Furamido benzothiazole 유도체에 관한 연구 : 6 Substituted-2-furamido benzothiazoles의 합성 및 향균시험 Synthesis and Antibacteral Activity of 6-Substituted-2Furamido-Benzothiazoles

임철부 中央醫學社 1973 中央醫學 Vol.24 No.2

The discovery of antibacterial and anti fungal activity in 2, 6-disubstituted benz othiazoles and furane derivatives ' suggested that some more new antimicrobial substances may also be found from the benzothiazole derivatives possessing furoyl group. In order to find newer benzothiazole derivatives possessing antibacterial and antifungal activity, fourteen new 2-furamido-6-substituted benzothiazoles were synthesized and evaluated for their antibacterial activity against staphylococcus aureus, (β-strepto coccus and Escherichia coli. These compounds generally showed strong growth-inhibitory activity against (β-streptococcus, and some of compounds (VIII, IX, X, VIV) showed growth inhibition against staphylococccus aureus in 10 pg/ml concentration.

N-치환 Piperazino Ciprofloxacin 誘導體의 合成 및 抗菌作用

任哲夫,韓完植 중앙대학교 약학연구소 1993 약학 논총 Vol.7 No.-

In order to find more potent antimicrobial agents, fourteen new 1-clyclo-propyl-6-fluoro-1,4-dihydro-4-oxo-7-[4-(N-substituted)-1-piperazinyl]-3-quinoline carboxylic acid derivatives(R=methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, phenyl, 2,4-dimethoxy phenyl) and their pivaloyloxymethyl esters were synthesized and evaluated for their antimirobial activities. Treatment of isocynates with 1-cyclopropyl-6-fluoro-1,4-digydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid[Ciprofloxacin]afforded N-substitued carbamoyl piperazino quinoline carboxylic [acids(1)-(8)]. Their pivaloyloxymethyl esters were obtained by the reaction of N-substitued ciprofloxacins with pivaloyloxymethyl chloride in the presence of potassium carbonate and potassium iodide[(9)-(14)]. The synthesized compounds were examined their antimicrobial activities in vitro against Streptococus pyogenes 77 A, Streptococcus faecium MD 8, b, Staphylococcus aureus SG 511, Escherichia coli 1507 E, Pseudomonas aeruginosa 1711 M, Pseudomonas aeruginosa 1592 E, Salmonella typhimurium, Klebsiella oxytoca 1082 E, Klebsiel la aerogenes 1522 E, Enterobacter cloacae 1321 E. 1. The most active compound [12], 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-[4-(N-isopropyl carbamoyl)-1-piperazinyl]-3-quinoline, carboxylic acid pivaloyoxymethyl ester, exhibited the growth inhibitory activity at a concentration of 0.5㎍/ml against St.pyogenes 77 A, 1.0㎍/ml against St.faecium MD 8b, 1.0㎍/ml against Staphylococcus aureus SG 511, 0.06㎍/ml against Escherichia coli 1507 E, 0.25㎍/ml aginst Peudomanas aeruginosa 1711 M, 0.25㎍/ml against Pseudomonas aeruginosa 1592 E, 0.25㎍/ml against Salmonella typhimurium, 0.06㎍/ml against Klebsiella oxytoca 1082 E, 0.06㎍/ml against Klebsiella aerogenes 1522 E, 0.25㎍/ml against Enterobacter cloacae 1321 E. 2. Most synthesized carbamoyl piperazino ciprofloxacins showed more potent antimicrobial activities than those their pivaloyloxymethyl esters.

Benzothiazole Bivalent Ligand 화합물의 합성

임철부,임채욱,이인숙 중앙대학교 약학연구소 1994 약학 논총 Vol.8 No.-

Twelve new bivalent ligands, that contain two benzothiazoles connected by a succinyl or a succinyl bisoligoglycyl chain in a molecule, were prepared and evaluated for antimicrobial activity. Compound[6], N, N' -succinyl bis(6-bromo-2-aminobenzothiazole) showed potent antifungal activity against M. canis and T.mentagrophytes. Compound[9],[12],[13]and [14]inhibited the growth of M. phlei at the concentration of 62.5㎍/ml.

Benzothiazolyl Biguanides의 합성

임철부,이인숙,임채욱 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-

In order to find new antimicrobial agents, twelve new alkylene bis benzothiazolyl biguanides and eight benzothiazoly biguanides were synthesized. The treatment of alkylenediamines·2HCI with sodium dicyanamide afforded alkylene bis cyanoguanidines. Alkylene bis benzothiazolyl biguanides were synthesized by the reaction of alkylene bis cyanoguanidines with 2-aminobenzothiazole. Benzothiazolyl biguanides were obtained from N-cyanoheterocyclylamidines and 2-aminobenzothiazoles through the similar procedures.

2-Benzothiazolylthiosemicarbazide 유도체의 항균작용에 관한 연구

임철부 中央醫學社 1979 中央醫學 Vol.37 No.5

N-Arly Quinoline Carboxamide유도체의 합성 및 항균작용에 관한 연구

임철부 中央醫學社 1979 中央醫學 Vol.37 No.5

Benzothiazolyl Biguanides의 항미생물작용

임철부,이인숙,임채욱 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-

The twenty benzothiazolyl biguanides synthesized were evaluated for their antimicrobial activities against Staphylococcus aureus. Bacillus subtilis, Mycobacterium phlei, Escherichia coli, Microsporium canis, Candida albicans, Sporothrix schenkii and Trichophyton mentagrophytes. The results obtained were as follow : The most active compound, 1,6-bis{N^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido} hexane·2HCI (14) showed the growth inhibitory activity against S. aureus at the concentration of 7.81ug/mL, against B.subtilis at 15.63ug/mL and against M. phlei at 31.25ug/mL. 1,6-Bis {N^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido} hexane·2HCI(14), 1,6-Bis{N^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido) hexane·2HCI (15) and N-(6-chlorobenzothiazol-2-yl)-1-piperidinylamidinoamidine·HCI (24) inhibited the growth of M. phlei at the concentration of 31.25ug/mL respectively. 1,4-Bis{N^5-(6-methylbenzothiazol-2yl)-N^1-biguanido}butane·2HCI(9) and 1,4-bis{N^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido}butane·2HCI(11) exhibited the antimicrobial activity against B.subtilils at the concentration of 31.25ug/mL. Twelve new biguanide compounds showed growth inhibitory activities against C. albicans at the concentration of 400ug/mL.

Alklthiocarbamylpiperazine 유도체의 합성 및 항균작용

임철부,이상필 중앙대학교 약학연구소 1991 약학 논총 Vol.5 No.-

The twelve new alkylthiocarbamylpiperazine derivatives and six alkythiocarbamylmorpholine derivatives were synthesized and evaluated for their antimicrobial activities. 1,4-Bis(N-alkythiocarbamyl) piperazines were prepared by treating piperazine with alkylisothiocyanates, which were obtained by the reaction of alkylamines with carbondisulfide, sodiumhydroxide, ethyl chloroformate. The treatment of 1-methylpiperazine with alkylisothiocyanates yielded 1-methyl-4-(N-alkylthiocarbamyl) piperazines. 4(N-alkylthiocarbamyl) morpholines were also synthesized by the reaction of morpholine with alkylisothiocyanates. Antimicrobial activities of the synthesized compounds were examined in vitro against Mycobacterium phloei, Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis and Escherichia coli. The results obtained were as follow : The most active compounds(XX, XXⅡ, XXⅢ, XXⅥ) showed the growth inhibitory activity against S. aureus at the concentration of 7.82㎍/㎖. 1,4-Bis(N-n-propylthiocarbamyl) piperazine(X) and 1,4-Bis(N-n-butylthiocarbamyl) piperazine(XⅡ) showed the growth inhibitory activity against B. subtilis at the concetration of 31.25㎍/㎖, respectively. 1-Methyl-4(N-n-butylthiocarbamyl) piperazine(XⅧ) exhibited the growth inhibitory activity against M. phlei at the concentration of 15.63㎍/㎖.

Quinolone-3-Carboxylic Acid계 항균제의 합성 연구

임철부 중앙대학교 약학연구소 1990 약학 논총 Vol.4 No.-

In an effort to find more potent antimicrobial substances, eight bivalent ligands containing enoxacin pharmacophore were prepared and evaluated for their antimicrobial activities. Theatment of enoxacin[1-ethyl-6-fluoro- 1.4-dihydro- 4-oxo-7-(1-piperdzinyl)-1.8-naphthyridine- 3-carboxylic acid] with active ester of alkane (or alkene) dioyl bisoligoglycine afforded eight dicarboxylic acid bis(oligoglycyl enoxacin)s. As a result of this study, N.N'-oxalyl bis(glycyl enoxacin) (1) and N · N'-malongylbis(glycyl enoxacin) (2) were found to show the most potent in vitro antibacterial activities.

新 抗微生物劑에 關한 硏究(Ⅰ) : 2-Benzothiazolylthiosemicarbazide 誘導體의 合成 Synthese of 2-Benzothiazolylthiosemicarbazide

任哲夫 中央醫學社 1975 中央醫學 Vol.29 No.1

Clean water supply is still remained as one of the most important problem for the prevention of water borne diseases in Korea as in other developing countries. Actually in Seoul, densely populated capital of Korea, about- ten percent (10 %) of inhabitants are using untreated well water as the drinking water source. A sanitary survey was carried out on 16 pump wells, 15 wells without lid, and 10 springs in Jungneung-dong area where a foot of Mt. Puk-Ak is located in. In this study, a special emphasis was given to the water temperature, acidity. consumption of KMnO4, hardness, Ammonia-nitrogen, coliform group bacilli, and chlorine demand of the sample waters to investigate potability. The results obtained were as follow; 1) Average values of the water tested were 6.6(pH), 3.36ppm (KMnO4 consumed), 192. 7 (hardness of well waters), and 10. 1ppm (hardness of spring water) respectively. 2) The quantitative analyze for Ammonia-nitrogen revealed 75.6%, coliform group 73.17%, and chlorine demand 05. 1.Oppm in 50% of samples. 3) There was a significant relationship between the Ammonia-nitrogen positive rate and the coliform group positive rate, that is 68. 2% of total samples showed positive in both the coliform group bacilli detection and the Ammonia-Nitrogen detection.