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Showing papers on "Morpholine published in 2020"


Journal ArticleDOI
TL;DR: The medicinal chemistry/pharmacological activity of morpholine derivatives on various therapeutically related molecular targets are described, attempting to highlight the importance of the morpholine ring in drug design and development as well as to justify its classification as a privileged structure.
Abstract: Morpholine is a heterocycle featured in numerous approved and experimental drugs as well as bioactive molecules. It is often employed in the field of medicinal chemistry for its advantageous physicochemical, biological, and metabolic properties, as well as its facile synthetic routes. The morpholine ring is a versatile and readily accessible synthetic building block, it is easily introduced as an amine reagent or can be built according to a variety of available synthetic methodologies. This versatile scaffold, appropriately substituted, possesses a wide range of biological activities. There are many examples of molecular targets of morpholine bioactive in which the significant contribution of the morpholine moiety has been demonstrated; it is an integral component of the pharmacophore for certain enzyme active-site inhibitors whereas it bestows selective affinity for a wide range of receptors. A large body of in vivo studies has demonstrated morpholine's potential to not only increase potency but also provide compounds with desirable drug-like properties and improved pharamacokinetics. In this review we describe the medicinal chemistry/pharmacological activity of morpholine derivatives on various therapeutically related molecular targets, attempting to highlight the importance of the morpholine ring in drug design and development as well as to justify its classification as a privileged structure.

85 citations


Journal ArticleDOI
TL;DR: The present review primarily focused on discussing the most promising synthetic leads containing morpholine ring along with structure-activity relationship (SAR) to reveal the active pharmacophores accountable for anticancer, anti-inflammatory, antiviral, anticonvulsant, antioxidant, antimicrobial and antileishmanial activity.

74 citations


Journal ArticleDOI
TL;DR: Significantly, this work illustrates a new role for amines in CO2 reduction: changing the product selectivity; this is pertinent more broadly to advancing CCR.
Abstract: Owing to the energetic cost associated with CO2 release in carbon capture (CC), the combination of carbon capture and recycling (CCR) is an emerging area of research. In this approach, "captured CO2," typically generated by addition of amines, serves as a substrate for subsequent reduction. Herein, we report that the reduction of CO2 in the presence of morpholine (generating mixtures of the corresponding carbamate and carbamic acid) with a well-established Mn electrocatalyst changes the product selectivity from CO to H2 and formate. The change in selectivity is attributed to in situ generation of the morpholinium carbamic acid, which is sufficiently acidic to protonate the reduced Mn species and generate an intermediate Mn hydride. Thermodynamic studies indicate that the hydride is not sufficiently hydritic to reduce CO2 to formate, unless the apparent hydricity, which encompasses formate binding to the Mn, is considered. Increasing steric bulk around the Mn shuts down rapid homolytic H2 evolution rendering the intermediate Mn hydride more stable; subsequent CO2 insertion appears to be faster than heterolytic H2 production. A comprehensive mechanistic scheme is proposed that illustrates how thermodynamic analysis can provide further insight. Relevant to a range of hydrogenations and reductions is the modulation of the hydricity with substrate binding that makes the reaction favorable. Significantly, this work illustrates a new role for amines in CO2 reduction: changing the product selectivity; this is pertinent more broadly to advancing CCR.

38 citations


Journal ArticleDOI
TL;DR: Molecular docking studies of the promising derivatives into DNA Gyrase binding site proved the usefulness of hybridizing quinoxaline scaffold with SO2 and morpholine moieties as a hopeful strategy in designing new DNA Gyrsase binding molecules.

37 citations


Journal ArticleDOI
TL;DR: In this article, a nano-sized SAPO-34 zeotype was synthesized using morpholine (MOR)-treated micrometer-sized seeds and MOR as the template.
Abstract: Uniformly nano-sized SAPO-34 zeotypes were synthesized using morpholine (MOR)-treated micrometer-sized SAPO-34 (MS-SAPO-34) seeds and MOR as the template. The samples were prepared with different amounts of MOR-treated MS-SAPO-34 seeds and characterized by XRD, SEM, ICP-OES, N2 adsorption-desorption, NH3-TPD, 29Si NMR, TGA and GC–MS. Using MOR-treated MS-SAPO-34 seeds decreased the crystal size of the SAPO-34 to 200–500 nm. In addition, the samples prepared with MOR-treated MS-SAPO-34 seeds had larger external surface areas, lower Si contents, and lower concentration and weaker strength of the strong acid sites than conventional SAPO-34. The effects of MOR treatment time on the seed properties and on the subsequent SAPO-34 fabrication were also investigated. After MOR-treatment of the MS-SAPO-34 seeds for 30 h, micrometer-sized seeds were broken into nanoparticles, which was indispensable for successful synthesis of nano-sized SAPO-34. When studied as a catalyst for the methanol to olefin reaction, the nano-sized SAPO-34 exhibited excellent catalytic performance.

32 citations


Journal ArticleDOI
TL;DR: It is shown that, in addition to the natural amine substrate 2-phenylethylamine, a range of simple aliphatic amines are coupled efficiently to the native carboxylic acid substrate 1-acetyl-9H-β-carboline-3-carboxYlic acid by the enzyme, to give amide products with up to >99% conversion.
Abstract: The biocatalytic synthesis of amides from carboxylic acids and primary amines in aqueous media can be achieved using the ATP-dependent amide bond synthetase McbA, via an adenylate intermediate, using only 1.5 equiv of the amine nucleophile. Following earlier studies that characterized the broad carboxylic acid specificity of McbA, we now show that, in addition to the natural amine substrate 2-phenylethylamine, a range of simple aliphatic amines, including methylamine, butylamine, and hexylamine, and propargylamine are coupled efficiently to the native carboxylic acid substrate 1-acetyl-9H-β-carboline-3-carboxylic acid by the enzyme, to give amide products with up to >99% conversion. The structure of wild-type McbA in its amidation conformation, coupled with modeling and mutational studies, reveal an amine access tunnel and a possible role for residue D201 in amine activation. Amide couplings were slower with anilines and alicyclic secondary amines such as pyrrolidine and piperidine. The broader substrate specificity of McbA was exploited in the synthesis of the monoamine oxidase A inhibitor moclobemide, through the reaction of 4-chlorobenzoic acid with 1.5 equiv of 4-(2-aminoethyl)morpholine, and utilizing polyphosphate kinases SmPPK and AjPPK in the presence of polyphosphoric acid and 0.1 equiv of ATP, required for recycling of the cofactor.

29 citations


Journal ArticleDOI
TL;DR: A facile and efficient two-step synthetic route for p-substituted tris(2-pyridylmethyl)amine (TPMA) ligands to form Cu complexes with the highest activity in Atom Transfer Radical Polymerization (ATRP) to-date is reported.
Abstract: A facile and efficient two-step synthesis of p-substituted tris(2-pyridylmethyl)amine (TPMA) ligands to form Cu complexes with the highest activity to date in atom transfer radical polymerization (ATRP) is presented. In the divergent synthesis, p-Cl substituents in tris(4-chloro-2-pyridylmethyl)amine (TPMA3Cl ) were replaced in one step and high yield by electron-donating cyclic amines (pyrrolidine (TPMAPYR ), piperidine (TPMAPIP ), and morpholine (TPMAMOR )) by nucleophilic aromatic substitution. The [CuII (TPMANR2 )Br]+ complexes exhibited larger energy gaps between frontier molecular orbitals and >0.2 V more negative reduction potentials than [CuII (TPMA)Br]+ , indicating >3 orders of magnitude higher ATRP activity. [CuI (TPMAPYR )]+ exhibited the highest reported activity for Br-capped acrylate chain ends in DMF, and moderate activity toward C-F bonds at room temperature. ATRP of n-butyl acrylate using only 10-25 part per million loadings of [CuII (TPMANR2 )Br]+ exhibited excellent control.

25 citations


Journal ArticleDOI
TL;DR: The aqua complex has shown a facile substitution chemistry with alicyclic secondary amines, pyrrolidine (pyro), and morpholine (morph), and only the piperidine system has experienced a reduction of copper(II).
Abstract: Copper(II) acetate has reacted in methanol with quinaldinic acid (quinoline-2-carboxylic acid) to form [Cu(quin)2(CH3OH)]∙CH3OH (1) (quin- = an anionic form of the acid) with quinaldinates bound in a bidentate chelating manner. In the air, complex 1 gives off methanol and binds water. The conversion was monitored by IR spectroscopy. The aqua complex has shown a facile substitution chemistry with alicyclic secondary amines, pyrrolidine (pyro), and morpholine (morph). trans-[Cu(quin)2(pyro)2] (2) and trans-[Cu(quin)2(morph)2] (4) were obtained in good yields. The morpholine system has produced a by-product, trans-[Cu(en)2(H2O)2](morphCOO)2 (5) (morphCOO- = morphylcarbamate), a result of the copper(II) quinaldinate reaction with ethylenediamine (en), an inherent impurity in morpholine, and the amine reaction with carbon dioxide. (pyroH)[Cu(quin)2Cl] (3) forms on the recrystallization of [Cu(quin)2(pyro)2] from dichloromethane, confirming a reaction between amine and the solvent. Similarly, a homologous amine, piperidine (pipe), and dichloromethane produced (pipeH)[Cu(quin)2Cl] (11). The piperidine system has afforded both mono- and bis-amine complexes, [Cu(quin)2(pipe)] (6) and trans-[Cu(quin)2(pipe)2] (7). The latter also exists in solvated forms, [Cu(quin)2(pipe)2]∙CH3CN (8) and [Cu(quin)2(pipe)2]∙CH3CH2CN (9). Interestingly, only the piperidine system has experienced a reduction of copper(II). The involvement of amine in the reduction was undoubtedly confirmed by identification of a polycyclic piperidine compound 10, 6,13-di(piperidin-1-yl)dodecahydro-2H,6H-7,14-methanodipyrido[1,2-a:1',2'-e][1,5]diazocine.

24 citations


Journal ArticleDOI
TL;DR: Compounds 5a–b are used as an initiative to prepare many new heterocyclic compounds such as 2-(3-methylbenzodifuran- 2-carbox-amido) pyrimidine, which had analgesic and anti-inflammatory activities and had the highest inhibitory activity on COX-2 selectivity.
Abstract: Novel (4-methoxy or 4,8-dimethoxy)-3-methyl-N-(6-oxo-2-thioxo-1,2,3, 6-tetrahydro- pyrimidin-4-yl) benzo [1,2-b: 5, 4-b’] difuran-2-carboxamide (5a–b) has been synthesized by the reaction of visnagenone–ethylacetate (2a) or khellinone–ethylacetate (2b) with 6-aminothiouracil in dimethylformamide or refluxing of benzofuran-oxy-N-(2-thioxopyrimidine) acetamide (4a–b) in sodium ethoxide to give the same products (5a,b) in good yields. Thus, compounds 5a–b are used as an initiative to prepare many new heterocyclic compounds such as 2-(4-(3-methylbenzodifuran- 2-carbox-amido) pyrimidine) acetic acid (6a–b), N-(thiazolo[3, 2-a]pyrimidine)-3-methylbenzo- difuran-2-carboxamide (7a–b), N-(2-thioxopyrimidine)-methylbenzodifuran-2-carbimidoylchloride (8a–b), N-(2-(methyl-thio) pyrimidine)-3-methylbenzodifuran-2-carbimidoylchloride (9a–b), N-(2, 6 -di(piperazine or morpholine)pyrimidine)-1-(3-methylbenzodifuran)-1-(piperazine or morpholine) methanimine(10a–d), 8-(methylbenzodifuran)-thiazolopyrimido[1,6-a][1,3,5]triazine-3,5-dione (11a –b), 8-(3-methyl benzodifuran)-thiazolopyrimido[6,1-d][1,3,5]oxadiazepine-trione (12a–b), and 2,10 -di(sub-benzylidene)-8-(3-methylbenzodifuran)-thiazolopyrimido[6,1-d][1,3,5]oxadiazepine-3,5,11- trione (13a–f). All new chemical structures were illustrated on the basis of elemental and spectral analysis (IR, NMR, and MS). The new compounds were screened as cyclooxygenase-1/ cyclooxygenase-2 (COX-1/COX-2) inhibitors and had analgesic and anti-inflammatory activities. The compounds 10a–d and 13a–f had the highest inhibitory activity on COX-2 selectivity, with indices of 99–90, analgesic activity of 51–42% protection, and anti-inflammatory activity of 68%–59%. The inhibition of edema for the same compounds, 10a–d and 13a–f, was compared with sodium diclofenac as a standard drug.

24 citations


Journal ArticleDOI
TL;DR: A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine showed moderate DPPH radical scavenging and metal chelating activity, and low ABTS cationradical scavenging activity.
Abstract: A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine were investigated. These compounds were ass...

23 citations


Journal ArticleDOI
TL;DR: The new photoreactive salts exhibit more reactivity but decreased conjugation compared to the commercial lithium salt and are of considerable practical potential in terms of tunable colours and greater range in UV, X-ray, and γ-ray dosimetry applications.
Abstract: In this work we develop photoreactive cocrystals/salts of a commercially-important diacetylene, 10,12-pentacosadiynoic acid (PCDA, 1) and report the first X-ray crystal structures of PCDA based systems. The topochemical reactivity of the system is modified depending on the coformer used and correlates with the structural parameters. Crystallisation of 1 with 4,4′-azopyridine (2), 4,4′-bipyridyl (3), and trans-1,2-bis(4-pyridyl)ethylene (4) results in unreactive 2 : 1 cocrystals or a salt in the case of 4,4′-bipiperidine (5). However, salt formation with morpholine (6), diethylamine (7), and n-butylamine (8), results in highly photoreactive salts 12·7 and 1·8 whose reactivity can be explained using topochemical criteria. The salt 1·6 is also highly photoreactive and is compared to a model morpholinium butanoate salt. Resonance Raman spectroscopy reveals structural details of the photopolymer including its conformational disorder in comparison to less photoactive alkali metal salts and the extent of solid state conversion can be monitored by CP-MAS NMR spectroscopy. We also report an unusual catalysis in which amine evaporation from photopolymerised PCDA ammonium salts effectively acts as a catalyst for polymerisation of PCDA itself. The new photoreactive salts exhibit more reactivity but decreased conjugation compared to the commercial lithium salt and are of considerable practical potential in terms of tunable colours and greater range in UV, X-ray, and γ-ray dosimetry applications.

Journal ArticleDOI
TL;DR: Regioselective routes are described for convenient preparation of novel piperazine/morpholine substituted quinoline derivatives that have the potential of drug candidates to treat of some diseases including glaucoma, epilepsy, Alzheimer’s disease (AD), leukemia, and type-2 diabetes mellitus (T2DM).

Journal ArticleDOI
25 Jul 2020
TL;DR: It was found that the presence of saturated heterocycles from the amine molecule, 1-methyl piperazine and morpholine, respectively, contributes to an increased biological activity, compared to aromatic amino analogs, diphenylamino-, 4-nitroamino- and 4-aminobenzoic acid.
Abstract: The tri-component synthesis of novel chiral benzimidazole Mannich bases, by reaction between benzimidazole, aqueous 30% formaldehyde and an amine, the biological evaluation and DFT studies of the new compounds are reported here. The 1H-NMR, 13C-NMR, FTIR spectra and elemental analysis confirm the structures of the new compounds. All synthesized compounds were screened by qualitative and quantitative methods for their in vitro antibacterial activity against 4 bacterial strains. DFT studies were accomplished using GAMESS 2012 software and HOMO–LUMO analysis allowed the calculation of electronic and structural parameters of the chiral Mannich bases. The geometry of 1-methylpiperazine, the cumulated Mullikan atomic charges of the two heteroatoms and of the methyl, and the value of the global electrophilicity index (ω = 0.0527) of the M-1 molecule is correlated with its good antimicrobial activity. It was found that the presence of saturated heterocycles from the amine molecule, 1-methyl piperazine and morpholine, respectively, contributes to an increased biological activity, compared to aromatic amino analogs, diphenylamino-, 4-nitroamino- and 4-aminobenzoic acid. The planarity of the molecules, specific bond lengths and localization of HOMO–LUMO orbitals is responsible for the best biological activities of the compounds.

Journal ArticleDOI
TL;DR: In this paper, the role of axial nitrogen-donor ligands was explored and the photophysical properties of these complexes were investigated in detail, revealing that they are photoluminescent in air-equilibrated pH 7.4 phosphate-buffered saline with quantum yields ranging from 1.7 to 3.1%.

Journal ArticleDOI
TL;DR: The results are discussed and compared with those of the pyridine-based compounds, which provides important insights into the parameters that govern the magnetic behavior of such one-dimensional coordination polymers.
Abstract: Reaction of Co(NCS)2 with different coligands leads to the formation of three compounds with the general composition [Co(NCS)2(L)2]n (L = aniline (1), morpholine (2), and ethylenethiourea (3)) In

Journal ArticleDOI
TL;DR: Molecular docking experiments showed a good correlation between the experimental activity and the calculated binding affinity to human inducible nitric oxide synthase, the enzymatic target for the anti-inflammatory response.

Journal ArticleDOI
TL;DR: Morpholine-2,5-diones are increasingly attractive monomers derived from amino-acids whose copolymerization with other monomers produces interesting biodegradable materials as mentioned in this paper.
Abstract: Morpholine-2,5-diones are increasingly attractive monomers derived from amino-acids whose copolymerization with other monomers produces interesting biodegradable materials. In this study, the rapid...

Journal ArticleDOI
TL;DR: In this paper, a new morpholine-based ligand was prepared from condensation of a branched amine containing morpholine, N1-(3-morpholinopropyl)-N1-((pyridine-2-yl)methyl)ethane-1,2-diamine (1), and salicylaldehyde.

Journal ArticleDOI
TL;DR: The result shows that synthesized compounds have good radical scavenging activity against DPPH radical and antimicrobial activities of synthesized ligand and its complexes have been tested against selected bacterial and fungal species.
Abstract: Copper(II) and zinc(II) complexes of the type [ML(AcO)2.H2O] were synthesized from bidentate-morpholine based Schiff base ligand (L - morpholinopropylimino)methyl)-6-methoxyphenol). The prepared li...

Journal ArticleDOI
TL;DR: Results revealed that para-bromo and fluoro substituted N-phenylselenazolo[4,5-d]pyrimidines containing pyrrolidine moiety exhibited similar and six times higher potency for death and blocking of Candida albicans fungus than ketoconazole, respectively.
Abstract: A straightforward strategy for the efficient synthesis of multi-functionalized 7-imino[1,3]selenazolo[4,5-d]pyrimidine-5(4H)-thiones bearing an incorporated N-phenylmethanethioamide fragment from the heteroannulation of several 2,4,5-trisubstituted 1,3-selenazoles with readily accessible phenyl isothiocyanates was established in boiling pyridine. To enrich the biological profile of the newly synthesized fused heterocyclic scaffold, some noted pharmacophores such as pyrrolidine, piperidine, morpholine, fluorine, and bromine were inserted into the framework. Inhibitory activities of the selenium-containing heterocycles were assessed against DPPH and Candida albicans. Antioxidant activities as IC50 values were observed in the range of 0.010–0.063 mM. Results revealed that 6-phenyl-substituted selenazolopyrimidines bearing C2-pyrrolidine and C2-piperidine both with IC50 value of 0.010 mM were superlative amongst others. Being far superior to ascorbic acid (IC50 = 0.022 mM), 4-fluorophenyl-substituted compounds bearing 2-morpholine residual (IC50 = 0.014 mM), and 2-piperidine (IC50 = 0.019 mM) were ranked in the second place and third place of antioxidant efficacy, respectively. Moreover, para-bromo and fluoro substituted N-phenylselenazolo[4,5-d]pyrimidines containing pyrrolidine moiety exhibited similar and six times higher potency for death and blocking of Candida albicans fungus than ketoconazole, respectively. Consequently, some of these selenazolopyrimidines are promising anti-Candida albicans as well as antioxidant lead compounds which can be used in the treatment of candidiasis, cancer, and neurodegenerative and diabetes diseases.


Journal ArticleDOI
TL;DR: Using the structure based drug design strategy, a library of hydroxylamine derivatives of morpholine were designed and synthesized as small molecule inhibitors of MARK4, finding that molecule 32 caused death of cancerous cells through the mechanism of apoptosis.
Abstract: Microtubule affinity-regulating kinase 4 (MARK4) is a serine/threonine kinase involved in the phosphorylation of MAP proteins that regulates microtubule dynamics and abets tumor progression by participating in oncogenic signaling pathways. It is overexpressed in multiple human malignancies and no drug is available for this potential therapeutic target at present. Therefore, using the structure based drug design strategy, a library of hydroxylamine derivatives of morpholine were designed and synthesized as small molecule inhibitors of MARK4. Compound 32 having the CF3 group at the ortho position of the phenyl ring tethered with the >CNOH core and the hinge binder morpholine component was found to be a potent and selective inhibitor of MARK4 over thirty other serine-threonine kinases. Study of cell viability and compound induced morphological changes in MCF-7 cancer cells discovered that molecule 32 caused death of cancerous cells through the mechanism of apoptosis. Compound 32 may be transported and delivered to the target site through the blood stream, and has promising antioxidant potential. Such bio-active molecules could serve as optimized lead candidates in drug discovery for cancer treatment through MARK4 inhibition.

Journal ArticleDOI
TL;DR: This protocol solves the limitation of acyclic 1,3-dicarbonyl compounds by one-pot synthesis of tetrahydroquinolines, featuring operational simplicity, broadly applicable substrates, and metal- and acid-free conditions with EtOH as a hydrogen-bonding donor.
Abstract: The hydrogen-bonding-assisted construction of tetrahydroquinolines decorated with structurally diverse 3,3′-difunctional groups has been realized via a hydride transfer-involved three-step cascade reaction in the presence of morpholine. This protocol solves the limitation of acyclic 1,3-dicarbonyl compounds by one-pot synthesis of tetrahydroquinolines, featuring operational simplicity, broadly applicable substrates, and metal- and acid-free conditions with EtOH as a hydrogen-bonding donor.

Journal ArticleDOI
TL;DR: A new non-natural β-amino acid, named 3-Ar-β-Morph, was designed and synthesized via a regio- and diastereoselective Pd-catalyzed C(sp3)H-arylation of the corresponding 2S,6S-(6-methoxymorpholin-2-yl)carboxylic acid, readily available from glucose.

Journal ArticleDOI
TL;DR: Cell cycle analysis, in vitro tubulin polymerization assay, and tubulin imaging in cells indicated that the anticancer activity of thiophenol derivative is associated with its ability to inhibit microtubule formation.

Journal ArticleDOI
TL;DR: All the ligands and complexes exhibited cytotoxicity to the normal human cell line; human embryonic kidney cells (HEK293), but they had good compatibility with the human red blood cells (RBCs) at 32 μg/mL.

Journal ArticleDOI
TL;DR: The Lineweaver-Burk plots analysis displayed that the inhibition type of 4k was the competitive mode like acarbose as standard, and Electron-donating groups such as methyl and methoxy on the phenyl ring played an important role in the inhibition.

Journal ArticleDOI
TL;DR: The application of kynurenic acid (KYNA) as an electron-rich aromatic system in the modified Mannich reaction has been examined and the dominant tautomer form of KYNA derivatives was determined.
Abstract: The application of kynurenic acid (KYNA) as an electron-rich aromatic system in the modified Mannich reaction has been examined. The extension possibility of the reaction was tested by using amines occurring in a number of bioactive products, such as morpholine, piperidine, or N-methylpiperazine and aldehydes of markedly different reactivities, like formaldehyde and benzaldehyde. The influence of substituents attached to position 3 on the aminoalkylation was also investigated. Thus, reactions of 3-carbamoyl-substituted precursors with tertiary amine containing side-chains were also tested to afford new KYNA derivatives with two potential cationic centers. By means of NMR spectroscopic measurements, supported by DFT calculations, the dominant tautomer form of KYNA derivatives was also determined.

Journal ArticleDOI
TL;DR: The series of new 4-substituted picolinohydrazonamides synthesized and evaluated for tuberculostatic activity revealed low cytotoxicity of compound 15, characterized by the selectivity of antimicrobial activity.

Journal ArticleDOI
TL;DR: In this paper, two tetra- or octa-substituted zinc(II) phthalocyanines (1 and 2) bearing 3-(morpholinomethyl)phenyl groups were synthesized via Suzuki-Miyaura coupling method.
Abstract: Two new tetra- or octa-substituted zinc(II) phthalocyanines (1 and 2) bearing 3-(morpholinomethyl)phenyl groups were synthesized via Suzuki-Miyaura coupling method. These phthalocyanines (1 and 2) were converted to their water-soluble derivatives (1Q and 2Q) by quaternization of nitrogen atoms on the morpholine groups. The photochemical and photophysical properties of the non-ionic zinc(II) phthalocyanines (1 and 2) were explored in DMSO. On the other hand, these properties of the quaternized cationic derivatives (1Q and 2Q) were studied in both DMSO and aqueous solutions for determination of their photosensitizing capabilities in photodynamic therapy. The ct-DNA interaction of synthesized 1Q and 2Q were investigated and binding constants were found as 6.3 × 104 and 1.5 × 105 M, respectively. The binding constant values were found at similar levels of ethidium bromide (EB), which is a well-known intercalator. The spontaneous and exothermic nature of binding mechanisms were proved according to the calculated thermodynamic constants. Strong interactions of 1Q and 2Q with ct-DNA were also found with EB displacement assay and gel electrophoresis. Additionally, the bovine serum albumin (BSA) binding behavior of the new compounds (1Q and 2Q) were determined in water solution to verify the transporting capability of these phthalocyanines in the circulatory system and these values were found as 7.0 × 105 and 1.6 × 107 M−1 for 1Q and 2Q, respectively.