Formula: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.HPLC of Formula: 21867-64-1

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

Synthesis and antibacterial activities of substituted 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acids was written by Hayakawa, Isao;Hiramitsu, Tokiyuki;Tanaka, Yoshiaki. And the article was included in Chemical & Pharmaceutical Bulletin in 1984.Computed Properties of C7H16N2 This article mentions the following:

Title compounds I [R = H, Me; R¹ = F, Cl; R² = (substituted) piperazino, piperidino, diazepino, pyrrolidino, etc.] (44 compounds) were prepared from nitrobenzenes II (R¹, R³, R⁴ = F, F, F; Cl, F, Cl; F, Cl, F) via benzoxazines III. I (R = Me, R¹ = F, R² = 4-methyl-1-piperazinyl) (DL-8280) showed potent antibacterial activity against Gram-pos. and -neg. pathogens, including Pseudomonas aeruginosa, and its metabolic disposition was shown in sep. experiments to be favorable. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Computed Properties of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. 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. Computed Properties of C7H16N2

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

Synthesis, biological evaluation, and molecular docking study of thiophene-, piperazine-, and thiazolidinone-based hybrids as potential antimicrobial agents was written by Desai, Nisheeth C.;Rupala, Yogesh M.;Khasiya, Ashvinkumar G.;Shah, Keyur N.;Pandit, Unnat P.;Khedkar, Vijay M.. And the article was included in Journal of Heterocyclic Chemistry in 2022.Reference of 21867-64-1 This article mentions the following:

Antibiotic resistance in bacteria exacerbates the issue of antimicrobial resistance. Bacteria that cause common or serious infections have evolved resistance to every new antibiotic that has been introduced into the market, to varying degrees, over several decades. Faced with this reality, one of societys most urgent needs is for new antimicrobial drugs with novel mechanisms of action. With this objective, we describe here the development of a novel set of compounds including piperazine- and thiophene-based thiazolidinones (5a-i) and thiophene-thiazolidinones (6a-i). Compounds (5a-i) and (6a-i) were developed, synthesized, and tested for their antimicrobial activity, and their structures were elucidated with the help of various anal. techniques. Compounds 5a and 5d showed excellent antibacterial efficacy against Pseudomonas aeruginosa, with MICs of 50 μg/mL, whereas compounds 6c and 6e showed similar potency against Staphylococcus aureus and Escherichia coli, resp. The antifungal efficacy of compounds 5e and 6i against Candida albicans was outstanding (MIC = 50 μg/mL). The only compound that had excellent antifungal efficacy against Aspergillus niger was compound 5e (MIC = 50 μg/mL). The chemico-in silico-biol. approach could provide valuable insights into the potential of this novel hybridized scaffold for the development of promising antimicrobial agents. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Reference of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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. Reference of 21867-64-1

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

A therapeutic approach to pantothenate kinase associated neurodegeneration was written by Sharma, Lalit Kumar;Subramanian, Chitra;Yun, Mi-Kyung;Frank, Matthew W.;White, Stephen W.;Rock, Charles O.;Lee, Richard E.;Jackowski, Suzanne. And the article was included in Nature Communications in 2018.Safety of 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

Pantothenate kinase (PANK) is a metabolic enzyme that regulates cellular CoA (CoA) levels. There are three human PANK genes, and inactivating mutations in PANK2 lead to pantothenate kinase associated neurodegeneration (PKAN). Here we performed a library screen followed by chem. optimization to produce PZ-2891, an allosteric PANK activator that crosses the blood brain barrier. PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK.ATP.Mg²⁺.PZ-2891 complex. The binding of PZ-2891 to one protomer locks the opposite protomer in a catalytically active conformation that is refractory to acetyl-CoA inhibition. Oral administration of PZ-2891 increases CoA levels in mouse liver and brain. A knockout mouse model of brain CoA deficiency exhibited weight loss, severe locomotor impairment and early death. Knockout mice on PZ-2891 therapy gain weight, and have improved locomotor activity and life span establishing pantazines as novel therapeutics for the treatment of PKAN. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Safety of 6-(Piperazin-1-yl)nicotinonitrile).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) 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.Safety of 6-(Piperazin-1-yl)nicotinonitrile

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

Design and synthesis of an anticancer diarylurea derivative with multiple-kinase inhibitory effect was written by El-Gamal, Mohammed I.;Oh, Chang-Hyun. And the article was included in Bulletin of the Korean Chemical Society in 2012.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

A pyrrolo[3,2-c]pyridine derivative [N-[1-[4-[[[[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenyl]-1H-pyrrolo[3,2-c]pyridin-4-yl]benzamide (I)] was designed and the synthesis of the target compound was achieved using N-[1-(4-aminophenyl)-1H-pyrrolo[3,2-c]pyridin-4-yl]benzamide and 4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzenamine as key reactants. I was evaluated in a five-dose mode to determine its IC₅₀, TGI, and LC₅₀ values over the 60 cell lines. I displayed high potency and good efficacy and was accordingly tested at a single dose concentration of 10 μM over a panel of 40 kinases. At this concentration, it completely inhibited the enzymic activities of a number of oncogenic kinases, including ABL [kinase (phosphorylating) gene abl protein], ALK [kinase (phosphorylating) gene ALK protein], c-RAF [kinase (phosphorylating) gene raf-1 protein], FLT3 [kinase (phosphorylating) gene FLT3 receptor], KDR [kinase (phosphorylating) gene flk-1 protein] and TrkB [kinase (phosphorylating) gene trkB neurotropic factor receptor]. I was subsequently tested over these 6 kinases in 10-dose testing mode in order to determine its IC₅₀ values. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. 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: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

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

Synthesis of 4-(4-guanidinobenzoyloxy)benzamides and 1-(4-guanidinobenzoyloxy)benzoyloxy acetamides as trypsin inhibitors was written by Zlatoidsky, P.;Maliar, T.. And the article was included in European Journal of Medicinal Chemistry in 1996.Safety of 1-Propylpiperazine This article mentions the following:

Seventeen new compounds of 4-(4-guanidinobenzoyloxy)benzamides and 4-(4-guanidinobenzoyloxy)benzoyloxyacetamides were prepared and their inhibitory activities on trypsin, thrombin and porcine pancreatic elastase were measured. These compounds were found to be selective trypsin inhibitors with inhibiting activities from 0.44 to 43 μM. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Safety of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Safety of 1-Propylpiperazine

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

Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists was written by Gore, Vijay K.;Ma, Vu V.;Tamir, Rami;Gavva, Narender R.;Treanor, James J. S.;Norman, Mark H.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Electric Literature of C13H18N2O2 This article mentions the following:

A novel series of 4,5-biarylimidazoles as TRPV1 antagonists were designed based on the previously reported 4,6-disubstituted benzimidazole series. The analogs were evaluated for their ability to block capsaicin- or acid-induced calcium influx in TRPV1-expressing CHO cells. These studies led to the identification of a highly potent and orally bioavailable TRPV1 antagonist, imidazole 33. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5Electric Literature of C13H18N2O2).

(R)-1-Cbz-3-methylpiperazine (cas: 623586-00-5) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Electric Literature of C13H18N2O2

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