排序方式: 共有54条查询结果,搜索用时 15 毫秒
1.
2.
Mubashir Hassan Balasaheb D. Vanjare Kyou-Yeong Sim Hussain Raza Ki Hwan Lee Saba Shahzadi Andrzej Kloczkowski 《Molecules (Basel, Switzerland)》2022,27(5)
A series of nine novel 1,2,4-triazole based compounds were synthesized through a multistep reaction pathway and their structures were scrutinized by using spectral methods such as FTIR, LC-MS, 1H NMR, and 13C NMR. The synthesized derivatives were screened for inhibitory activity against the mushroom tyrosinase and we found that all the synthesized compounds demonstrated decent inhibitory activity against tyrosinase. However, among the series of compounds, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide exhibited more prominent activity when accompanied with the standard drug kojic acid. Furthermore, the molecular docking studies identified the interaction profile of all synthesized derivatives at the active site of tyrosinase. Based on these results, N-(4-fluorophenyl)-2-(5-(2-fluorophenyl)-4-(4-fluorophenyl)-4H-1,2,4-triazol-3-ylthio) acetamide could be used as a novel scaffold to design some new drugs against melanogenesis. 相似文献
3.
Satish Balasaheb Nimse Junghoon Kim Keum-Soo Song Chan-Yong Jung Sudhakara Reddy Seelam 《Tetrahedron letters》2010,51(21):2840-551
We report the new water-soluble aminocalix[4]arene hosts 1 and 2 with deep hydrophobic cavity facilitating hydrophobic mouth and hydrophilic mouth, respectively. The 1H NMR titrations revealed that host 1 shows high selectivity for neutral guests 9 and 10, with log K of 4.2 and 4.6, respectively. The host 2 shows log K of 4.9 for binding with guest 15. Moreover, the binding ability of the host 2 for guest 14 is stronger by a factor of 1000 than that of the host 1. 相似文献
4.
Toche RB Janrao RA Bagul SM Patil SP Pagar BP Nikam PS 《Journal of fluorescence》2011,21(4):1617-1624
Suzuki-Miyaura cross coupling was successfully used for C5-arylation in 4-amino-2-chloroquinoline-3-carbaldehyde using arylbornic acid and tetrakistriphenylphosphine palladium catalyst in water. Friedländer condensation reaction on 4-amino-2-chloro/2-arylquinoline-3-carbaldehyde and aromatic ketones gave novel aryl and diarylbenzo[h] [1, 6]naphthyridines in good yields. Fluorescence quantum yields were increased by introducing C2 and C5 π donor aryl benzo[h][1, 6]naphthyridines derivatives. 相似文献
5.
Satish Balasaheb Nimse Junghoon Kim Van-Thuan Nguyen Chan-Yong Jung Taisun Kim 《Tetrahedron letters》2010,51(47):6156-6160
The pH of a solution shows a significant effect on the dynamics of the gate (formed by eight benzylic functions) and portal on the hydrophobic cavity of receptor. At pH 5.8 the gate closes and prohibits the entry of anionic guests. However, at pH 7.3 the gate opens and allows the entry of anionic guests into the hydrophobic cavity. It is the first time that anionic receptor efficiently recognizes anionic guests. 相似文献
6.
Katkar Santosh Shriram Lande Machhindra Karbhari Arbad Balasaheb Ramrao Gaikwad Suresh Tukaram 《中国化学》2011,29(1):199-202
4H‐Benzo[b]pyrans was synthesized under reflux condition in ethanol via condensation of benzaldehyde, malononitrile and dimedone with ZnO‐beta zeolite as an inexpensive and effective catalyst. The key features of the reported protocols are good to excellent yields, short reaction time and recovery and reusability of catalytic material. 相似文献
7.
Satish Balasaheb NimseJunbae Kim Keum-Soo Song Junghoon Kim Jeong Tae LeeVan-Thuan Nguyen Van-Thao TaTaisun Kim 《Tetrahedron letters》2011,52(29):3751-3755
In this Letter, the role of the depth of the cavity in the recognition processes of the guests by the hosts has been investigated. The hosts 2, 3 interact with both the cationic function and the aromatic moiety in the guests 5, 6 but with a slight preference for the cationic functions. The host 4 selectively recognizes the trimethylammonium functions of the guests 5 and 6. However, the host 1 selectively recognizes the aromatic moiety of the ditopic trimethylammonium guests 5 and 6. The recognition and orientation of the guest in the cavity of the host are directly dependent on the depth of the hydrophobic cavity of the host. 相似文献
8.
Bharat B. Kashid Anil A. Ghanwat Vijay M. Khedkar Balasaheb B. Dongare Mubarak H. Shaikh Prathmesh P. Deshpande Yogesh B. Wakchaure 《Journal of heterocyclic chemistry》2019,56(3):895-908
A series of novel 2‐substituted benzimidazole and benzoxazole derivatives as a potential antimicrobial and antioxidant agent were synthesized via coupling of N‐methyl‐o‐phenylenediamine or 2‐amino‐phenol with aromatic aldehyde and acid in the presence of polyphosphoric acid as an efficient catalyst as well as solvent by conventional method in short reaction times with excellent yield. The newly synthesized benzimidazole and benzoxazole derivatives were evaluated for antimicrobial and antioxidant activity and exhibited excellent to good activities compared to the standard drugs. Furthermore, the theoretical predictions based on molecular docking against microbial DNA gyrase could provide an insight into the plausible mechanism of action and establish a link between the observed antimicrobial activity and the binding affinity shedding light on specific thermodynamic (bonded and nonbonded) interactions governing the activity. Furthermore, the synthesized compounds were analyzed for absorption, distribution, metabolism, and excretion properties and exhibited potential properties to build up as good oral drug candidates. 相似文献
9.
Harfmann RG Deshmukh BK Conklin J Turowski M Lynch S 《Journal of AOAC International》2007,90(3):786-793
A collaborative study was performed to determine the reproducibility of a method for the determination of methylcellulose (MC) and hydroxypropyl methylcellulose (HPMC) in food. These widely used food gums possess unusual solubility characteristics and cannot accurately be determined by existing dietary fiber methods. The new method uses the enzyme-digestion procedure of AOAC Official Method 991.43. Digestate solutions must be refrigerated to fully hydrate MC or HPMC. The chilled solutions are filtered and analyzed by size-exclusion liquid chromatography. Collaborating laboratories received 28 samples containing MC or HPMC in the range of 0-100%. The sample set included blind duplicates of 5 food matrixes (bread, milk, fish, potato, and powdered juice drink). Cochran and Grubbs tests were used to eliminate outliers. For food samples containing MC, values for within-laboratory precision, repeatability relative standard deviation (RSDr), ranged from 4.2 to 16%, and values for among-laboratories precision, reproducibility relative standard deviation (RSDR), ranged from 11 to 20%. For HPMC samples, RSDr values ranged from 6.4 to 27%, and RSDR values ranged from 17 to 39%. Recoveries of MC and HPMC from the food matrixes ranged from 78 to 101%. These results show acceptable precision and reproducibility for the determination of MC and HPMC, for which no Official AOAC Methods exist. It is recommended that this method be adopted as AOAC Official First Action. 相似文献
10.
Prasad G. Mahajan Nilam C. Dige Balasaheb D. Vanjare Hussain Raza Mubashir Hassan Sung-Yum Seo Seong-Karp Hong Ki Hwan Lee 《Journal of fluorescence》2018,28(6):1305-1315
Herein, we design and synthesized new fluorescein based derivatives by insitu formation of fluorescein ester and further treated with corresponding hydrazide and amine to yield respective compounds i.e. FB1, FB2, FB3 and FB4. The spectral purity and characterization was done by using IR, NMR and Mass spectroscopies. The synthesized derivatives were examined for their photophysical properties by using variety of organic solvents and results were discussed in details. The structural diversity of synthesized compounds motivate us to evaluate these compounds for urease inhibition. The compound FB3 (IC50?=?0.0456 μM) shows 100 fold more active against Jack bean urease than standard drug thiourea (IC50?=?4.7455 μM). Other synthesized compounds showed potent activity. Free radical percentage scavenging assay further supported the capacity of compounds to urease inhibition. While, molecular docking simulations helps to examine the molecular interactions of active compounds FB1, FB2, FB3 and FB4 within the binding site of urease enzyme. 相似文献