Month: October 2022

《Synthesis of new antimicrobials. IV. Synthesis of alkylenebis(thiourea) derivatives and their related compounds》 was published in Chemical & Pharmaceutical Bulletin in 1975. These research results belong to Yabuuchi, Takahiro; Hisaki, Masakatu; Matuda, Masahiro; Kimura, Ryuichi. Formula: C5H14Cl2N2 The article mentions the following:

3,3′-Substituted 1,1′-alkylenebis(thiourea) derivatives, e.g. Et2NCH2CH2NHCSNHCH2CH2NHCSNHCH2CH2NEt2 were prepared from alkylenebis(isothiocyanates) and amines. Also, 3,3′-alkylenebis[2-thio-2,4(1H,3H)quinazolinediones] I (m = 3, 4, 6) were prepared by the reaction of alkylenebis(isothiocyanates) and anthranilic acid, or alkylene diamines and Et o-isothiocyanatobenzoate, resp. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Formula: C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Formula: C5H14Cl2N2

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

Product Details of 34352-59-5On October 1, 2020 ,《Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo》 was published in European Journal of Medicinal Chemistry. The article was written by Sudol, Sylwia; Kucwaj-Brysz, Katarzyna; Kurczab, Rafal; Wilczynska, Natalia; Jastrzebska-Wiesek, Magdalena; Satala, Grzegorz; Latacz, Gniewomir; Gluch-Lutwin, Monika; Mordyl, Barbara; Zeslawska, Ewa; Nitek, Wojciech; Partyka, Anna; Buzun, Kamila; Doroz-Plonka, Agata; Wesolowska, Anna; Bielawska, Anna; Handzlik, Jadwiga. The article contains the following contents:

This study had supplied highly potent 5-HT6R agents with procognitive effects, which represent an original chem. class of 1,3,5-triazines, different than widely studied sulfone and indole-like 5-HT6R ligands. The new compounds I (R1 = Ph, 2,3-Cl2C6H3, 2,5-Cl2C6H3, 3,4-Cl2C6H3, 3,5-Cl2C6H3, 2,4-Cl2C6H3; R2 = H, Me, Et, n-Pr, n-Bu, X = nothing; R2 = H, X = CH2CH2) were rationally designed as modifications of lead, 4-(1-(2-chlorophenoxy)ethyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine, involving an introduction of: (i) two chlorines at the benzene ring and (ii) varied linkers joining the triazine ring to aromatic ethers. Synthesis, in vitro and in vivo biol. tests and computer-aided SAR anal. for new compounds were carried out. Most of the new triazines displayed high affinity and selectivity toward 5-HT6R with respect to 5-HT2AR, 5-HT7R and D2R. The crystallog.-supported docking studies, including quantum-polarized ligand docking (QPLD), indicated that chlorine atoms might be involved in different type of halogen bonding, however, the linker properties seem to predominately affect the 5-HT6R affinity. Compound I (R1 = 2,5-Cl2C6H3; R2 = Et; X = nothing), which displayed: the highest affinity (Ki = 6 nM), very strong 5-HT6R antagonistic action (KB = 27 pM), procognitive effects in vivo in novel object recognition (NOR) test in rats, a very good permeability in PAMPA model and satisfying safety in vitro, was identified as the most potent 1,3,5-triazine agent so far, useful as a new lead for further research. In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Product Details of 34352-59-5)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Product Details of 34352-59-5

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

Miller-Moslin, Karen; Peukert, Stefan; Jain, Rishi K.; McEwan, Michael A.; Karki, Rajesh; Llamas, Luis; Yusuff, Naeem; He, Feng; Li, Yanhong; Sun, Yingchuan; Dai, Miao; Perez, Lawrence; Michael, Walter; Sheng, Tao; Lei, Huangshu; Zhang, Rui; Williams, Juliet; Bourret, Aaron; Ramamurthy, Arun; Yuan, Jing; Guo, Ribo; Matsumoto, Melissa; Vattay, Anthony; Maniara, Wieslawa; Amaral, Adam; Dorsch, Marion; Kelleher, Joseph F. III published an article in Journal of Medicinal Chemistry. The title of the article was 《1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity》.COA of Formula: C11H14N4 The author mentioned the following in the article:

Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-mol. inhibitors of this pathway represents a promising route toward novel anticancer therapeutics. A cell-based screen performed in our laboratories identified a new class of Hh pathway inhibitors, 1-amino-4-benzylphthalazines, e.g. I, that act via antagonism of the Smoothened receptor. A variety of analogs were synthesized and their structure-activity relationships determined This optimization resulted in the discovery of high affinity Smoothened antagonists, one of which was further profiled in vivo. This compound displayed a good pharmacokinetic profile and also afforded tumor regression in a genetic mouse model of medulloblastoma. After reading the article, we found that the author used (R)-6-(3-Methylpiperazin-1-yl)nicotinonitrile(cas: 1057682-05-9COA of Formula: C11H14N4)

(R)-6-(3-Methylpiperazin-1-yl)nicotinonitrile(cas: 1057682-05-9) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.COA of Formula: C11H14N4

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

Zajdel, Pawel; Kos, Tomasz; Marciniec, Krzysztof; Satala, Grzegorz; Canale, Vittorio; Kaminski, Krzysztof; Holuj, Malgorzata; Lenda, Tomasz; Koralewski, Robert; Bednarski, Marek; Nowinski, Leszek; Wojcikowski, Jacek; Daniel, Wladyslawa A.; Nikiforuk, Agnieszka; Nalepa, Irena; Chmielarz, Piotr; Kusmierczyk, Justyna; Bojarski, Andrzej J.; Popik, Piotr published an article on February 10 ,2018. The article was titled 《Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects》, and you may find the article in European Journal of Medicinal Chemistry.Quality Control of 4-(Piperazin-1-yl)-1H-indole The information in the text is summarized as follows:

Currently used antipsychotics are characterized by multireceptor mode of action. While antagonism of dopamine D2 receptors is responsible for the alleviation of “”pos.”” symptoms of schizophrenia and the effects at other, particularly serotonergic receptors are necessary for their addnl. therapeutic effects, there is no consensus regarding an “”ideal”” target engagement. Here, a detailed SAR anal. in a series of 45 novel azinesulfonamides of cyclic amine derivatives, involving the aryl-piperazine/piperidine pharmacophore, central alicyclic amine and azinesulfonamide groups has led to the selection of (S)-4-((2-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)isoquinoline (62). The polypharmacol. profile of 62, characterized by partial 5-HT1AR agonism, 5-HT2A/5-HT7/D2/D3R antagonism, and blockade of SERT, reduced the “”pos.””-like, and “”neg.””-like symptoms of psychoses. Compound 62 produced no catalepsy, demonstrated a low hyperprolactinemia liability and displayed pro-cognitive effects in the novel object recognition task and attentional set-shifting test. While association of in vitro features with the promising in vivo profile of 62 is still not fully established, its clin. efficacy should be verified in further stages of development. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Quality Control of 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. 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).Quality Control of 4-(Piperazin-1-yl)-1H-indole

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

《Synthesis, biological evaluation and molecular docking studies of some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles as potential antibacterial, anticancer and antifungal agents》 was written by Bhardwaj, Harsh; Sharma, C. S.. Related Products of 109-01-3 And the article was included in Indian Journal of Heterocyclic Chemistry in 2020. The article conveys some information:

Some new 2-(2-(substituted piperazin-1-yl)-phenyl)-1H-benzo[d]imidazoles I [R = H, 2-Me, 4-Et, etc.] were designed, synthesized and evaluated by the docking studies using glide tool for their antimicrobial and anticancer activities. The structures of these compounds I were characterized by IR, proton NMR, mass spectral data, and elemental anal. Each analog was tested in-vitro for various types of pharmacol. activities, including antibacterial, antifungal and anticancer activity. The compound I [R = 3-Me] was found to be most active against Escherichia coli and Pseudomonas aeruginosa and compound I [R = 2-Et] against Bacillus subtilis and Staphylococcus aureus. The derivative I [R = 4-Et] showed good activity against Candida albicans and Aspergillus niger. Among all the tested compounds, I [R = H, 2-Me] were found with significant anticancer activity in comparison to Adriamycin standard drug. The obtained results revealed that most of the synthesized compounds I exhibited significant antifungal, antibacterial and anticancer activity. It was deduced that these synthesized compounds I can be regarded as a promising starting point for developing a single mol. with multiple targets.1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Related Products of 109-01-3

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