Tag: 100-200

Chemotherapeutically active anthraquinones. II. Aminomethylanthraquinones was written by Winkelmann, E.;Raether, W.. And the article was included in Arzneimittel-Forschung in 1986.SDS of cas: 21867-64-1 This article mentions the following:

Anthraquinones [I, R = OAc, S₂CNEt₂, Sc(:NH)NH₂, NH₂, dialkylamino, heterocyclic, S(CH₂)₂NEt₂, OC₆H₄NH₂, R¹ = H, XR, R² = H, XR, Me, R³ = R⁵ = H, OH, heterocyclic, R⁴ = H, OH] were prepared and tested in vitro and in vivo (in hamster) against Entamoeba histolytica and interferon-inducing property in mice. Activity against Trichomonas foetus (in mice) was also tested. Most of the compounds showed chemotherapeutic activities in these tests. Structure-activity relations are discussed. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 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. 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.SDS of cas: 21867-64-1

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

Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) was written by Park, Chun-Ho;Chun, Kwangwoo;Joe, Bo-Young;Choi, Jong-Hee;Lee, Han-Chang;Ku, Il-Whea;Kim, Hyun Young;Koh, Seong-Ho;Cho, Goang Won;Kim, Seung Hyun;Kim, Myung-Hwa. And the article was included in Medicinal Chemistry Research in 2012.Product Details of 21867-64-1 This article mentions the following:

A series of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxamides, were successfully synthesized, and their PARP-1 inhibitory activity was evaluated. These compounds were prepared from the corresponding carboxylate and appropriate amines, and a number of the synthesized compounds were found to have significant PARP-1 activity. Among them, one compound showed potent activity in a PARP-1 enzymic and cell-based assay (IC₅₀ = 0.045 μM, ED₅₀ = 0.54 μM). Mol. modeling confirmed the obtained biol. results. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

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. 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.Product Details of 21867-64-1

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

Synthesis, characterization, and biological activity of novel metronidazole-piperazine amides was written by Al-Qtaitat, Malath A.;Saadeh, Haythem A.;Al-Bakri, Amal G.;Kaur, Hargobinder;Goyal, Kapil;Sehgal, Rakesh;Mubarak, Mohammad S.. And the article was included in Monatshefte fuer Chemie in 2015.Safety of 1-Propylpiperazine This article mentions the following:

A new series of metronidazole derivatives containing piperazine rings were prepared via the reaction of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)acetyl chloride with selected substituted piperazines in the presence of a base. Structures of the new compounds were confirmed by NMR and MS spectral data and by elemental analyses. The antibacterial and anti-parasitic activities of these compounds were evaluated in vitro. Some of the newly synthesized compounds exhibited superior activity against Clostridium sporogenes bacteria compared to the standard drug metronidazole (I). On the other hand, other derivatives exhibited remarkable antigiardial activity and were found to be more active than metronidazole with IC₅₀ ranging from 1.8 to 6.7 μg/dm³. 1-Ethyl-4-[2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl]piperazine (II) also exhibited antigiardial activity with similar IC₅₀ value (7.6 μg/cm³) as compared to the reference drug metronidazole (IC₅₀ = 7.4 μg/cm³). Similarly, several of the new compounds exhibited significant antitrichomonal activity and found to be more active than metronidazole with IC₅₀ ranging from 6.7 to 8.65 μg/cm³ as compared to the reference drug metronidazole (8.9 μg/cm³). 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. 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.Safety of 1-Propylpiperazine

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

[(S)-γ-(4-Aryl-1-piperazinyl)-L-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors was written by Yoshida, Tomohiro;Sakashita, Hiroshi;Akahoshi, Fumihiko;Hayashi, Yoshiharu. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.COA of Formula: C10H12N4 This article mentions the following:

In the search for an inhibitor of dipeptidyl peptidase IV (DPP-IV) highly potent both in vitro and in vivo, a series of L-prolylthiazolidine-based DPP-IV inhibitors, e.g., I, having 4-arylpiperazine or 4-arylpiperidine at the γ-position of the proline structure was synthesized. Of these compounds, the 4-(5-nitro-2-pyridyl)piperazine analog I showed a sub-nanomolar (IC₅₀ = 0.92 nmol/L) DPP-IV inhibitory activity and a long-lasting in vivo DPP-IV inhibition profile. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0COA of Formula: C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C10H12N4

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

Syntheses of Mannich basic compounds of tetrahydronaphthol containing piperazine side chains was written by Gao, Shouhai;Li, Fulin. And the article was included in Zhongguo Yaowu Huaxue Zazhi in 1993.Application of 21867-64-1 This article mentions the following:

Title compounds I (R = Me, Et, Pr, Me₂CH, Bu, iso-Bu, EtCHMe, pentyl, isopentyl) were prepared starting from 1-naphthol. I (R = Bu, EtCHMe, isopentyl) showed antimalarial activity comparable to that of chloroquine. 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. 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. 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 of 21867-64-1

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

Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides was written by Lory, Pedro M. J.;Estrella-Jimenez, Maria E.;Shashack, Matthew J.;Lokesh, Ganesh L.;Natarajan, Amarnath;Gilbertson, Scott R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Quality Control of 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

Methods appropriate for the parallel synthesis of libraries based on the thioxanthen-9-one 10,10-dioxide scaffold are reported. The novel compounds were synthesized from previously reported 3-chlorothioxanthen-9-one-10,10-dioxide and com. available 3-carboxythioxanthen-9-one 10,10-dioxide. The library members were screened for activity in a fluorescence polarization assay for inhibitors of BRCT domains of breast cancer gene 1 and in cell-based secreted alk. phosphatase reported replicon system for activity against hepatitis C virus. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Quality Control of 6-(Piperazin-1-yl)nicotinonitrile).

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

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

Substituted (ω-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants was written by Kikumoto, Ryoji;Tobe, Akihiro;Fukami, Harukazu;Ninomiya, Kunihiro;Egawa, Mitsuo. And the article was included in Journal of Medicinal Chemistry in 1984.Synthetic Route of C7H16N2 This article mentions the following:

(ω-Aminoalkoxy)stilbenes I [R¹ = H, Cl, F, 2-MeO, 2-Me, 3,4-Cl₂; R² = H, 3-MeO, 5-Cl; R³ = NMe₂, NEt₂, NHMe, NPr₂, 1-pyrrolidinyl, 1-piperidinyl, morpholino, 4-alkyl-1-piperazinyl, 3-R⁴-substituted-1-piperidinyl (R⁴ = OH, alkoxy, OAc, CH₂OH, CONH₂, CO₂Me, Me, CO₂H); n = 2-5] and II (butoxy at 2, 3, 4) were prepared by successive Grignard reaction of benzyl chlorides III with salicylaldehydes IV, dehydration of (1-hydroxyphenethyl)phenols, ω-bromoalkylation of hydroxy-trans-stilbenes, and amination of the product bromoalkyl ethers with amines. The effect of structural modification of these mols. on the activities was examined Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1-piperazinyl)butoxy]stilbene and piperidinobutoxystilbene derivatives V (R⁴ = OH, OMe, OEt, and OAc) as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. V (R⁴ = OH) exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacol. tests in rats, and its therapeutic index was superior to those of two antiepileptic drugs. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Synthetic Route of C7H16N2).

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. 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.Synthetic Route of C7H16N2

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

Bis(β-haloethyl)amines. VII. A new synthesis of N-monoalkylpiperazines was written by Prelog, V.;Stepan, V.. And the article was included in Collection of Czechoslovak Chemical Communications in 1935.Electric Literature of C7H16N2 This article mentions the following:

The N- and N,N’ -substituted piperazines are readily obtained by interaction of primary amines with (XCH₂CH₂)₂NR (X = Cl or, better, Br). (HOCH₂CH₂)₂NMe (I) (60 g.) in 100 g. 48% HBr, evaporated to a sirup and heated 6 hrs. at 160-80°, yields 66% (BrCH₂CH₂)₂NMe (II), m. 151-2° (picrate, m. 121-2°). In 170 g. CHCl₃, 20 g. I and 87 g. SOCl₂, refluxed 1 hr. give 56% (ClCH₂CH₂)₂NMe (III), m. 116-17°. Refluxed 15 hrs. in 100 cc. MeOH, 48 g. II and 28 g. PhNH₂ give, after fractional distillation, 58% N-methyl-N’-phenylpiperazine (IV), b₃ 140-2°; similarly, III gives the HCl salt, m. 233.5°, in 26% yield. With MeI. IV gives an impure methiodide, m. 238-9°, which with AgCl yields a methochloride, decomposing at 215°. Treated with NaNO₂ followed by SO₂ (cf. Friedländer, III, 957), IV is decomposed to N-methyl-piperazine (V), b. 134-6° (dihydrochloride monohydrate, m. 242-3°; dichloroplatinate; dipicrate, decomposing at 272°; addition compound with CS₂, subliming without decomposition about 180°). With BzCl, V gives C₁₂H₁₇ON₂Cl, m. 240°. Prepared like II, in 58% yield, (BrCH₂CH₂)₂NEt m. 170° (picrate, m. 120.5°) and yields 63.5% N-ethyl-N’-phenylpiperazine,m. 50-1°. This, with NaNO₂, gives the unstable di-HCl salt of N-ethyl-N’-p-nitrosophenylpiperazine, decomposing near 210°, which with SO₂ yields N-ethylpiperazine (di-HCl salt, m. 210-11°; dipicrate,decomposes at 257°). Similarly obtained are (BrCH₂CH₂)₂N-Pr, m. 157° (picrate, m. 101-2°); N-propyl-N’-phenylpiperazine, b<0.1 102-3° (HBr salt, m. 231-2°) and N-propylpiperazine (di-HCl salt, decomposes at 256°; dipicrate, m. 241-2° (decomposition)). In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Electric Literature of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Electric Literature of C7H16N2

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

Non-imidazole histamine H₃ ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H₃-antagonists was written by Walczynski, Krzysztof;Zuiderveld, Obbe P.;Timmerman, Henk. And the article was included in European Journal of Medicinal Chemistry in 2005.Safety of 1-Propylpiperazine This article mentions the following:

Propylpiperazinyl benzoxazoles, benzothiazoles, oxazolopyridines, and thiazolopyridines I [X = O, S; Y, Z, A, B = CH, N (either none or one of the variable groups is N)] and their hydrobromide salts are prepared as selective histamine H₃ receptor antagonists; their histamine H₃ antagonist activities and the relationship between their structures and activities are discussed. Propylpiperazinyl-substituted thiazolopyridines and a propylpiperazinyl-substituted benzothiazole are better histamine H₃ antagonists than propylpiperazinyl-substituted oxazolopyridines and a propylpiperazinyl-substituted benzooxazole. I (X = S; Y = A = B = CH; Z = N) is the most potent histamine H₃ antagonist of the series, with a pA₂ value of 7.25, while the corresponding oxazolopyridine I (X = O; Y = A = B = CH; Z = N) has a pA₂ value of 6.9. 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of 1-Propylpiperazine

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

Producing of a novel condensed heterocycles and combinatorial libraries on the basis of 2-amino-5-bromopyridine-3-sulfochloride was written by Dorogov, M. V.;Solov’ev, M. Yu.;Kravchenko, D. V.;Blyumina, M. V.;Tkachenko, S. E.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2005.COA of Formula: C7H16N2 This article mentions the following:

2-Amino-5-bromopyridine-3-sulfonyl chloride (I) was readily prepared by chlorosulfonylation of 2-amino-5-bromopyridine. Subsequent amination of I with primary or secondary amines or with amino acids, such as sarcosine or β-alanine, gave the libraries of the corresponding 2-amino-5-bromo-3-pyridinesulfonamides and 2-amino-5-bromo-3-pyridinesulfonylamino-substituted carboxylic acids, resp. The latter were further amidated with various primary and secondary amines to afford the libraries of pyridylsulfonylamino-functionalized carboxamides. On the other hand, N-(2-amino-5-bromopyridine-3-sulfonyl)-N-Me aminoacetic acid, available from I and sarcosine, undergoes intramol. cyclization on treatment with 1,1′-carbonyldiimidazole (CDI) at 40-100° to form novel pyrido[2,3-f][1,2,5]thiadiazepinone S,S-dioxide II. The reaction of N,N’-unsubstituted 2-amino-5-bromopyridine-3-sulfonamide with succinic anhydride afforded novel trioxocyclopenta[3,4]pyrido[2,3-e][1,2,4]thiadiazine III, which readily reacts with amines in the presence of CDI to provide the combinatorial library of pyrido[2,3-e][1,2,4]thiadiazines IV (R¹R²NH is primary or secondary aliphatic cycloaliphatic, aromatic or heterocyclic amine). The mol. parameters, such as mol. weight, lipophilicity or a total number of hydrogen bond donors and acceptors, have been calculated for some of the products. 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. 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).COA of Formula: C7H16N2

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