Sulfonamide類의 N⁴-acyl誘導體에 關한 硏究(Ⅰ) : N⁴-Orotylsulfonamide類의 合成과 그 抗菌作用 Synthesis and antibacterial action of the N⁴-orotylsulfonamides

千文宇 대구효성가톨릭대학교 1972 연구논문집 Vol.10 No.1

Orotic acid analogs were reported that they have considerably active antibacterial action and also diminish the toxicity of drugs. In order to diminish the side effects of sulfonamides and increase their antibacterial action on chemotherapy, orotyl radical were introduced to N⁴-position of sulfonamides. Five N⁴-orotyl derivatives of sulfonamides such as N⁴-orotyl-N¹-2-pyrimidinyl sulfanilamide, N⁴-orotyl-N¹-(4-methyl-2-pyrimidinyl) sulfanilamide, N⁴-orotyl-N¹-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N⁴-orotyl-N¹-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N⁴-orotyl-N¹-2-thiazolylsulfanilamide were synthesized. They were obtained by the action of N¹-2-pyrimidinyl sulfanilamide, N¹-(4-methl-2-pyrimidinyl) sulfanilamide, N¹-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N¹-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N¹-2-thiazolylsulfanilamide with orotyl chloride in 4% NaOH solution. Of the above five compounds. N⁴-orotylsulfadiazine and N⁴-orotylsulfamerazine exhibited a considerably good antibacterial action against Staphylococcus aureus 209p.

抗菌性物質의 合成 및 그 抗菌作用에 關한 硏究 : 5-nitrofuran 誘導體의 合成과 그 抗菌作用 Synthesis and antibacterial action of 5-nitrofuran derivatives

千文宇 대구효성가톨릭대학교 1974 연구논문집 Vol.14 No.1

The many studies on the synthesis and antibacterial action of 5-nitrofuran derivatives have been reported in pharmaceutical chemistry field. They reported that the antibacterial action of 5-nitrofuran derivatives depend mostly on the nitro radical of 5-position of furan nucleus and that the introduction of -CH=CH-or-CH=N-groups to the above nitrofuryl group may result to enhance the antibacterial action to some extent. In order to diminish the side effects of 5-nitrofuran derivatives and to obtain notable antibacterial agents, several significant groups which are furyl group, nitrofuryl group, uracil, p-arsanilic acid and morpholine were introduced to the nitrofuran ring, and -CH=CH-, -CH=N- groups also introduced. The six synthesized compounds are (5-nitro-2-furylacryloyl)-5'-nitro-2'-furfuraldoxime(Ⅰ), 5-nitro-2-furfurylidene-(5-nitro-2-furylacryloyl) hydrazone(Ⅱ), 2-furfurylidene-(5-nitro-2-furylacryloyl) hydrazone(Ⅲ), orotic acid-(5-nitro-2-furylacryloyl) hydrazide(Ⅳ), N-(5-nitrofurylacryloyl)-p-arsanilic acid(Ⅵ) and N-(5-nitro-2-furylacryloyl)morpholine(Ⅶ). On the other hand, two compounds which expected the antitubercular action also were synthesized. They are N-(5-nitro-2-furylacryloyl) isonicotinic acid hydrazide(Ⅴ) and Bis-(2-furfurylidene imino) thiourea(Ⅷ). And antibacterial action of the eight synthesized compounds against Staphylococcus aureus 209p, Escherichia coli 0111, salmonella typhi 0901, Shigella Flexineri 2a and Pseudomonas aeruginosa were carried out. Three compounds(Ⅰ,Ⅱ and Ⅳ) exhibited good antibacterial actions against four stains except Pseudomonas aeruginosa, and LD50 determination test against the above three compounds were carried out. And the antitubercular action of the two compounds(ⅤandⅧ) against mycobacterium tuberculosis H37Rv were carried out, but they did not show remarkably the growth inhibition of M. tuberculosis ??Rv at the concentration of 100r/ml.

Sulfonamide類의 N⁴-acyl 誘導體에 關한 硏究(2) : N⁴-2-furylacrylsulfonamide 및 N⁴-2-furoylsulfonamide類의 合成 Synthesis of N⁴-2-furylacrylsulfonamides and N⁴-2-furoylsulfonamides

千文宇 대구효성가톨릭대학교 1973 연구논문집 Vol.12 No.1

Paper I of these studies has previously been reported in this journal. Author wishes to report now the influence of -CH=CH- group on the antibacterial activities. The relationship between the antibacterial activities and the chemical structure of 5-nitrofuran derivatives was reported in many studies. The antibacterial activity of 5-nitro furan derivatives depends mostly on the nitro radical of 5-position of furan ring, but the introduction of -CH=CH-group or-CH=N-group between the nitrofuryl group and the end group of side chain might result to enhance the antibacterial activity to some extent. Author's intrest led to the synthesis of five N4-furylacryl derivatives with -CH=CH-group in their structure and five N4-furoyl derivatives without the above group considering of the possibility of application this-CH=CH-group to the sulfonamides. The antibacterial activity tests will be carried out to compare the five N4-2-furylacry1 derivatives with the five N4-2-furoyl derivatives. Five N4-2-furylacryl derivatives such as N4-2-furylacryl-N1-2-pyrimidinyl sulfanilamide, N4-2-furylacryl-N1-(4-methyl-2-pyrimidinyl) sulfanilamide, n4-2-furylacryl-N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N4-2-furylacryl-N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide, N4-2-furylacryl-N1-2-thyazolylsulfanilamide and five N4-2-furoyl derivatives such as N4-2-furoyl-N1-2-pyrimidinyl sulfanilamide, N4-2-furoyl-N1-(4-methyl-2-pyrimidinyl) sulfanilamide, N4-2-furoyl-N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N4-2-furoyl-N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N4-2-furoyl-N1-thiazolyl sulfanilamide were synthesized. They were obtained by the action of N1-2-pyrimidinyl sulfanilamide, N1-(4-methyl-2-pyrimidinyl) sulfanilamide, N1-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N1-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide and N1-2-thiazolyl sulfanilamide with 2-furylacryl chloride and 2-furoyl chloride in 4% NaOH solution.

Isonicotinic acid hydrazide 誘導體의 合成 및 抗菌作用에 關한 硏究

千文宇 대구효성카톨릭대학 1971 연구논문집 Vol.8 No.1

Isonicotinic acid hydrazde(INAH) is wellknown chemotherapeutics as antubercular agent. And its good antitubercular action was reported by many workers. But that INAH produce the side action such as neuritis by formation Schiff's base with pyridoxine was reported. So in order to diminish this side action, several derivatives of INAH such as Sodium isonicotinic acid hydrazide methanesulfonate(IHMS), D-Glucuronolactone isonicotinyl hydrazone were synthesized and used in therapy of tuberculosis. Author's interst led to the synthesis of three new acyl derivatives of INAH such as N-(3.5-dinitorbenzoyl)-isonicitinic acid hydrazide, N-phenoxyacetyl-isonicotinic acid hydrazide and N-cinnamoyl-isonicotinic acid hydrazide. They were obtained by the action of 3,5-dinitrobenzoyl chloride, phenoxyacetyl chloride and cinnamoyl chloride with isonicotinic acid hydrazide in pyridine solution. And their in vitro antitubercular and antibacterial action test were carried out.

化學療法劑의 對象物로서 Orotic acid hydrazide類의 合成및 그 抗菌作用에 關한 硏究

千文宇 대구효성카톨릭대학 1971 연구논문집 Vol.8 No.1

Since the discovery of the pharmacological properties of orotic acid and its derivatives as antibacterial and antitumor agents, a number of analogs and related antibacterial and alkylating agents which have clinical value have been developed. Especially, uracil was eported as to produce not only the affinity to the tumor cells but also diminish the toxicity of alkylatin groups contained in uracil. Author's intrest led to the synthesis of 9 derivatives of orotic acid hydrazide as potential antibacterial and antitumor agents. Nine new Schiff's base of orotic acid hydrazide were synthesized. They were obtained by the action of o-chlorobenzaldehyde, 2,4-dichlorobenzaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, p-hydroxybenzaldehyde, m-nitrobenzaldehyde. 3.4-dihydroxybenzaldehyde, m-chlorobenzaldehyde, p-anisaldehyde and n-capronaldehyde with orotic acid hydrazide in ethanol solution. And antibacterial activities of the nine synthesized compounds against Salmomella typhiO 901, Staphylococcus aureus 209p, Escherichia coli Olll, Pseudomonas aeruginosa and Shigella flexineri were carried out. All of the nine synthesized compounds exhibited good antibacterial actions against Staphylococcus aureaus only.

"No man's land"에서의 수지 굴근건 손상시 일차 건봉합술의 임상적 고찰

이종문,박승하,김우경,정전은 大韓成形外科學會 1991 Archives of Plastic Surgery Vol.18 No.1

In past years repair of acute flexor tendon injuries in zone Ⅱ developed a poor reputation because of the high frequency of adhesion. More recently with the development of new techniques, especially early controlled mobilization and microscope, the result have improved and direct repair has again come into favor. In this study, 94 digits with complete laceration of the flexor tendon in zone Ⅱ were treated by primary repair and early controlled mobilization. Using the Strickland formula of total active motion of the interphalangeal joints, 64 digits(68%) were rated "excellent" ; 14 digits(15%) were rated "Good" ; 12 digit(13%) were rated "Fair" ; 4 digits(4%) were rated "Poor"

韓國人血液群 A,B,및 AB 赤血球의 被疑集性에 關한 硏究

梁學道,李楨浩,尹秉文,芮薰海,全東雨,李文玉,金晉郁 醫藥係社 1955 綜合 醫學 Vol.12 No.8

항진균제 알릴아민류의 합성과 생물학적 평가

정병호,조원제,천승훈,박면지,유진철,천문우 朝鮮大學校 1998 藥學硏究誌 Vol.19 No.2

For the development of antifungal agents. modification of naftifine which exhibits significant antimycotic activity was performed by replacing the naphthalene ring of it to hetero cyclic rings such as morpholine. benzothiazole. piperidine and pyridine derivatives. The synthesized compounds were tested in vitro antifungal activity against five different fungi with naftifine as a comparative antimycotic molecule. From the biological evaluation two compounds. (E)-N-(3-phenyl-2-propenyl)-N-(4-piperidinylmethyl)amine(3d) and (E)-N-(3-phenyl-2-propenyl)-N-(3-pyndylmethyl)amine(3D) showed relatively noticeable activity(MIC=50㎍/㎖). On the other hand. the other compounds had no activity.

Synthesis of 2-(3' azido- and 3'-amino-3'-deoxy-β-D-ribofuranosyl)-thiazole-4-carboxamide

Chun Moon-Woo,Liang Cheng-Wu,Shin Ji-Hye 大韓藥學會 2003 大韓藥學會 總會 및 學術大會 Vol.2003 No.2

SYNTHESIS OF NOVEL 3´-DEOXY-3´-C-HYDROXYMETHYL NUCLEOSIDES WITH CONFORMATIONALLY RIGID SUGAR MOIETY AS POTENTIAL ANTIVIRAL AGENTS

Chun, Moon Woo,Kim, Myung Jung,Jo, Un Hee,Kim, Joong Hyup,Kim, Hee-Doo,Jeong, Lak Shin 梨花女子大學校 藥學硏究所 2001 藥學硏究論文集 Vol.- No.10

Based on the fact that the ring expanded 3'-C-hydroxymethy analogue of oxetanocin A exhibited potent antiviral activity two types of conformationally rigid 3'-C-hydroxymethyl derivatives in which 2'hydroxyyl group is linked to the 4'-position or to the 6'-position were synthesized starting from 1.2:5.6-di-O-isopropylidene-D-glucose, respectively.