138385-04-3Relevant academic research and scientific papers
Synthesis of Bi-heterocyclic sulfonamides as tyrosinase inhibitors: Lineweaver-burk plot evaluation and computational ascriptions
Abbasi, Muhammad Athar,Aziz-Ur-Rehman,Hassan, Mubashir,Nazir, Majid,Raza, Hussain,Seo, Sung-Yum,Shah, Syed Adnan Ali,Siddiqui, Sabahat Zahra,Zia-Ur-Rehman
, p. 403 - 414 (2020/07/31)
The designed bi-heterocyclic sulfonamides were synthesized through a two-step protocol and their structures were ascertained by spectral techniques including IR, 1H NMR and 13C NMR along with CHN analysis. The in vitro inhibitory effects of these sulfonam
Synthesis, Structural Analysis, and Screening of Some Novel 5-Substituted Aryl/Aralkyl-1,3,4-Oxadiazol-2-Yl 4-(Morpholin-4-Ylsulfonyl)Benzyl Sulfides As Potential Antibacterial Agents
Aziz-Ur-Rehman,Gul, Samreen,Abbasi, Muhammad Athar,Nafeesa, Khadija,Akhtar, Muhammad Nadeem,Ahmad, Irshad,Afzal, Saira
, p. 1045 - 1055 (2015/08/04)
A series of new 5-substituted aryl/aralkyl-1,3,4-oxadiazol-2-yl 4-(morpholin-4-ylsulfonyl)benzyl sulfides 6a-k were synthesized by converting multifarious aryl/aralkyl organic acids 1a-k successively into corresponding esters 2a-k, hydrazides 3a-k, and 5-substituted aryl/aralkyl-1,3,4-oxadiazole-2-thiols 4a-k. Finally, the target compounds, 6a-k were prepared by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with 4-(4-(bromomethyl)phenylsulfonyl) morpholine (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the newly synthesized compounds were elucidated by spectroscopic techniques. In addition, the antibacterial activity of all the synthesized compounds was investigated in vitro against Gram-positive and Gram-negative bacteria by using ciprofloxacin as reference standard drug and the results showed that some of the tested compounds possessed good antibacterial activity.
Synthesis and initial biological evaluation of new mimics of the LXR-modulator 22(S)-hydroxycholesterol
?strand, O. Alexander H.,Sandberg, Marcel,Sylte, Ingebrigt,G?rbitz, Carl Henrik,Thoresen, G. Hege,Kase, Eili T.,Rongved, P?l
, p. 643 - 650 (2014/01/17)
The generic, synthetic oxysterol 22(S)-hydroxycholesterol (22SHC) has shown antagonistic effects towards liver X receptor (LXR) in vitro and promising effects on plasma triacylglycerol level and body weight-gain in animal studies.1,2 On the contrary, the endogenic LXR agonist 22(R)-hydroxycholesterol (22RHC) and synthetic LXR agonists convincingly have shown agonistic effects on genes involved in lipogenesis, and inhibitory effects on cell proliferation in vitro and in vivo.3 We hypothesized that the carbon side chain containing the hydroxyl group at the 22-position was a pharmacophore affecting these opposite effects on LXR. This prompted us to initiate a rational drug design incorporating the 22-hydroxylated 20-27 cholesterol moiety into cholesterol-mimicking building blocks. The two enantiomers of the 22-hydroxylated 20-27 cholesterol moiety were synthesized with an excellent enantiomeric excess and the stereochemistry are supported by X-ray crystallography. Molecular modelling of the new compounds showed promising LXR selectivity (LXRβ over LXRα) and initial in vitro biological evaluation in human myotubes showed that compound 16b had agonistic effects on the gene expression of SCD1 and increased lipogenesis.
Rhodium-catalyzed cross-coupling reaction of arylboronates and diazoesters and tandem alkylation reaction for the synthesis of quaternary r,r-heterodiaryl carboxylic esters
Tsoi, Yuk-Tai,Zhou, Zhongyuan,Yu, Wing-Yiu
supporting information; experimental part, p. 5370 - 5373 (2011/12/03)
A rhodium-catalyzed one-pot three-component coupling reaction was developed for the synthesis of quaternary α,α-heterodiaryl carboxylic esters. This reaction involves cross-coupling of the arylrhodium(I) complexes with R-aryldiazoacetates to form oxa-π-al
Design, synthesis, and invitro antifungal activity of 1-[(4-substituted-benzyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols
Guillon, Remi,Pagniez, Fabrice,Giraud, Francis,Crepin, Damien,Picot, Carine,LeBorgne, Marc,Morio, Florent,Duflos, Muriel,Loge, Cedric,LePape, Patrice
experimental part, p. 816 - 825 (2012/01/06)
As part of our studies focused on the design of 1-[((hetero)aryl- and piperidinylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents, we report the development of new extended benzylamine derivatives substituted at the para p
Palladium-catalyzed cross coupling reaction of benzyl bromides with diazoesters for stereoselective synthesis of (E)-α,β-diarylacrylates
Yu, Wing-Yiu,Tsoi, Yuk-Tai,Zhou, Zhongyuan,Chan, Albert S. C.
supporting information; experimental part, p. 469 - 472 (2009/07/11)
(Chemical Equation Presented) A Pd-catalyzed cross-coupling reaction of benzyl bromides with α-aryldiazoesters is described, and E-α,β-diarylacrylates were obtained in good yields and excellent E-to-Z selectivity (>20:1).
QUINOLINES AND THEIR THERAPEUTIC USE
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Page/Page column 132, (2008/06/13)
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1- C6fluoroalkyl, cyclopropyl, halo, -S(O)nR6, -SO2NR7R8, -NR7R8, -NR7C(O)R6, -CO2R7, -C(O)NR7R8, -C(O)R6, -NO2, -CN or a group -OR9; wherein each R6 is independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group -SO2R6; A is -CHR10-, -C(O)-, -S(O)n-, -0-, or -NR10- wherein n is an integer from 0-2 and R10 is hydrogen, C1-C3alkyl, or C1-C6fluoroalkyl group; B is a direct bond, or a divalent radical selected from -CH2-, -CH2CH2-, -CHR11-, -CR11R12-, -CH2CHR11-, -CH2CR11R12-, -CHR11CHR12-, and divalent radicals of formula -(CR11R12)P-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -NH-, or -S(O)n-, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(=O)NHSO2R6or SO2NHC(=O)R6; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.
ORGANIC COMPOUNDS
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Page/Page column 26, (2008/06/13)
There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing t
BICYCLIC HΞTEROYCLIC COMPOUNDS AS ANTIINFLAMMATORY AGENTS
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Page/Page column 23, (2010/11/27)
There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for preparin
