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ABSTRACT:
A series of novel 4-Substituted/Heterocyclic-N-(4-thiomorpholinothieno[3,2-d]pyrimidin-2-yl)benzamide (8aj)derivatives were synthesized by a Five-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The structures of the final compounds were confirmed by IR, NMR, EI-MS. The final compounds were screened for their anti-bacterial activity against Staphylococcus aureus (S. aureus) and Bacillus subtilis (B. subtilis)from Gram positive group of bacteria and Pseudomonas aeruginosa (P. aeruginosa) and Escherichia coli (E. coli)from Gram negative group of bacteria and antifungal activity against Aspergillus niger (A. niger) and Candida albicans (C. albicans). Anti-bacterial and anti-fungal activities were Evaluated and compared with the standard drugsSuch asAmoxicillin &Flucanazole From anti-bacterial and antifungal activity screening results, it has been observed that compounds 8j, 8i, 8e and 8fpossess good activity.
KEYWORDS: Thieno [3, 2-d] Pyrimidine, 2-chloro-4-thio morpholine Thieno[3, 2-d]Pyrimidine synthesis, Anti-bacterial; Anti-fungal activity, HATU.
INTRODUCTION:
ThienoPyrimidine is a bicyclic heterocyclic compound consists of a five membered thiophene ring is fused to a six membered heterocyclic ring with two nitrogen atoms. The fusion may occur in three different orientations that results in three important types of thienopyrimidines namely; Thieno[2,3-d]Pyrimidine (a), Thieno[3,2d]Pyrimidine (b) and thieno[3,4-J]Pyrimidine (c). Thienopyrimidines are a class of fused heterocycles, which are common sources for the development of new potential therapeutic agents. There are three isomeric thienopyrimidines corresponding to the three possible types of annulations of thiophene to the pyrimidine ring: thieno[2,3-íi]pyrimidine, thieno[3,4-^]pyrimidine, and thieno[3,2d]pyrimidine.
The formation of novel fused heterocycles is an important for heterocyclic chemists from various points of view for the development of living things. Furthermore, many condensed heterocyclic systems especially, when linked to a Pyrimidine ring have attracted attention in the past few years as they are found in variety of natural products (eg. purines, pyrrolopyrimidines, pyridopyrimidines, pteridines). Among these heterocycles, the thienopyrimidine class is also of interest because some derivatives such as Tiprinast have been shown to clinically effective antiallergic [1-7]. In addition, antianaphilactic, antineoplastic[8], antiatherosclerotic[9], antibacterial[1017], anti-depressive[18-19], antidiabetic[20], antihypertensive[21-24], antihistaminic[25-26], analgesic, anti-inflammatory[27-44], antiviral[45-46], spasmolytic[47], antipyretic[48-50], anticonvulsant[51], fungicidal[52], antiplatelet[53-55] and other Central Nervous System(CNS) affecting[56] activities have been reported for certain thieno-pyrimidine derivatives.
This work aimed to synthesize some new thieno [3, 2-d] Pyrimidine derivatives starting with methyl 3aminothiophene-2-carboxylateand to evaluate their biological activities. Encouraged by the diverse biological activities of Thieno[3,2-d]Pyrimidine Heterocyclic compounds, it...