Benzothieno[3,2‐<i>e</i>][1,2,4]triazolo[4,3‐<i>c</i>]pyrimidines: Synthesis, Characterization, Antimicrobial Activity, and Incorporation into Solid Lipid Nanoparticles

Panchamukhi, Shridhar I.; Mulla, Jameel Ahmed S.; Shetty, Nitinkumar S.; Khazi, Mohammed Iqbal; Khan, Ashraf Y.; Kalashetti, M. B.; Khazi, Imitiyaz Ahmed M.

doi:10.1002/ardp.201000227

Cited by 10 publications

(6 citation statements)

References 34 publications

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“…El-Sayed and Faddaet: Synthesis and Cytotoxic Activity of Some Novel ... Cyclization of compound 16 in acetic anhydride afforded the corresponding 7-(chloromethyl)-1,3-dimethyl-8-(pyridin-2-yl)thieno[2,3-d:4,5-d']dipyrimidine-2,4,9-(1H,3H,8H)-trione (17). The assignment of structure 17 was supported by elemental analysis and spectral data.…”

Section: Methodsmentioning

confidence: 99%

“…[2][3][4] On the other hand, the classes of tricyclic compounds bearing thienopyrimidine scaffolds have been the focus of great interest because of their pharmacological activities, such as antitumor, [5][6][7][8][9] antiallergic, anti-inflammatory, analgesic, antifungal and antibacterial activities. [10][11][12][13][14][15][16][17][18][19][20] Consequently, thienopyrimidines have become an important class of compounds in drug discovery programs and the medicinal chemistry. [21][22][23][24][25] In continuation of our previous work on biologically active nitrogen and sulfur heterocycles, [26][27][28][29] it was of interest to synthesize some novel thieno [2,3-d:4,5-d`]dipyrimidine derivatives and evaluate these compounds for their cytotoxic activity.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

El‐Sayed¹,

Fadda²

2018

ACSi

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Synthesis of some novel tricyclic compounds bearing thienodipyrimidine moiety by the reaction of ethyl 6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,2-d]pyrimidine-7-carboxylate (1) with different types of aromatic amines to give the corresponding carboxamide derivatives 2-11, which cyclized with triethyl orthoformate in acetic anhydride to afford thieno[2,3-d:4,5-d']dipyrimidine derivatives 12-15 is described. Similarly, thieno[2,3-d:4,5-d']dipyrimidine derivative 17 was also prepared via the reaction of carboxamide derivative 2 with chloroacetyl chloride in chloroform to give thieno[3,2-d]pyrimidine-7-carboxamide derivative 16, followed by a cyclization in boiling acetic anhydride. The structure of these compounds was confirmed on the basis of their spectral and analytical data such as IR, 1 H-NMR, 13 C-NMR spectroscopy and mass spectral data. The synthesized compounds were screened for their cytotoxic activity.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

El‐Sayed¹,

Fadda²

2018

ACSi

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“…Forty-three mo lecules belonging to thienopyrimidine derivatives as antibacterial were taken fro m the literature 8,9,16,17 and used for QSAR analysis. The above reported series of thienopyrimidine derivatives showed wide variat ions in their structures and potency profiles.…”

Section: Data Setmentioning

confidence: 99%

Rational Design of Antibacterial Thienopyrimidines by 2d-Qsar Study

Mulla¹,

Palkar²,

Maddi³

et al. 2012

J. Drug Delivery Ther.

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Available online 15 Ma rch 2012 ABS TRACTQSAR studies were performed on a set of 43 analogs of thienopyrimidine using V-Life M olecular Design Suite (M DS 3.5) QSAR plus module by using M ultiple Linear Regression (M LR) and Partial Least Squares (PLS) Regression methods against a gram positive (S.aureus) and a gram negative (E.coli) bacteria. M LR method has shown a very promising prediction results in both S.aureus and E.coli. QSAR model was generated by a training set of 34 molecules with correlation coefficient (r 2 ) of 0.9849, 0.8719, significant cross validated correlation coefficient (q 2 ) of 0.8881, 0.7811 and F test of 40.4301, 40.4768 respectively . In the selected descriptors, alignment independent descriptors such as T_C_C_7, T_N_O_3, T_2_N_1, T_N_O_1, T_O_O_7 and T_N_Cl_4 were the most important descriptors in predicting antibacterial activity.

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“…Nanoparticles have the advantages of biocompatibility, protecting drugs from the inactivation of external conditions, sustained release and the efficient permeation through the skin, have been demonstrated for their beneficial effect in the treatment of skin disorders 4,5 .…”

Section: Introductionmentioning

confidence: 99%

Untitled

2019

IJPSR

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Pyrazolines were prepared from the corresponding chalcones by using isonicotinylhydrazine as cyclizing agent. The synthesized compounds were characterized by spectral data and screened for antimicrobial activity. Insilico studies of physiochemical and drug-like properties revealed that these compounds have good bioavailability and drug-likeness properties. Compound PZ2 which exhibited good antimicrobial activity was incorporated into polymeric nanoparticles using PLGA polymer by solvent evaporation method. The prepared nanoparticles were characterized by particle size, entrapment efficiency (EE%), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and in-vitro release studies. Prepared nanoparticles were incorporated into different hydrogel systems, which were prepared by using Carbopol 934 and HPMC in different concentrations ratio 2:1, 1:1 & 1:2. Hydrogel formulations were evaluated for drug content, spreadability, viscosity and drug release studies. Hence, the studies confirmed that entrapment of pyrazolthe ine as antimicrobial drugs in nanoparticle systems has found to be an inventive alternative that improves therapeutic effectiveness and curtails undesirable side effects of the drugs. Further, incorporation of pyrazoline nanoparticles into hydrogel provides an additional benefit of advanced permeation features of antimicrobial constituents for transdermal application.

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Benzothieno[3,2‐e][1,2,4]triazolo[4,3‐c]pyrimidines: Synthesis, Characterization, Antimicrobial Activity, and Incorporation into Solid Lipid Nanoparticles

Cited by 10 publications

References 34 publications

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

Rational Design of Antibacterial Thienopyrimidines by 2d-Qsar Study

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