SYNTHESIS, IDENTIFICATION AND ANTIBACTERIAL EVALUATION OF SOME 1,3,4- OXADIAZOLES DERIVATIVE ON 1,8-NAPHTHYRIDINE RING
Journal Title: WORLD JOURNAL PHARMACY AND PHARMACEUTICAL SCIENCE - Year 2017, Vol 6, Issue 9
Abstract
Several 1,8-naphthyridine derivative were prepared using Vilsmeier-Haack synthization. 2-chloro-3-formyl-1,8-naphthyridine was synthesized by reacting N-(pyridin-2-yl) acetamide with POCl3 in dimethylformamide. 1,8-naphthyridine group was oxidized with NIS-K2CO3 in methanol at room temperature to yield 2-chloro-3-methoxy carbonyl -1,8-naphthyridine (2), acid hydrazide was then prepared by treating the methyl ester with hydrazine hydrate in ethanol (3), the synthesis of 2-chloro-3[2(1,3,4-oxadiazol-5-thiol-1,8-naphthyridine (4) was obtained from compound(3) reaction with CS2 in basic medium, acid hydrazide was then converted to the corresponding carbothioamide (5) by treating with benzyl isothiocyanate respectively. Thiosemicarbazide (5) was reacted with mercuric oxide in methanol to produce 1,3,4-oxadiazole (6). 2-chloro-3-[2(1,3,4-oxadiazole)]-1,8-naphthyridine (8) was yielded from acid hydrazide reaction with formic acid followed by PbO2. Acid hydrazide (3) was treated with benzaldehyde to formhydrazone (9) which then reacted with PbO2 to give 1,3,4-oxadiazole (10). Finally. The structures of synthesized compounds were confirmed spectroscopically using IR and1HNMR in addition to another physical data. The newly synthesized compounds (4,6,8,10) show a significant antibacterial activity.
Authors and Affiliations
Mohanad Y. Saleh
Keywords
Related Articles
- EP ID EP618660
- DOI -
- Views 159
- Downloads 0
POSTMENOPAUSAL BLEEDING CLINICAL GUIDELINE; RISK AND INVESTIGATION PROSPECTIVE STUDYPOSTMENOPAUSAL BLEEDING CLINICAL GUIDELINE; RISK AND INVESTIGATION PROSPECTIVE STUDY
Postmenopausal uterine bleeding is defined as uterine bleeding after permanent cessation of menstruation resulting from loss of ovarian follicular activity. Bleeding can be spontaneous or related to ovarian hormone repla...
IRRITABILITY IN SKIN WITH PRODUCTS WITH MENTHOL AND CAMPHOR. BASE TEST
A study was conducted to determine the sensitizing effect of ointments and possible dermal irritability. The study was carried out in albino rabbits by the general method of irritability in skin analysis using the techni...
BIOCHEMICAL STUDY ON THE REGENERATIVE EFFECT OF CHROMIUM PICOLINATE ON EXPERIMENTALLY INDUCED DIABETES
In the present study, the potential therapeutic effect of Chromium picolinate administration diabetic rats was evaluated. Thirty male albino rats were divided into three equal groups of 10 rats each. Group Ι :( Control g...
CHARAK’S CHATURVIMSHATI UPKRAMA AND ITS CONTEMPORARY VIEW
Poison has been polluting human and non-human forms since antiquity. Our acharyas had given a separate place for Agadtantra that deals with the management of animate and inanimate poisoning. Since ancient time Agadtantra...
IDENTIFICATION OF FATTY ACIDS AND FATTY ACID ESTERS FROM ETHYL ACETATE BARK EXTRACT OF HOLOPTELEA INTEGRIFOLIA (ROXB.) PLANCH BY GC-MS
It is an ornamental plant with certain medicinal characteristics due to many valuable and active Phytoconstituents in various parts of the plant. Ethyl acetate extract of the bark was triturated with warm n-hexane and wa...