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  1. Fulltext Multi-method evaluation of a 2-(1,3,4-thiadiazole-2-yl)pyrrolidine corrosion inhibitor for mild steel in HCl: combining gravimetric, electrochemical, and DFT approaches
    Al-Amiery A, Isahak WNRW, Al-Azzawi WK
    Sci Rep, 2023 Jun 16;13(1):9770.
    PMID: 37328536 DOI: 10.1038/s41598-023-36252-8
    The corrosion inhibition properties of 2-(1,3,4-thiadiazole-2-yl)pyrrolidine (2-TP) on mild steel in a 1 M HCl solution were investigated using weight loss, potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and open circuit potential (OCP) measurements. In addition, DFT calculations were performed on 2-TP. The polarization curves revealed that 2-TP is a mixed-type inhibitor. The results indicate that 2-TP is an effective inhibitor for mild steel corrosion in a 1.0 M HCl solution, with an inhibition efficiency of 94.6% at 0.5 mM 2-TP. The study also examined the impact of temperature, revealing that the inhibition efficiency increases with an increasing concentration of 2-TP and decreases with a rise in temperature. The adsorption of the inhibitor on the mild steel surface followed the Langmuir adsorption isotherm, and the free energy value indicated that the adsorption of 2-TP is a spontaneous process that involves both physical and chemical adsorption mechanisms. The DFT calculations showed that the adsorption of 2-TP on the mild steel surface is mainly through the interaction of the lone pair of electrons on the nitrogen atom of the thiadiazole ring with the metal surface. The results obtained from the weight loss, potentiodynamic polarization, EIS and OCP measurements were in good agreement with each other and confirmed the effectiveness of 2-TP as a corrosion inhibitor for mild steel in 1.0 M HCl solution. Overall, the study demonstrates the potential use of 2-TP as a corrosion inhibitor in acid environments.
    Matched MeSH terms: Thiadiazoles*
  2. Fulltext The use of umbelliferone in the synthesis of new heterocyclic compounds
    Al-Amiery AA, Musa AY, Kadhum AA, Mohamad AB
    Molecules, 2011 Aug 10;16(8):6833-43.
    PMID: 21832973 DOI: 10.3390/molecules16086833
    New coumarin derivatives, namely 7-[(5-amino-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one, 5-[(2-oxo-2H-chromen-7-yloxy)methyl]-1,3,4-thiadiazol-2(3H)-one, 2-[2-(2-oxo-2H-chromen-7-yloxy)acetyl]-N-phenylhydrazinecarbothioamide, 7-[(5-(phenylamino)-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one and 7-[(5-mercapto-4-phenyl-4H-1,2,4-triazol-3-yl)methoxy]-2H-chromen-2-one were prepared starting from the natural compound umbelliferone. The newly synthesized compounds were characterized by elemental analysis and spectral studies (IR, ¹H-NMR and ¹³C-NMR).
    Matched MeSH terms: Thiadiazoles/chemistry
  3. Fulltext PFO-DBT:MEH-PPV:PC₇₁BM ternary blend assisted platform as a photodetector
    Zafar Q, Ahmad Z, Sulaiman K
    Sensors (Basel), 2015;15(1):965-78.
    PMID: 25574936 DOI: 10.3390/s150100965
    We present a ternary blend-based bulk heterojunction ITO/PEDOT:PSS/PFO-DBT: MEH-PPV:PC71BM/LiF/Al photodetector. Enhanced optical absorption range of the active film has been achieved by blending two donor components viz. poly[2,7-(9,9-di-octyl-fluorene)-alt-4,7-bis(thiophen-2-yl)benzo-2,1,3-thiadiazole] (PFO-DBT) and poly(2-methoxy-5(2'-ethylhexyloxy) phenylenevinylene (MEH-PPV) along with an acceptor component, i.e., (6,6)-phenyl-C71 hexnoic acid methyl ester. The dependency of the generation rate of free charge carriers in the organic photodetector (OPD) on varied incident optical power density was investigated as a function of different reverse biasing voltages. The photocurrent showed significant enhancement as the intensity of light impinging on active area of OPD is increased. The ratio of Ilight to Idark of fabricated device at -3 V was ~3.5 × 10(4). The dynamic behaviour of the OPD under on/off switching irradiation revealed that sensor exhibits quick response and recovery time of ∼800 ms and 500 ms, respectively. Besides reliability and repeatability in the photoresponse characteristics, the cost-effective and eco-friendly fabrication is the added benefit of the fabricated OPD.
    Matched MeSH terms: Thiadiazoles
  4. Synthesis and biological evaluation of novel substituted 1,3,4-thiadiazole and 2,6-di aryl substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives
    Chandrakantha B, Isloor AM, Shetty P, Fun HK, Hegde G
    Eur J Med Chem, 2014 Jan;71:316-23.
    PMID: 24321835 DOI: 10.1016/j.ejmech.2013.10.056
    A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2-yl]-2,2-dimethyl-propionamide 4 (a-l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)-3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a-l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-ylamine. The synthesized compounds were characterized by IR, NMR, mass spectral and elemental analysis. All the compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by well plate method (zone of inhibition). Compounds 4a, 4c and 6e, 6g displayed appreciable activity at the concentration 0.5-1.0 mg/mL.
    Matched MeSH terms: Thiadiazoles/chemical synthesis; Thiadiazoles/pharmacology*; Thiadiazoles/chemistry*
  5. Synthesis of novel quinoline-based thiadiazole, evaluation of their antileishmanial potential and molecular docking studies
    Almandil NB, Taha M, Rahim F, Wadood A, Imran S, Alqahtani MA, et al.
    Bioorg Chem, 2019 04;85:109-116.
    PMID: 30605884 DOI: 10.1016/j.bioorg.2018.12.025
    New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, 1H NMR and 13C NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC50 values in the range of 0.04 ± 0.01 to 5.60 ± 0.21 µM showed tremendously potent inhibition as compared to the standard pentamidine with IC50 value 7.02 ± 0.09 µM. Analogs 11, 14, 15 and 20 with IC50 8.20 ± 0.35, 9.20 ± 0.40, 7.20 ± 0.20 and 9.60 ± 0.40 µM respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.
    Matched MeSH terms: Thiadiazoles/chemical synthesis; Thiadiazoles/metabolism; Thiadiazoles/pharmacology*
  6. Synthesis and biological activity of oxadiazole and triazolothiadiazole derivatives as tyrosinase inhibitors
    Lam KW, Syahida A, Ul-Haq Z, Abdul Rahman MB, Lajis NH
    Bioorg Med Chem Lett, 2010 Jun 15;20(12):3755-9.
    PMID: 20493688 DOI: 10.1016/j.bmcl.2010.04.067
    A series of 16 oxadiazole and triazolothiadiazole derivatives were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. Five derivatives were found to display high inhibition on the tyrosinase activity ranging from 0.87 to 1.49 microM. Compound 5 exhibited highest tyrosinase inhibitory activity with an IC(50) value of 0.87+/-0.16 microM. The in silico protein-ligand docking using AUTODOCK 4.1 was successfully performed on compound 5 with significant binding energy value of -5.58 kcal/mol. The docking results also showed that the tyrosinase inhibition might be due to the metal chelating effect by the presence of thione functionality in compounds 1-5. Further studies revealed that the presence of hydrophobic group such as cycloamine derivatives played a major role in the inhibition. Piperazine moiety in compound 5 appeared to be involved in an extensive hydrophobic contact and a 2.9A hydrogen bonding with residue Glu 182 in the active site.
    Matched MeSH terms: Thiadiazoles/chemical synthesis; Thiadiazoles/pharmacology; Thiadiazoles/chemistry*
  7. Synthesis of indole-based-thiadiazole derivatives as a potent inhibitor of α-glucosidase enzyme along with in silico study
    Alomari M, Taha M, Rahim F, Selvaraj M, Iqbal N, Chigurupati S, et al.
    Bioorg Chem, 2021 03;108:104638.
    PMID: 33508679 DOI: 10.1016/j.bioorg.2021.104638
    A series of nineteen (1-19) indole-based-thiadiazole derivatives were synthesized, characterized by 1HNMR, 13C NMR, MS, and screened for α-glucosidase inhibition. All analogs showed varied α-glucosidase inhibitory potential with IC50 value ranged between 0.95 ± 0.05 to 13.60 ± 0.30 µM, when compared with the standard acarbose (IC50 = 1.70 ± 0.10). Analogs 17, 2, 1, 9, 7, 3, 15, 10, 16, and 14 with IC50 values 0.95 ± 0.05, 1.10 ± 0.10, 1.30 ± 0.10, 1.60 ± 0.10, 2.30 ± 0.10, 2.30 ± 0.10, 2.80 ± 0.10, 4.10 ± 0.20 and 4.80 ± 0.20 µM respectively showed highest α-glucosidase inhibition. All other analogs also exhibit excellent inhibitory potential. Structure activity relationships have been established for all compounds primarily based on substitution pattern on the phenyl ring. Through molecular docking study, binding interactions of the most active compounds were confirmed. We further studied the kinetics study of analogs 1, 2, 9 and 17 and found that they are Non-competitive inhibitors.
    Matched MeSH terms: Thiadiazoles/chemical synthesis; Thiadiazoles/pharmacology*; Thiadiazoles/chemistry
  8. Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives
    Taha M, Tariq Javid M, Imran S, Selvaraj M, Chigurupati S, Ullah H, et al.
    Bioorg Chem, 2017 10;74:179-186.
    PMID: 28826047 DOI: 10.1016/j.bioorg.2017.08.003
    α-Amylase is a target for type-2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized thiadiazole quinoline analogs (1-30), characterized by different spectroscopic techniques such as 1HNMR and EI-MS and screened for α-amylase inhibitory potential. Thirteen analogs 1, 2, 3, 4, 5, 6, 22, 23, 25, 26, 27, 28 and 30 showed outstanding α-amylase inhibitory potential with IC50 values ranges between 0.002±0.60 and 42.31±0.17μM which is many folds better than standard acarbose having IC50 value 53.02±0.12μM. Eleven analogs 7, 9, 10, 11, 12, 14, 15, 17, 18, 19 and 24 showed good to moderate inhibitory potential while seven analogs 8, 13, 16, 20, 21 and 29 were found inactive. Our study identifies novel series of potent α-amylase inhibitors for further investigation. Structure activity relationship has been established.
    Matched MeSH terms: Thiadiazoles/chemical synthesis; Thiadiazoles/pharmacology*; Thiadiazoles/chemistry
  9. Synthesis, in vitro α-glucosidase inhibitory potential and molecular docking study of thiadiazole analogs
    Javid MT, Rahim F, Taha M, Rehman HU, Nawaz M, Wadood A, et al.
    Bioorg Chem, 2018 08;78:201-209.
    PMID: 29597114 DOI: 10.1016/j.bioorg.2018.03.022
    α-Glucosidase is a catabolic enzyme that regulates the body's plasma glucose levels by providing energy sources to maintain healthy functioning. 2-Amino-thiadiazole (1-13) and 2-amino-thiadiazole based Schiff bases (14-22) were synthesized, characterized by 1H NMR and HREI-MS and screened for α-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of α-glucosidase inhibitory potential with IC50 values ranging between 2.30 ± 0.1 to 38.30 ± 0.7 μM, when compare with standard drug acarbose having IC50 value of 39.60 ± 0.70 μM. Among the series eight derivatives 1, 2, 6, 7, 14, 17, 19 and 20 showed outstanding α-glucosidase inhibitory potential with IC50 values of 3.30 ± 0.1, 5.80 ± 0.2, 2.30 ± 0.1, 2.70 ± 0.1, 2.30 ± 0.1, 5.50 ± 0.1, 4.70 ± 0.2, and 5.50 ± 0.2 μM respectively, which is many fold better than the standard drug acarbose. The remaining analogs showed good to excellent α-glucosidase inhibition. Structure activity relationship has been established for all compounds. The binding interactions of these compounds were confirmed through molecular docking.
    Matched MeSH terms: Thiadiazoles/pharmacology*; Thiadiazoles/chemistry
  10. Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
    Salar U, Taha M, Ismail NH, Khan KM, Imran S, Perveen S, et al.
    Bioorg Med Chem, 2016 Apr 15;24(8):1909-18.
    PMID: 26994638 DOI: 10.1016/j.bmc.2016.03.020
    Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50=2.16±0.01-58.06±1.60μM as compare to standard d-saccharic acid 1,4-lactone (IC50=48.4±1.25μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques (1)H, (13)C NMR, and EIMS.
    Matched MeSH terms: Thiadiazoles
  11. Fulltext Determining the Effect of Centrifugal Force on the Desired Growth and Properties of PCPDTBT as p-Type Nanowires
    Doris M, Aziz F, Alhummiany H, Bawazeer T, Alsenany N, Mahmoud A, et al.
    Nanoscale Res Lett, 2017 Dec;12(1):67.
    PMID: 28116608 DOI: 10.1186/s11671-017-1851-0
    In this study, low-bandgap polymer poly{[4,4-bis(2-ethylhexyl)-cyclopenta-(2,1-b;3,4-b')dithiophen]-2,6-diyl-alt-(2,1,3-benzothiadiazole)-4,7-diyl} (PCPDTBT) nanostructures have been synthesized via a hard nanoporous alumina template of centrifugal process. Centrifuge has been used to infiltrate the PCPDTBT solution into the nanoporous alumina by varying the rotational speeds. The rotational speed of centrifuge is directly proportional to the infiltration force that penetrates into the nanochannels of the template. By varying the rotational speed of centrifuge, different types of PCPDTBT nanostructures are procured. Infiltration force created during the centrifugal process has been found a dominant factor in tuning the morphological, optical, and structural properties of PCPDTBT nanostructures. The field emission scanning electron microscopy (FESEM) images proved the formation of nanotubes and nanowires. The energy-dispersive X-ray spectroscope (EDX) analysis showed that the nanostructures were composed of PCPDTBT with complete dissolution of the template.
    Matched MeSH terms: Thiadiazoles
  12. Induction, Subculture Cycle, and Regeneration of Callus in Safed Musli (Chlorophytum borivilianum) using Different Types of Phytohormones
    Nakasha JJ, Sinniah UR, Kemat N, Mallappa KS
    Pharmacogn Mag, 2016 Jul;12(Suppl 4):S460-S464.
    PMID: 27761075
    BACKGROUND: Chlorophytum borivilianum is an industrially valued medicinal crop. Propagation through seeds is not feasible because of low germination percentage and long dormancy period. Therefore, callus culture and plant regeneration can be an alternative to improve this crop production. Also, callus can serve as an alternative source of bioactive compounds.

    OBJECTIVE: To evaluate the effect of different phytohormones on callus induction, subculture cycle, and regeneration studies of callus in C. borivilianum.

    MATERIALS AND METHODS: Young shoot buds of C. borivilianum were inoculated on Murashige and Skoog medium fortified with 3% sucrose and different concentrations (0, 1, 5, 10, and 15 mg/L) of either naphthalene acetic acid or 2,4-dichlorophenoxyacetic acid or indole-3-acetic acid and callus induction was evaluated up to four subcultures cycles. Shoot regeneration from callus was studied on Murashige and Skoog media fortified with 6-benzylaminopurine andkinetin or thidiazuron at varied levels (0, 0.5, 1, 2, and 3 mg/L). Microshoots were rooted on Murashige and Skoog media supplemented with 1.0 mg/L indole-3-butyric acid and plantlets were acclimatized before transferred to the natural conditions.

    RESULTS: Callus induction was better evidenced on Murashige and Skoog media containing 5 mg/L 2,4-dichlorophenoxyacetic acid up to fourth subculture. Callus differentiated into shoots on Murashige and Skoog media fortified with 6-benzylaminopurine or kinetin, whereas thidiazuron completely failed to regenerate shoots. Furthermore, microshoots rooted on 1.0 mg/L indole-3-butyric acid containing Murashige and Skoog media. The rooted plantlets were successfully acclimatized and established in soil with 88.3% survivability.

    CONCLUSION: The type of auxins played an important role in inducing callus tissue from shoot bud explants of Safed musli. In future, this in vitro protocol could benefit in crop improvement programs and serve as a new source of bioactive compounds from Safed musli callus tissue for various therapeutic applications.

    SUMMARY: Explants de-differentiated to form callus on Murashige and Skoog media containing 5 mg/L 2,4-D up to fourth subculture.Callus re-differentiated into shoots on Murashige and Skoog media fortified with 0.5 mg/L BAP.In vitro rooting of shoots was achieved on 1.0 mg/L IBA containing Murashige and Skoog media.The rooted plantlets were successfully acclimatized and established in soil with 88.3% survivability. Abbreviations used: MS: Murashige and Skoog, NAA: naphthalene acetic acid, 2,4-D: 2,4-dichlorophenoxyacetic acid, IAA: indole-3-acetic acid, BAP: 6-benzylaminopurine, Kn: Kinetin, TDZ: thidiazuron, IBA: indole-3-butyric acid, RCBD: Randomized Complete Block Design, DMRT: Duncan's Multiple Range Test.

    Matched MeSH terms: Thiadiazoles
  13. Fulltext Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor
    Taha M, Rahim F, Khan AA, Anouar EH, Ahmed N, Shah SAA, et al.
    Sci Rep, 2020 05 14;10(1):7969.
    PMID: 32409737 DOI: 10.1038/s41598-020-64729-3
    The current study describes synthesis of diindolylmethane (DIM) derivatives based-thiadiazole as a new class of urease inhibitors. Diindolylmethane is natural product alkaloid reported to use in medicinal chemistry extensively. Diindolylmethane-based-thiadiazole analogs (1-18) were synthesized and characterized by various spectroscopic techniques 1HNMR, 13C-NMR, EI-MS and evaluated for urease (jack bean urease) inhibitory potential. All compounds showed excellent to moderate inhibitory potential having IC50 value within the range of 0.50 ± 0.01 to 33.20 ± 1.20 µM compared with the standard thiourea (21.60 ± 0.70 µM). Compound 8 (IC50 = 0.50 ± 0.01 µM) was the most potent inhibitor amongst all derivatives. Structure-activity relationships have been established for all compounds. The key binding interactions of most active compounds with enzyme were confirmed through molecular docking studies.
    Matched MeSH terms: Thiadiazoles/chemistry*
  14. Design, synthesis, in vitro evaluation, molecular docking and ADME properties studies of hybrid bis-coumarin with thiadiazole as a new inhibitor of Urease
    Alomari M, Taha M, Imran S, Jamil W, Selvaraj M, Uddin N, et al.
    Bioorg Chem, 2019 11;92:103235.
    PMID: 31494327 DOI: 10.1016/j.bioorg.2019.103235
    Hybrid bis-coumarin derivatives 1-18 were synthesized and evaluated for their in vitro urease inhibitory potential. All compounds showed outstanding urease inhibitory potential with IC50 value (The half maximal inhibitory concentration) ranging in between 0.12 SD 0.01 and 38.04 SD 0.63 µM (SD standard deviation). When compared with the standard thiourea (IC50 = 21.40 ± 0.21 µM). Among these derivatives, compounds 7 (IC50 = 0.29 ± 0.01), 9 (IC50 = 2.4 ± 0.05), 10 (IC50 = 2.25 ± 0.05) and 16 (IC50 = 0.12 ± 0.01) are better inhibitors of the urease compared with thiourea (IC50 = 21.40 ± 0.21 µM). To find structure-activity relationship molecular docking as well as absorption, distribution, metabolism, and excretion (ADME) studies were also performed. Various spectroscopic techniques like 1H NMR, 13C NMR, and EI-MS were used for characterization of all synthesized analogs. All compounds were tested for cytotoxicity and found non-toxic.
    Matched MeSH terms: Thiadiazoles/chemistry*
  15. Optimization of in vitro regeneration and Agrobacterium tumefaciens-mediated transformation with heat-resistant cDNA in Brassica oleracea subsp. italica cv. Green Marvel
    Ravanfar SA, Aziz MA, Saud HM, Abdullah JO
    Curr Genet, 2015 Nov;61(4):653-63.
    PMID: 25986972 DOI: 10.1007/s00294-015-0494-x
    An efficient system for shoot regeneration and Agrobacterium tumefaciens-mediated transformation of Brassica oleracea cv. Green Marvel cultivar is described. This study focuses on developing shoot regeneration from hypocotyl explants of broccoli cv. Green Marvel using thidiazuron (TDZ), zeatin, and kinetin, the optimization of factors affecting Agrobacterium-mediated transformation of the hypocotyl explants with heat-resistant cDNA, followed by the confirmation of transgenicity of the regenerants. High shoot regeneration was observed in 0.05-0.1 mg dm(-3) TDZ. TDZ at 0.1 mg dm(-3) produced among the highest percentage of shoot regeneration (96.67 %) and mean number of shoot formation (6.17). The highest percentage (13.33 %) and mean number (0.17) of putative transformant production were on hypocotyl explants subjected to preculture on shoot regeneration medium (SRM) with 200 µM acetosyringone. On optimization of bacterial density and inoculation time, the highest percentage and mean number of putative transformant production were on hypocotyl explants inoculated with a bacterial dilution of 1:5 for 30 min. Polymerase chain reaction (PCR) assay indicated a transformation efficiency of 8.33 %. The luciferase assay showed stable integration of the Arabidopsis thaliana HSP101 (AtHSP101) cDNA in the transgenic broccoli regenerants. Three out of five transgenic lines confirmed through PCR showed positive hybridization bands of the AtHSP101 cDNA through Southern blot analysis. The presence of AtHSP101 transcripts in the three transgenic broccoli lines indicated by reverse transcription-PCR (RT-PCR) confirmed the expression of the gene. In conclusion, an improved regeneration system has been established from hypocotyl explants of broccoli followed by successful transformation with AtHSP101 for resistance to high temperature.
    Matched MeSH terms: Thiadiazoles/pharmacology
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