- Effect of photodynamic antibacterial chemotherapy combined with antibiotics on Gram-positive and gram-negative bacteria
-
The well-known and rapidly growing phenomenon of bacterial resistance to antibiotics is caused by uncontrolled, excessive and inappropriate use of antibiotics. One of alternatives to antibiotics is Photodynamic Antibacterial Chemotherapy (PACT). In the present study, the effect of PACT using a photosensitizer Rose Bengal alone and in combination with antibiotics including methicillin and derivatives of sulfanilamide synthesized by us was tested against antibiotic-sensitive and antibiotic-resistant clinical isolates of Gram-positive S. aureus and Gram-negative P. aeruginosa. Antibiotic-sensitive and resistant strains of P. aeruginosa were eradicated by Rose Bengal under illumination and by sulfanilamide but were not inhibited by new sulfanilamide derivatives. No increase in sensitivity of P. aeruginosa cells to sulfanilamide was observed upon a combination of Rose Bengal and sulfanilamide under illumination. All tested S. aureus strains (MSSA and MRSA) were effectively inhibited by PACT. When treated with sub-MIC concentrations of Rose Bengal under illumination, the minimum inhibitory concentrations (MIC) of methicillin decreased significantly for MSSA and MRSA strains. In some cases, antibiotic sensitivity of resistant strains can be restored by combining antibiotics with PACT.
- Ilizirov, Yana,Formanovsky, Andrei,Mikhura, Irina,Paitan, Yossi,Nakonechny, Faina,Nisnevitch, Marina
-
-
- Pyrrole and pyrazole compound of preparation and use as medicaments (by machine translation)
-
The invention relates to the field of medical technology, this invention has offered a kind of sulfonamide and nitrogen mixed uncle butane pyrrole and pyrazole compound, including optical isomers, racemic modification, and any combination of the trans isomer or a pharmaceutically acceptable salt thereof, having a structure of formula (I); the invention also provides the preparation method of the compound and its application, in particular in the preparation of anti-tumor drug application. (by machine translation)
- -
-
Paragraph 0091; 0092; 0093; 0094
(2018/03/26)
-
- Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors
-
Novel 2-chloro-4-anilino-quinazolines designed as EGFR and VEGFR-2 dual inhibitors were synthesized and evaluated for inhibitory effects. EGFR and VEGFR-2 are validated targets in cancer therapy and combined inhibition might be synergistic for both antitumor activity and resistance prevention. The biological data obtained proved the potential of 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors, highlighting compound 8o, which was approximately 7-fold more potent on VEGFR-2 and approximately 11-fold more potent on EGFR compared to the prototype 7. SAR and docking studies allowed the identification of pharmacophoric groups for both kinases and demonstrated the importance of a hydrogen bond donor at the para position of the aniline moiety for interaction with conserved Glu and Asp amino acids in EGFR and VEGFR-2 binding sites.
- Barbosa, Maria Letícia De Castro,Lima, Lídia Moreira,Tesch, Roberta,Sant'Anna, Carlos Mauricio R.,Totzke, Frank,Kubbutat, Michael H.G.,Sch?chtele, Christoph,Laufer, Stefan A.,Barreiro, Eliezer J.
-
-
- SUBSTITUTED PYRAZOLE ANALOGUES AS RAR ANTAGONISTS
-
The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.
- -
-
Page/Page column 17
(2013/05/22)
-
- PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS
-
The present invention relates to compounds II useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.
- -
-
Page/Page column 101-102
(2011/02/24)
-
- Microwave-assisted efficient methylation of alkyl and arenesulfonamides with trimethylsulfoxonium iodide and KOH
-
A solvent-free synthesis of N-methyl and N,N-dimethylsulfonamides has been achieved by treating the primary and secondary sulfonamides with Me3S+OI- and KOH under microwave irradiation on alumina support. Copyright Taylor & Francis Group, LLC.
- Malik, Sarika,Nadir, Upender K.,Pandey, Pramod S.
-
p. 3074 - 3081
(2008/12/22)
-
- TRIAZOLE COMPOUNDS AS LIPOXYGENASE INHIBITORS
-
There is provided compounds of formula (I) wherein W is an optionally substituted aryl or heteroaryl group, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15- lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
- -
-
Page/Page column 41
(2008/06/13)
-
- BIFUNCTIONAL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
-
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional hetercyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.
- -
-
Page/Page column 312-313
(2010/02/06)
-
- AROMATIC AMIDES
-
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
- -
-
-
- Cyclopentanoindoles, compositions containing such compounds and methods of treatment
-
Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
- -
-
-
- Therapeutic heterocycles
-
A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
- -
-
-
- Neuropeptide Y antagonists
-
The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
- -
-
Page column 37
(2010/02/05)
-
- 4-Aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases
-
This invention is directed to aminothiazole compounds of formula (I) wherein R1 is a substituted or unsubstituted group selected from : C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; C1-6-alkoxyl; C1-6-alcohol; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; carbonyl; ether; (C1-6-alkyl)-carbonyl; (C1-6-alkyl)-aryl; (C1-6-alkyl)-cycloalkyl; (C1-6-alkyl)-(C1-6-alkoxyl); aryl-(C1-6-alkoxyl); thioether; thiol; and sulfonyl; wherein when R1 is substituted, each substituent independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol, thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; and R2 is a carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, ring structure having a substituent at the position adjacent to the point of attachment, which ring structure is optionally further substituted, where each substituent of R2 independently is a halogen; haloalkyl; C1-6-alkyl; C1-6-alkenyl; C1-6-alkynyl; hydroxyl; C1-6-alkoxyl; amino; nitro; thiol; thioether; imine; cyano; amido; phosphonato; phosphine; carboxyl; thiocarbonyl; sulfonyl; sulfonamide; ketone; aldehyde; ester; oxygen; carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, cycloalkyl; or carbocyclic or heterocyclic, monocyclic or fused or non-fused polycyclic, aryl; or a pharmaceutically acceptable salt of a compound of formula (I), or a prodrug or pharmaceutically active metabolite of a compound of formula (I) or pharmaceutically acceptable salt thereof, for inhibiting cyclin-dependent kinases (CDKs), such as CDK1, CDK2, CDK4, and CDK6. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds and to methods of treating malignancies and other disorders by administering effective amounts of such compounds.
- -
-
Example C(109)
(2010/11/29)
-
- Azo coupling of o- and p-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid in citrate-phosphate buffer solution
-
Dependences of the partial rate constants for azo coupling of o-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid (N-Acetyl-I-acid) on the fraction of the dianionic form of the latter indicate considerable steric hindrances to the second stage of the reaction. Ionization of the hydroxy group of N-acetyl-I-acid gives rise to additional electrostatic repulsion at the stage of formation of the σ complex, which reduces the rate of azo coupling at the 3-position of orthanilic acid.
- Kornev,Zheltov
-
p. 962 - 968
(2007/10/03)
-
- 4-Sulfonamidoanilide tertiary carbinols: A novel series of potassium channel openers
-
Sulfonamides are viable replacements for the phenylsulfonyl and benzoyl moieties initially described for the anilide tertiary carbinol series of K(ATP) potassium channel openers. The SAR of this new series and the synthetic chemistry employed to generate its members are described.
- Empfield,Mayhugh,Ohnmacht,Frank,Grant,Li
-
p. 775 - 778
(2007/10/03)
-
- 1,2-Diarylpyrroles as potent and selective inhibitors of cyclooxygenase- 2
-
Series of 1,2-diarylpyrroles has been synthesized and found to contain very potent and selective inhibitors of the human cyclooxygenase-2 (COX-2) enzyme. The paper describes short and practical syntheses of the target molecules utilizing the Paal-Knorr reaction. Electrophilic substitution on 1 proceeds in a regioselective fashion, and the method was used to generate a number of tetrasubstituted pyrroles. Detailed SAR on the series has been studied by modifications of the aryl rings and the substituents in the pyrrole ring. Diarylpyrrole 1 is a very potent (COX-2, IC50 = 60 nm) and selective (COX-1/COX-2 = > 1700) inhibitor whereas the isomeric 2 is completely inactive against COX-2. Modifications of the substituents on the fluorophenyl ring in 1 yields very potent inhibitors of COX-2 (IC50 = 40- 80 nm) with excellent selectivity(1200 to >2500) vs COX-1, Analog 20 containing a sulfonamide group is an excellent inhibitor of COX-2 with an IC50 of 14 nm. Tetrasubstituted pyrroles containing groups such as COCF3, SO2CF3, or CH2OAr at position 3 in the pyrrole ring give excellent inhibitors (COX-2, IC50 = 30-120 nm). In vivo testing in the carrageenan- induced paw edema model in the rat establishes that the 1,2-diarylpyrroles are orally active antiinflammatory agents. Compound 3 is the most potent inhibitor of edema with an ED50 of 4.7 mpk.
- Khanna, Ish K.,Weier, Richard M.,Yu, Yi,Collins, Paul W.,Miyashiro, Julie M.,Koboldt, Carol M.,Veenhuizen, Amy W.,Currie, Jerry L.,Seibert, Karen,Isakson, Peter C.
-
p. 1619 - 1633
(2007/10/03)
-
- Aminosulfonylphenyl compounds for treating urinary incontinence
-
Compounds of formula I STR1 wherein R 1, R 2, R 3, R 4, R 5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
- -
-
-
- Syntheses of N4-(Alkyl or arylsulfonyl)sulfanilyl Derivatives
-
2,4-Dichloro, 2,5-dichloro and 3,4-dichloro-benzene-sulfanilides react with chlorosulfonic acid at low temperature to give good yields of the corresponding dichlorobenzenesulfonyl sulfanilyl chlorides.A number of chlorides have been converted into derivatives by reaction with nucleophiles, such as dimethylamine, hydrazine and sodium azide.N4-Acetamidobenzenesulfonylsulfanilyl derivatives have been prepared by the condensation of N4-acetylsulfanilyl chloride with the appropriate sulfanilyl derivative.Methylsulfonanilide reacts with chlorosulfonic acid to give N4-(methylsulfonyl)sulfanilyl chloride.The compounds have been tested for their antibacterial and antifungal activity.
- Cremlyn, R. J.,Swinbourne, F. J.,Devlukia, P.,Shode, O.
-
p. 249 - 253
(2007/10/02)
-
